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Chemically induced degradation of epigenetic targets

CHEMICAL SOCIETY REVIEWS (2023)

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Article Chemistry, Multidisciplinary

Targeted Degradation of PRC1 Components, BMI1 and RING1B, via a Novel Protein Complex Degrader Strategy

Kwang-Su Park et al.

Summary: The study discovered MS147, the first degrader of PRC1 core components BMI1 and RING1B, through a novel protein complex degradation strategy. MS147 degrades BMI1 and RING1B by binding to an EED small-molecule binder linked to the E3 ligase von Hippel-Lindau (VHL), effectively reducing the level of H2AK119ub and inhibiting the proliferation of cancer cell lines insensitive to PRC2 inhibitors/degraders.

ADVANCED SCIENCE (2023)

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Article Biochemistry & Molecular Biology

Functional E3 ligase hotspots and resistance mechanisms to small-molecule degraders

Alexander Hanzl et al.

Summary: This study utilizes haploid genetics to demonstrate that hotspot mutations cluster in substrate receptors of hijacked ligases, where mutation type and frequency correlate with gene essentiality. The intersection with deep mutational scanning reveals hotspots that are conserved or specific for chemically distinct degraders and targets, and the biophysical and structural validation suggests that hotspot mutations frequently converge on altered ternary complex assembly. Moreover, hotspots mutated in patients that relapse from degrader treatment are validated.

NATURE CHEMICAL BIOLOGY (2023)

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Article Biochemistry & Molecular Biology

CRISPR Screen Reveals BRD2/4 Molecular Glue-like Degrader via Recruitment of DCAF16

Andrea G. Shergalis et al.

Summary: Molecular glues (MGs) are monovalent small molecules that enhance protein-protein interactions. Immunomodulatory drugs and indisulam have been found to exhibit a molecular glue effect. However, the discovery of new MGs remains challenging.

ACS CHEMICAL BIOLOGY (2023)

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Review Biochemistry & Molecular Biology

KATs off: Biomedical insights from lysine acetyltransferase inhibitors

Samuel D. Whedon et al.

Summary: Lysine acetyltransferase (KAT) enzymes are important in modulating chromatin structure and transcription regulation. Recent progress has been made on developing chemical probes for p300 and MYST family of KATs, which can be useful tools for basic and translational research.

CURRENT OPINION IN CHEMICAL BIOLOGY (2023)

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Article Biochemical Research Methods

Design, Synthesis, and Evaluation of Trivalent PROTACs Having a Functionalization Site with Controlled Orientation

Yifan Huang et al.

Summary: Trivalent PROTACs with controlled orientation were designed and synthesized, showing similar activity to the target compound MZ1 by modifying the substitution patterns on the benzene ring and the number of ethylene glycol units. These compounds may serve as efficient platforms for further applications.

BIOCONJUGATE CHEMISTRY (2022)

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Article Chemistry, Multidisciplinary

Discovery of a Covalent FEM1B Recruiter for Targeted Protein Degradation Applications

Nathaniel J. Henning et al.

Summary: This study describes a covalent ligand EN106 that targets FEM IB, an E3 ligase involved in the cellular response to reductive stress. EN106 disrupts the recognition of the reductive stress substrate FNIP1 by targeting C186 in FEM1B. Additionally, EN106 can serve as a covalent recruiter for FEM1B in targeted protein degradation (TPD) applications, leading to the degradation of BRD4 and BCR-ABL when linked to BET bromodomain inhibitor JQ1 or kinase inhibitor dasatinib, respectively.

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2022)

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Article Biochemistry & Molecular Biology

A chemical probe targeting the PWWP domain alters NSD2 nucleolar localization

David Dilworth et al.

Summary: NSD2 is an enzyme responsible for dimethylation of lysine 36 of histone 3, with multiple domains involved in chromatin reading. The chemical probe UNC6934 can modulate NSD2 activity and localization, affecting cellular functions.

NATURE CHEMICAL BIOLOGY (2022)

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Review Biotechnology & Applied Microbiology

PROTAC targeted protein degraders: the past is prologue

Miklos Bekes et al.

Summary: Targeted protein degradation (TPD) is a new therapeutic modality that can tackle disease-causing proteins which are difficult to target with conventional small molecules. PROTAC molecules, utilizing the ubiquitin-proteasome system to degrade target proteins, has achieved clinical proof-of-concept and attracted significant industry activity. Future directions include identifying target classes suitable for TPD, expanding the use of ubiquitin ligases for precision medicine, and extending the modality beyond oncology.

NATURE REVIEWS DRUG DISCOVERY (2022)

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Article Pharmacology & Pharmacy

Preclinical pharmacokinetics and metabolism of MAK683, a clinical stage selective oral embryonic ectoderm development (EED) inhibitor for cancer treatment

Ji Yue (Jeff) Zhang et al.

Summary: MAK683 is a potent and orally bioavailable EED inhibitor for potential treatment in oncology. It shows complex metabolic pathways both in vitro and in vivo, with the primary pathways involving hydroxylation and oxidative reactions in the liver. These pathways are observed in human and other animal species.

XENOBIOTICA (2022)

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Article Oncology

EP300 Selectively Controls the Enhancer Landscape of MYCN-Amplified Neuroblastoma

Adam D. Durbin et al.

Summary: Gene expression is regulated by histone modifications, and EP300 plays a significant role in high-risk neuroblastoma. The compound JQAD1, which targets EP300, effectively induces cell apoptosis in neuroblastoma cells with limited toxicity to normal cells.

CANCER DISCOVERY (2022)

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Review Chemistry, Medicinal

Targeting epigenetic modulators using PROTAC degraders: Current status and future perspective

Thomas Webb et al.

Summary: Epigenetic modulators play a crucial role in gene expression and their dysregulation is associated with disease pathogenesis. Small molecule inhibitors targeting epigenetic proteins have limitations, but protein degraders can better exploit target druggability.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2022)

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Article Oncology

A proteolysis-targeting chimera molecule selectively degrades ENL and inhibits malignant gene expression and tumor growth

Xin Li et al.

Summary: This study designed and synthesized compounds that can degrade ENL, a protein involved in MLL1-rearranged leukemia and other cancers. Compound 1 efficiently degraded ENL, suppressed malignant gene signatures, selectively inhibited cell proliferation of leukemia and cancer cells, and induced cell differentiation and apoptosis. It also showed significant antitumor activity in a mouse model of MLL1-rearranged leukemia and could degrade mutant ENL in Wilms tumor.

JOURNAL OF HEMATOLOGY & ONCOLOGY (2022)

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Article Cell Biology

EZH2 noncanonically binds cMyc and p300 through a cryptic transactivation domain to mediate gene activation and promote oncogenesis

Jun Wang et al.

Summary: The study reveals the noncanonical oncogenic roles of EZH2 in acute leukaemia, demonstrating its additional functions in binding cMyc and activating gene expression. To target the multifaceted tumorigenic functions of EZH2, the researchers developed a degrader, MS177, which effectively depletes both canonical and noncanonical complexes of EZH2 and shows a faster and more potent effect in suppressing cancer growth.

NATURE CELL BIOLOGY (2022)

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Article Biochemistry & Molecular Biology

Discovery of a dual WDR5 and Ikaros PROTAC degrader as an anti-cancer therapeutic

Dongxu Li et al.

Summary: A new proteolysis targeting chimera (PROTAC) named MS40 has been developed to selectively degrade WDR5 and Ikaros, showing promising anti-cancer effects in MLL-rearranged leukemias.

ONCOGENE (2022)

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Article Chemistry, Multidisciplinary

Radiotherapy-Triggered Proteolysis Targeting Chimera Prodrug Activation in Tumors

Chunrong Yang et al.

Summary: Proteolysis targeting chimera (PROTAC) is an emerging protein degradation strategy that shows great potential in targeting difficult-to-drug proteins. This study introduces a radiotherapy-triggered PROTAC prodrug (RT-PROTAC) activation strategy for precise and spatiotemporal control of protein degradation through X-ray radiation. The activated RT-PROTAC effectively degrades target proteins and exhibits synergistic anticancer activity with radiotherapy. This research provides an alternative approach for controlling protein degradation in vivo, offering a potential solution to minimize the systemic toxicity of PROTACs.

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2022)

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Article Chemistry, Multidisciplinary

Bridged Proteolysis Targeting Chimera (PROTAC) Enables Degradation of Undruggable Targets

Yan Xiong et al.

Summary: Proteolysis Targeting Chimeras (PROTACs) are effective for degrading disease-causing proteins. A novel approach called bridged PROTAC has been developed to target undruggable proteins by bringing the protein complex close to an E3 ubiquitin ligase using a small molecule binder of the target protein's binding partner. This approach has led to the discovery of MS28, the first-in-class degrader of cyclin D1, and it shows superior degradation efficiency and proliferation inhibition compared to CDK4/6 inhibitors and degraders. The bridged PROTAC strategy could serve as a generalizable platform for targeting undruggable proteins.

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2022)

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Article Chemistry, Medicinal

Discovery of precision targeting EZH2 degraders for triple-negative breast cancer

Cheng Wang et al.

Summary: EZH2 is often overexpressed in TNBC and other tumors, affecting tumor development and prognosis. The designed PROTACs molecule U3i precision targets EZH2 and shows good inhibitory effects on TNBC cells, inducing apoptosis without causing much damage to normal cells. U3i is a potential anticancer molecule for TNBC treatment.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2022)

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Article Multidisciplinary Sciences

Selective PROTAC-mediated degradation of SMARCA2 is efficacious in SMARCA4 mutant cancers

Jennifer Cantley et al.

Summary: This study reports the discovery of a potent and selective SMARCA2 proteolysis-targeting chimera molecule (PROTAC), A947. The authors demonstrate that selective SMARCA2 degradation can be achieved in the absence of selective SMARCA2/4 PROTAC binding, resulting in potent in vitro growth inhibition and in vivo efficacy in SMARCA4 mutant models. The study highlights a potential new therapeutic opportunity for patients with SMARCA4 mutations.

NATURE COMMUNICATIONS (2022)

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Article Chemistry, Medicinal

Discovery of a First-in-Class Degrader for Nuclear Receptor Binding SET Domain Protein 2 (NSD2) and Ikaros/Aiolos Published as part of the Journal of Medicinal Chemistry special issue Epigenetics 2022.

Fanye Meng et al.

Summary: In this study, a first-in-class NSD2 proteolysis targeting chimera (PROTAC) degrader was discovered, which effectively degraded NSD2 and CRBN. This compound was more effective in suppressing cancer cell growth compared to existing inhibitors and showed bioavailability in mice.

JOURNAL OF MEDICINAL CHEMISTRY (2022)

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Review Biochemistry & Molecular Biology

A comprehensive review of BET-targeting PROTACs for cancer therapy

Xiao-Li Zhou et al.

Summary: Targeted protein degradation using proteolysis-targeting chimeras (PROTACs) is an effective strategy for drug discovery, especially in cancer therapy. BET proteins, as therapeutic targets in cancer treatment, have been extensively studied and there have been recent advances in BET-targeting PROTACs.

BIOORGANIC & MEDICINAL CHEMISTRY (2022)

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Article Chemistry, Medicinal

Discovery of a potent and selective proteolysis targeting chimera (PROTAC) degrader of NSD3 histone methyltransferase

Yaoliang Sun et al.

Summary: This study reports the discovery of small-molecule NSD3 degraders based on the PROTAC strategy and demonstrates that inducing NSD3 degradation is a more effective approach than blocking the NSD3-PWWP domain in inhibiting NSD3 function, providing a potential therapeutic approach for lung cancer.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2022)

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Article Multidisciplinary Sciences

A selective and orally bioavailable VHL-recruiting PROTAC achieves SMARCA2 degradation in vivo

Christiane Kofink et al.

Summary: Targeted protein degradation using bifunctional molecules provides a new therapeutic option for undruggable targets. In this study, the authors developed orally bioavailable VHL-recruiting degraders that selectively degrade SMARCA2, demonstrating the feasibility of broadening the E3 ligase and physicochemical space for achieving oral efficacy with bifunctional molecules.

NATURE COMMUNICATIONS (2022)

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Article Computer Science, Artificial Intelligence

Accelerated rational PROTAC design via deep learning and molecular simulations

Shuangjia Zheng et al.

Summary: Proteolysis-targeting chimeras (PROTACs) are effective tools for degrading disease-related proteins, but their design and optimization is challenging. This study proposes a novel approach using deep learning and molecular simulations to accelerate rational PROTAC design, leading to the discovery of a novel BRD4-degrading PROTAC.

NATURE MACHINE INTELLIGENCE (2022)

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Article Chemistry, Medicinal

Targeting Triple-Negative Breast Cancer by a Novel Proteolysis Targeting Chimera Degrader of Enhancer of Zeste Homolog 2

Brandon Dale et al.

Summary: EZH2 overexpression is associated with poor prognosis in TNBC. A novel EZH2 PROTAC degrader, MS8815, has been discovered and shown to effectively suppress the growth of TNBC cells.

ACS PHARMACOLOGY & TRANSLATIONAL SCIENCE (2022)

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Review Chemistry, Multidisciplinary

Degrader-antibody conjugates

Peter S. Dragovich

Summary: This review provides a current summary of degrader-antibody conjugates (DACs), comparing them with traditional cytotoxic antibody-drug conjugates (ADCs) and highlighting different strategies and challenges associated with DAC generation. The examples demonstrate that biologically-active DACs can be successfully prepared using a variety of PROTAC payloads.

CHEMICAL SOCIETY REVIEWS (2022)

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Article Biochemistry & Molecular Biology

A NSD3-targeted PROTAC suppresses NSD3 and cMyc oncogenic nodes in cancer cells

Chenxi Xu et al.

Summary: This study reports a proteolysis targeting chimera (PROTAC) that specifically targets Nuclear receptor binding SET domain protein 3 (NSD3) and its associated cMyc node in tumor cells. The PROTAC effectively suppressed the growth of NSD3-dependent hematological cancer cells and resulted in similar gene expression changes as the knockout of NSD3 by CRISPR-Cas9.

CELL CHEMICAL BIOLOGY (2022)

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Article Multidisciplinary Sciences

Targeting SWI/SNF ATPases in enhancer-addicted prostate cancer

Lanbo Xiao et al.

Summary: The SWI/SNF complex plays a crucial role in chromatin remodeling and is altered in over 20% of cancers. A newly developed proteolysis-targeting chimera (PROTAC) named AU-15330 can degrade the SWI/SNF ATPase subunits, SMARCA2 and SMARCA4, leading to inhibition of tumor growth in prostate cancer cells that are sensitive to this degradation. Impeding SWI/SNF-mediated enhancer accessibility could be a promising therapeutic approach for enhancer-addicted cancers.

NATURE (2022)

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Article Oncology

BRD9 Is a Critical Regulator of Androgen Receptor Signaling and Prostate Cancer Progression

Aktan Alpsoy et al.

Summary: The SWI/SNF chromatin-remodeling complexes, particularly the GBAF subcomplex, play a critical role in prostate cancer by interacting with AR and CTCF, modulating AR-dependent gene expression, and exhibiting overlapping genome localization and transcriptional targets with BET proteins. Targeting the BRD9 subunit of GBAF complex may provide a promising alternative for treating AR-positive prostate cancers, including those resistant to androgen deprivation therapies, by coordinating SWI/SNF-BET cooperation.

CANCER RESEARCH (2021)

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Article Biochemistry & Molecular Biology

Structure-guided discovery of novel potent and efficacious proteolysis targeting chimera (PROTAC) degrader of BRD4

Wang Xiang et al.

Summary: BRD4 protein is a potential target in cancer treatment, with several related drugs in clinical studies. Research shows that BRD4 degraders can overcome resistance to BRD4 inhibitors, but most degraders have poor solubility and bioavailability.

BIOORGANIC CHEMISTRY (2021)

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Article Chemistry, Medicinal

Development of photocontrolled BRD4 PROTACs for tongue squamous cell carcinoma (TSCC)

Zhenzhen Li et al.

Summary: The catalytic properties of small-molecule proteolysis targeting chimeras (PROTACs) may lead to uncontrolled degradation. The main disadvantages of PROTACs are non-cancer specificity and relatively high toxicity, which limit their clinical application. Photocontrolled PROTACs (photoPROTACs) can be triggered by ultraviolet A (UVA) or visible light to induce the degradation of the target protein. A study successfully designed photoPROTACs to degrade bromodomain-containing protein 4 (BRD4) using 365 nm light, with compound N2 proving effective in inducing BRD4 degradation and inhibiting tumor growth in a zebrafish xenograft model of skin cancer tongue squamous cell carcinoma (TSCC) in a photocontrol manner.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2021)

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Article Cell Biology

Functional Genomics Identify Distinct and Overlapping Genes Mediating Resistance to Different Classes of Heterobifunctional Degraders of Oncoproteins

Ryosuke Shirasaki et al.

Summary: The resistance mechanisms to degraders targeting different oncoproteins are mainly due to prevention, rather than adaptation, of the breakdown of target oncoproteins, which is possibly caused by the loss of function of the cognate E3 ligase or its interactors/regulators.

CELL REPORTS (2021)

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Article Biochemistry & Molecular Biology

Trivalent PROTACs enhance protein degradation via combined avidity and cooperativity

Satomi Imaide et al.

Summary: Tri-valent PROTACs with increased binding valency enhance protein degradation efficacy and anti-cancer activity, forming highly stable ternary complexes with positive cooperativity. SIM1 engages with both BET bromodomains with high avidity and forms a productive 1:1:1 complex with VHL, demonstrating prolonged residence time and improved functional outcomes.

NATURE CHEMICAL BIOLOGY (2021)

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Article Chemistry, Medicinal

Design and Synthesis of EZH2-Based PROTACs to Degrade the PRC2 Complex for Targeting the Noncatalytic Activity of EZH2

Zhihao Liu et al.

Summary: This study presents a novel strategy for treating cancer by targeting proteasomal degradation to block the oncogenic activity of EZH2, offering a new approach compared to current EZH2 inhibitors.

JOURNAL OF MEDICINAL CHEMISTRY (2021)

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Article Multidisciplinary Sciences

Elevated NSD3 histone methylation activity drives squamous cell lung cancer

Gang Yuan et al.

Summary: Amplification of the chromosomal region 8p11-12 is common in lung squamous cell carcinoma (LUSC) and the NSD3 gene in this region is identified as a key regulator of LUSC tumorigenesis. NSD3 depletion attenuates tumor growth and enhances survival in LUSC, suggesting its potential as a therapeutic target. Additionally, NSD3-dependent LUSC xenografts are sensitive to bromodomain inhibition, indicating a vulnerability of LUSC to this treatment.

NATURE (2021)

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Article Cell Biology

A selective WDR5 degrader inhibits acute myeloid leukemia in patient-derived mouse models

Xufen Yu et al.

Summary: This study proposes pharmacological degradation of WDR5 as a promising therapeutic strategy for treating WDR5-dependent tumors and presents two high-resolution crystal structures of WDR5-degrader-E3 ligase ternary complexes. The designed WDR5 degrader, MS67, potently and selectively depleted WDR5, demonstrating higher efficacy than WDR5 PPI inhibitors in suppressing transcription of WDR5-regulated genes and inhibiting cancer cell proliferation. These findings suggest structure-based design can effectively identify highly active degraders for potential treatment of WDR5-dependent cancers.

SCIENCE TRANSLATIONAL MEDICINE (2021)

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Review Oncology

Achieving clinical success with BET inhibitors as anti-cancer agents

Tatiana Shorstova et al.

Summary: Transcriptional upregulation of oncogenes drives tumor progression, and targeting BET proteins with inhibitors has shown promise in suppressing oncogenic networks in tumors. Understanding the biology of BET proteins, designing better BET inhibitors, and incorporating BET inhibitors into combination therapies can enhance their efficacy in clinical settings.

BRITISH JOURNAL OF CANCER (2021)

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Article Chemistry, Medicinal

Design, Synthesis, and Evaluation of WD-Repeat-Containing Protein 5 (WDR5) Degraders

Anja Doelle et al.

Summary: H3K4 methylation is a hallmark of actively transcribed genes, with WDR5 associated with noncoding RNAs and MYC. WDR5 has been identified as a potential drug target, and the design of WDR5 degraders and the nature of the linker play a key role in degradation efficacy.

JOURNAL OF MEDICINAL CHEMISTRY (2021)

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Article Chemistry, Multidisciplinary

Cancer Selective Target Degradation by Folate-Caged PROTACs

Jing Liu et al.

Summary: PROTACs are emerging as a promising therapeutic modality for degrading intracellular protein targets, but potential toxicity in normal cells limits their applications. By conjugating a folate group to a ligand of the VHL E3 ubiquitin ligase, a cancer cell selective delivery strategy for PROTACs was developed to achieve targeted degradation of proteins of interest in cancer cells. Folate-PROTACs provide a platform for selective degradation of proteins of interest in cancer cells.

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2021)

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Article Biochemistry & Molecular Biology

Targeting non-canonical activation of GLI1 by the SOX2-BRD4 transcriptional complex improves the efficacy of HEDGEHOG pathway inhibition in melanoma

Silvia Pietrobono et al.

Summary: The study identified a novel mechanism involving the SOX2-BRD4 transcriptional complex driving the expression of GLI1, an effector in the HH/GLI pathway, independently of SMO activation. Combining a SMO inhibitor with a BRD4 degrader showed synergistic anti-proliferative effects in melanoma cells, providing a new potential treatment strategy for melanomas with an active SOX2-BRD4-GLI1 axis.

ONCOGENE (2021)

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Article Chemistry, Multidisciplinary

Chemical Inhibition of ENL/AF9 YEATS Domains in Acute Leukemia

Leopold Garnar-Wortzel et al.

Summary: The inhibition of the YEATS domain is an effective approach to disrupt the pathogenic function of ENL in acute leukemia, providing the first thoroughly characterized chemical probe for the ENL YEATS domain.

ACS CENTRAL SCIENCE (2021)

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Article Chemistry, Multidisciplinary

Aptamer-PROTAC Conjugates (APCs) for Tumor-Specific Targeting in Breast Cancer

Shipeng He et al.

Summary: The aptamer-PROTAC conjugation strategy shows potential in improving the tumor-specific targeting ability and in vivo antitumor potency of conventional PROTACs, paving the way for the design of tumor-specific targeting PROTACs.

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2021)

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Article Chemistry, Medicinal

Design, Synthesis, and Evaluation of VHL-Based EZH2 Degraders to Enhance Therapeutic Activity against Lymphoma

Yalin Tu et al.

Summary: In this study, PROTAC-based EZH2 degraders were developed to target whole EZH2 in lymphoma, showing better therapeutic activity compared to traditional EZH2 inhibitors, especially in DLBCL. This research demonstrates the potential of EZH2 degraders as a promising anticancer strategy for treating lymphoma.

JOURNAL OF MEDICINAL CHEMISTRY (2021)

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Article Chemistry, Multidisciplinary

Harnessing the E3 Ligase KEAP1 for Targeted Protein Degradation

Jieli Wei et al.

Summary: PROTACs are a promising new therapeutic modality that utilize a limited number of E3 ligases for selective protein degradation. This study demonstrates that the KEAP1 E3 ligase can be utilized to generate highly selective PROTACs, expanding the toolbox for targeted protein degradation.

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2021)

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Article Biochemistry & Molecular Biology

Small-molecule inhibitors targeting Polycomb repressive complex 1 RING domain

Shirish Shukla et al.

Summary: Novel compounds targeting PRC1 have been developed to modulate its activity and induce differentiation in leukemia cells.

NATURE CHEMICAL BIOLOGY (2021)

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Article Biochemistry & Molecular Biology

Chemo-proteomics exploration of HDAC degradability by small molecule degraders

Yuan Xiong et al.

Summary: The study synthesized a pan-HDAC degrader library for exploring acute degradation of chromatin-modifying enzymes, identifying leads for targeting HDACs 1-8 and 10. Cell line-driven target specificity and collateral loss of HDAC-containing repressive complexes were discovered upon HDAC degradation, potentially offering a new mechanism for controlling chromatin structure.

CELL CHEMICAL BIOLOGY (2021)

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Review Oncology

Advancing targeted protein degradation for cancer therapy

Brandon Dale et al.

Summary: The development of small-molecule degraders such as proteolysis-targeting chimeras (PROTACs) has enabled the targeting of previously considered undruggable oncoproteins. This review discusses recent advances in the field, with a focus on opportunities and challenges for future development.

NATURE REVIEWS CANCER (2021)

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Article Biochemistry & Molecular Biology

Targeted degradation of the enhancer lysine acetyltransferases CBP and p300

Raghu Vannam et al.

Summary: The study presents a chemical degrader of p300/CBP, dCBP-1, designed by leveraging structures of ligand-bound p300/CBP through in silico modeling of ternary complex formation. It is exceptionally potent at killing multiple myeloma cells and can abolish the enhancer driving oncogene expression. This efficient degrader provides a useful tool for dissecting the mechanism by which these factors coordinate enhancer activity in normal and diseased cells, alongside domain inhibitors.

CELL CHEMICAL BIOLOGY (2021)

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Article Biochemistry & Molecular Biology

Chemoproteomics-enabled discovery of covalent RNF114-based degraders that mimic natural product function

Mai Luo et al.

Summary: This study found that the natural product nimbolide can be used as a recruiter of the E3 ubiquitin ligase RNF114 for targeted protein degradation, which is important in modern drug discovery. Through activity-based protein profiling-enabled ligand screening, fully synthetic molecules mimicking nimbolide were discovered, showing potential for degrading therapeutic targets.

CELL CHEMICAL BIOLOGY (2021)

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Article Biochemical Research Methods

E3 Ligase Ligands for PROTACs: How They Were Found and How to Discover New Ones

Tasuku Ishida et al.

Summary: PROTACs, or bifunctional degrader molecules, are a novel approach for understanding and treating human diseases by targeting specific proteins for degradation. Advances in nonpeptidic small-molecule E3 ligase ligands, such as VHL and CRBN, have revolutionized the field and led to the development of drug-like PROTACs with powerful degradation capabilities. Ongoing research aims to expand the chemical diversity of PROTACs and explore new approaches for targeted protein degradation.

SLAS DISCOVERY (2021)

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Article Chemistry, Multidisciplinary

Optical Control of Small Molecule-Induced Protein Degradation

Yuta Naro et al.

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2020)

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Article Biochemistry & Molecular Biology

Discovery of a first-in-class EZH2 selective degrader

Anqi Ma et al.

NATURE CHEMICAL BIOLOGY (2020)

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Article Multidisciplinary Sciences

Light-induced control of protein destruction by opto-PROTAC

Jing Liu et al.

SCIENCE ADVANCES (2020)

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Article Multidisciplinary Sciences

PHOTACs enable optical control of protein degradation

Martin Reynders et al.

SCIENCE ADVANCES (2020)

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Review Oncology

The role ofSIRT2in cancer: A novel therapeutic target

Guangyuan Chen et al.

INTERNATIONAL JOURNAL OF CANCER (2020)

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Article Chemistry, Medicinal

Development of Selective Histone Deacetylase 6 (HDAC6) Degraders Recruiting Von Hippel-Lindau (VHL) E3 Ubiquitin Ligase

Ka Yang et al.

ACS MEDICINAL CHEMISTRY LETTERS (2020)

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Review Biochemistry & Molecular Biology

Proteolysis targeting chimeras (PROTACs) for epigenetics research

Anja Vogelmann et al.

CURRENT OPINION IN CHEMICAL BIOLOGY (2020)

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Review Oncology

EZH2: a novel target for cancer treatment

Ran Duan et al.

JOURNAL OF HEMATOLOGY & ONCOLOGY (2020)

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Article Chemistry, Medicinal

Discovery of First-in-Class Protein Arginine Methyltransferase 5 (PRMT5) Degraders

Yudao Shen et al.

JOURNAL OF MEDICINAL CHEMISTRY (2020)

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Article Chemistry, Medicinal

Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight

Terence C. S. Ho et al.

JOURNAL OF MEDICINAL CHEMISTRY (2020)

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Article Multidisciplinary Sciences

Bardoxolone conjugation enables targeted protein degradation of BRD4

Bingqi Tong et al.

SCIENTIFIC REPORTS (2020)

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Review Cell Biology

Recent Update of HDAC Inhibitors in Lymphoma

I-Chung Chen et al.

FRONTIERS IN CELL AND DEVELOPMENTAL BIOLOGY (2020)

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Article Biochemistry & Molecular Biology

EED-Targeted PROTACs Degrade EED, EZH2, and SUZ12 in the PRC2 Complex

Jessie Hao-Ru Hsu et al.

CELL CHEMICAL BIOLOGY (2020)

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Article Biochemistry & Molecular Biology

Degradation of Polycomb Repressive Complex 2 with an EED-Targeted Bivalent Chemical Degrader

Frances Potjewyd et al.

CELL CHEMICAL BIOLOGY (2020)

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Article Chemistry, Multidisciplinary

Discovery of histone deacetylase 3 (HDAC3)-specific PROTACs

Yufeng Xiao et al.

CHEMICAL COMMUNICATIONS (2020)

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Letter Biochemistry & Molecular Biology

In vivo target protein degradation induced by PROTACs based on E3 ligase DCAF15

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Different Degradation Mechanisms of Inhibitor of Apoptosis Proteins (IAPs) by the Specific and Nongenetic IAP-Dependent Protein Eraser (SNIPER)

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Acquired Resistance to BET-PROTACs (Proteolysis-Targeting Chimeras) Caused by Genomic Alterations in Core Components of E3 Ligase Complexes

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MOLECULAR CANCER THERAPEUTICS (2019)

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BRD9 binds cell type-specific chromatin regions regulating leukemic cell survival via STAT5 inhibition

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CELL DEATH & DISEASE (2019)

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NATURE COMMUNICATIONS (2019)

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Review Biochemistry & Molecular Biology

Targeted protein degradation: elements of PROTAC design

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CURRENT OPINION IN CHEMICAL BIOLOGY (2019)

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Development of Multifunctional Histone Deacetylase 6 Degraders with Potent Antimyeloma Activity

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Harnessing the anti-cancer natural product nimbolide for targeted protein degradation

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BAF complex vulnerabilities in cancer demonstrated via structure-based PROTAC design

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Electrophilic PROTACs that degrade nuclear proteins by engaging DCAF16

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Reversible Spatiotemporal Control of Induced Protein Degradation by Bistable PhotoPROTACs

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Light-Induced Protein Degradation with Photocaged PROTACs

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MDM2-Recruiting PROTAC Offers Superior, Synergistic Antiproliferative Activity via Simultaneous Degradation of BRD4 and Stabilization of p53

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Iterative Design and Optimization of Initially Inactive Proteolysis Targeting Chimeras (PROTACs) Identify VZ185 as a Potent, Fast, and Selective von Hippel-Lindau (VHL) Based Dual Degrader Probe of BRD9 and BRD7

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Letter Cell Biology

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Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds

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Chemically Induced Degradation of Sirtuin 2 (Sirt2) by a Proteolysis Targeting Chimera (PROTAC) Based on Sirtuin Rearranging Ligands (SirReals)

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Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression

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Translation Termination Factor GSPT1 Is a Phenotypically Relevant Off-Target of Heterobifunctional Phthalimide Degraders

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Discovery of QCA570 as an Exceptionally Potent and Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of the Bromodomain and Extra-Terminal (BET) Proteins Capable of Inducing Complete and Durable Tumor Regression

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Plasticity in binding confers selectivity in ligand-induced protein degradation

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Functional TRIM24 degrader via conjugation of ineffectual bromodomain and VHL ligands

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Discovery of Spiro Oxazolidinediones as Selective, Orally Bioavailable Inhibitors of p300/CBP Histone Acetyltransferases

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Structure-guided development of YEATS domain inhibitors by targeting pi-pi-pi stacking

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Targeted degradation of BRD9 reverses oncogenic gene expression in synovial sarcoma

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A Chemoproteomic Approach to Query the Degradable Kinome Using a Multi-kinase Degrader

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Lessons in PROTAC Design from Selective Degradation with a Promiscuous Warhead

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The Advantages of Targeted Protein Degradation Over Inhibition: An RTK Case Study

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Induced protein degradation: an emerging drug discovery paradigm

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BET Bromodomain Proteins Function as Master Transcription Elongation Factors Independent of CDK9 Recruitment

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Structural basis of PROTAC cooperative recognition for selective protein degradation

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Review Cell Biology

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The Role of Nuclear Receptor-Binding SET Domain Family Histone Lysine Methyltransferases in Cancer

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COLD SPRING HARBOR PERSPECTIVES IN MEDICINE (2017)

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Targeted Degradation of BET Proteins in Triple-Negative Breast Cancer

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Degradation of the BAF Complex Factor BRD9 by Heterobifunctional Ligands

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Article Chemistry, Medicinal

Discovery of a Chemical Tool Inhibitor Targeting the Bromodomains of TRIM24 and BRPF

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Article Chemistry, Medicinal

Structure-Guided Design of IACS-9571, a Selective High-Affinity Dual TRIM24-BRPF1 Bromodomain Inhibitor

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Review Biochemistry & Molecular Biology

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Identification and Development of 2,3-Dihydropyrrolo[1,2-a]quinazolin-5(1H)-one Inhibitors Targeting Bromodomains within the Switch/Sucrose Nonfermenting Complex

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Article Chemistry, Medicinal

Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor

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Amplification of WHSC1L1 regulates expression and estrogen-independent activation of ERα in SUM-44 breast cancer cells and is associated with ERα over-expression in breast cancer

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The Taf14 YEATS domain is a reader of histone crotonylation

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PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer

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PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2016)

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Clinical Response of Carcinomas Harboring the BRD4-NUT Oncoprotein to the Targeted Bromodomain Inhibitor OTX015/MK-8628

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In Vivo Functional Platform Targeting Patient-Derived Xenografts Identifies WDR5-Myc Association as a Critical Determinant of Pancreatic Cancer

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Article Cell Biology

Non-canonical PRC1.1 Targets Active Genes Independent of H3K27me3 and Is Essential for Leukemogenesis

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HDACs and HDAC Inhibitors in Cancer Development and Therapy

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COLD SPRING HARBOR PERSPECTIVES IN MEDICINE (2016)

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Article Biochemistry & Molecular Biology

Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4

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ACS CHEMICAL BIOLOGY (2015)

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Review Biochemistry & Molecular Biology

The PRMT5 arginine methyltransferase: many roles in development, cancer and beyond

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Protein Lysine Acetylation by p300/CBP

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CHEMICAL REVIEWS (2015)

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Identification of Histone Deacetylase Inhibitors with Benzoylhydrazide Scaffold that Selectively Inhibit Class I Histone Deacetylases

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Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4

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Article Chemistry, Medicinal

Structure-Based Design of γ-Carboline Analogues as Potent and Specific BET Bromodomain Inhibitors

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Transcriptional plasticity promotes primary and acquired resistance to BET inhibition

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Pharmacological targeting of the Wdr5-MLL interaction in C/EBP alpha N-terminal leukemia

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A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models

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Phthalimide conjugation as a strategy for in vivo target protein degradation

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Expression and clinicopathological significance of EED, SUZ12 and EZH2 mRNA in colorectal cancer

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TRIM24 promotes glioma progression and enhances chemoresistance through activation of the PI3K/Akt signaling pathway

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Residual Complexes Containing SMARCA2 (BRM) Underlie the Oncogenic Drive of SMARCA4 (BRG1) Mutation

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Structure of the DDBI-CRBN E3 ubiquitin ligase in complex with thalidomide

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Review Biotechnology & Applied Microbiology

Histone deacetylases and their inhibitors in cancer, neurological diseases and immune disorders

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NATURE REVIEWS DRUG DISCOVERY (2014)

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Functional epigenetics approach identifies BRM/SMARCA2 as a critical synthetic lethal target in BRG1-deficient cancers

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PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2014)

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Erasers of Histone Acetylation: The Histone Deacetylase Enzymes

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COLD SPRING HARBOR PERSPECTIVES IN BIOLOGY (2014)

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The central role of EED in the orchestration of polycomb group complexes

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Somatic mutations of amino acid metabolism-related genes in gastric and colorectal cancers and their regional heterogeneity - a short report

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Review Genetics & Heredity

Epigenetic modulation in the treatment of atherosclerotic disease

[Anonymous]

FRONTIERS IN GENETICS (2014)

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An Orally Bioavailable Chemical Probe of the Lysine Methyltransferases EZH2 and EZH1

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ACS CHEMICAL BIOLOGY (2013)

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Article Biochemistry & Molecular Biology

Small-molecule inhibition of MLL activity by disruption of its interaction with WDR5

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EZH2 overexpression in natural killer/T-cell lymphoma confers growth advantage independently of histone methyltransferase activity

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BLOOD (2013)

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Identification of Driver Genes in Hepatocellular Carcinoma by Exome Sequencing

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High-Affinity, Small-Molecule Peptidomimetic Inhibitors of MLL1/WDR5 Protein-Protein Interaction

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Proteomic and bioinformatic analysis of mammalian SWI/SNF complexes identifies extensive roles in human malignancy

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Article Multidisciplinary Sciences

Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2

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PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2013)

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Review Oncology

Protein arginine methyltransferases and cancer

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NATURE REVIEWS CANCER (2013)

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Histone Recognition and Large-Scale Structural Analysis of the Human Bromodomain Family

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CELL (2012)

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Structural Basis for WDR5 Interaction (Win) Motif Recognition in Human SET1 Family Histone Methyltransferases

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JOURNAL OF BIOLOGICAL CHEMISTRY (2012)

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Article Chemistry, Medicinal

Selective Histone Deacetylase 6 Inhibitors Bearing Substituted Urea Linkers Inhibit Melanoma Cell Growth

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JOURNAL OF MEDICINAL CHEMISTRY (2012)

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Article Biochemistry & Molecular Biology

The plasticity of WDR5 peptide-binding cleft enables the binding of the SET1 family of histone methyltransferases

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NUCLEIC ACIDS RESEARCH (2012)

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Article Multidisciplinary Sciences

Crystal structure of the human PRMT5:MEP50 complex

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PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2012)

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The Brd4 Extraterminal Domain Confers Transcription Activation Independent of pTEFb by Recruiting Multiple Proteins, Including NSD3

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MOLECULAR AND CELLULAR BIOLOGY (2011)

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NSD2 Links Dimethylation of Histone H3 at Lysine 36 to Oncogenic Programming

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MOLECULAR CELL (2011)

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Review Oncology

SWI/SNF nucleosome remodellers and cancer

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NATURE REVIEWS CANCER (2011)

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Oncogenesis by sequestration of CBP/p300 in transcriptionally inactive hyperacetylated chromatin domains

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EMBO JOURNAL (2010)

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Histone deacetylases 1 and 2 act in concert to promote the G1-to-S progression

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TRIM24 links a non-canonical histone signature to breast cancer

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