Related references
Note: Only part of the references are listed.Discovery of pan-IAP degraders via a CRBN recruiting mechanism
Seulki Park et al.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2023)
Design and characterization of a heterobifunctional degrader of KEAP1
Hao Chen et al.
REDOX BIOLOGY (2023)
PROTAC targeted protein degraders: the past is prologue
Miklos Bekes et al.
NATURE REVIEWS DRUG DISCOVERY (2022)
Targeted protein degradation and drug discovery
Mikihiko Naito
JOURNAL OF BIOCHEMISTRY (2022)
Homobivalent, Trivalent, and Covalent PROTACs: Emerging Strategies for Protein Degradation
Jianyu Yan et al.
JOURNAL OF MEDICINAL CHEMISTRY (2022)
Exploring the target scope of KEAP1 E3 ligase-based PROTACs
Guangyan Du et al.
CELL CHEMICAL BIOLOGY (2022)
PROTACs: past, present and future
Ke Li et al.
CHEMICAL SOCIETY REVIEWS (2022)
Homo-PROTAC mediated suicide of MDM2 to treat non-small cell lung cancer
Shipeng He et al.
ACTA PHARMACEUTICA SINICA B (2021)
Targeted protein degraders crowd into the clinic
Asher Mullard
NATURE REVIEWS DRUG DISCOVERY (2021)
From Conception to Development: Investigating PROTACs Features for Improved Cell Permeability and Successful Protein Degradation
Carlotta Cecchini et al.
FRONTIERS IN CHEMISTRY (2021)
Von Hippel-Lindau (VHL) small-molecule inhibitor binding increases stability and intracellular levels of VHL protein
Julianty Frost et al.
JOURNAL OF BIOLOGICAL CHEMISTRY (2021)
Unraveling the Role of Linker Design in Proteolysis Targeting Chimeras
Troy A. Bemis et al.
JOURNAL OF MEDICINAL CHEMISTRY (2021)
Selective degradation-inducing probes for studying cereblon (CRBN) biology
Chelsea E. Powell et al.
RSC MEDICINAL CHEMISTRY (2021)
DIA-NN: neural networks and interference correction enable deep proteome coverage in high throughput
Vadim Demichev et al.
NATURE METHODS (2020)
Proteolysis-Targeting Chimeras as Therapeutics and Tools for Biological Discovery
George M. Burslem et al.
CELL (2020)
Medicinal Chemistry of Inhibiting RING-Type E3 Ubiquitin Ligases
Nicole Blaquiere et al.
JOURNAL OF MEDICINAL CHEMISTRY (2020)
Future Therapeutic Directions for Smac-Mimetics
Emma Morrish et al.
CELLS (2020)
Prey for the Proteasome: Targeted Protein Degradation-A Medicinal Chemist's Perspective
Laura M. Luh et al.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2020)
diaPASEF: parallel accumulation-serial fragmentation combined with data-independent acquisition
Florian Meier et al.
NATURE METHODS (2020)
PROTACs: An Emerging Therapeutic Modality in Precision Medicine
Dhanusha A. Nalawansha et al.
CELL CHEMICAL BIOLOGY (2020)
Systematic exploration of different E3 ubiquitin ligases: an approach towards potent and selective CDK6 degraders
Christian Steinebach et al.
CHEMICAL SCIENCE (2020)
Cereblon versus VHL: Hijacking E3 ligases against each other using PROTACs
Miriam Girardini et al.
BIOORGANIC & MEDICINAL CHEMISTRY (2019)
Inhibitor of Apoptosis Protein (IAP) Antagonists in Anticancer Agent Discovery: Current Status and Perspectives
Hui Cong et al.
JOURNAL OF MEDICINAL CHEMISTRY (2019)
Rapid and Reversible Knockdown of Endogenously Tagged Endosomal Proteins via an Optimized HaloPROTAC Degrader
Hannah Tovell et al.
ACS CHEMICAL BIOLOGY (2019)
Development of selective small molecule MDM2 degraders based on nutlin
Bo Wang et al.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2019)
Development of targeted protein degradation therapeutics
Philip P. Chamberlain et al.
NATURE CHEMICAL BIOLOGY (2019)
Discovery of ERD-308 as a Highly Potent Proteolysis Targeting Chimera (PROTAC) Degrader of Estrogen Receptor (ER)
Jiantao Hu et al.
JOURNAL OF MEDICINAL CHEMISTRY (2019)
Discovery of MD-224 as a First-in-Class, Highly Potent, and Efficacious Proteolysis Targeting Chimera Murine Double Minute 2 Degrader Capable of Achieving Complete and Durable Tumor Regression
Yangbing Li et al.
JOURNAL OF MEDICINAL CHEMISTRY (2019)
Discovery of ARD-69 as a Highly Potent Proteolysis Targeting Chimera (PROTAC) Degrader of Androgen Receptor (AR) for the Treatment of Prostate Cancer
Xin Han et al.
JOURNAL OF MEDICINAL CHEMISTRY (2019)
Differential PROTAC substrate specificity dictated by orientation of recruited E3 ligase
Blake E. Smith et al.
NATURE COMMUNICATIONS (2019)
PROTAC-mediated crosstalk between E3 ligases
Christian Steinebach et al.
CHEMICAL COMMUNICATIONS (2019)
Derivatization of inhibitor of apoptosis protein (IAP) ligands yields improved inducers of estrogen receptor degradation
Nobumichi Ohoka et al.
JOURNAL OF BIOLOGICAL CHEMISTRY (2018)
Novel smac mimetic APG-1387 elicits ovarian cancer cell killing through TNF-alpha, Ripoptosome and autophagy mediated cell death pathway
Bao-Xia Li et al.
JOURNAL OF EXPERIMENTAL & CLINICAL CANCER RESEARCH (2018)
ASTX660, a Novel Non-peptidomimetic Antagonist of cIAP1/2 and XIAP, Potently Induces TNFα-Dependent Apoptosis in Cancer Cell Lines and Inhibits Tumor Growth
George A. Ward et al.
MOLECULAR CANCER THERAPEUTICS (2018)
Small Molecule Modulators of RING-Type E3 Ligases: MDM and Cullin Families as Targets
Emil Bulatov et al.
FRONTIERS IN PHARMACOLOGY (2018)
Homo-PROTACs for the Chemical Knockdown of Cereblon
Christian Steinebach et al.
ACS CHEMICAL BIOLOGY (2018)
Thalidomide promotes degradation of SALL4, a transcription factor implicated in Duane Radial Ray syndrome
Katherine A. Donovan et al.
ELIFE (2018)
Drugging the undruggabl: targeting challenging E3 ligases for personalized medicine
Carles Galdeano
FUTURE MEDICINAL CHEMISTRY (2017)
Homo-PROTACs: bivalent small-molecule dimerizers of the VHL E3 ubiquitin ligase to induce self-degradation
Chiara Maniaci et al.
NATURE COMMUNICATIONS (2017)
Small-Molecule Modulation of Protein Homeostasis
George M. Burslem et al.
CHEMICAL REVIEWS (2017)
A novel Smac mimetic APG-1387 demonstrates potent antitumor activity in nasopharyngeal carcinoma cells by inducing apoptosis
Ning Li et al.
CANCER LETTERS (2016)
PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer
Kanak Raina et al.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2016)
Activation of concurrent apoptosis and necroptosis by SMAC mimetics for the treatment of refractory and relapsed ALL
Scott McComb et al.
SCIENCE TRANSLATIONAL MEDICINE (2016)
Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4
Michael Zengerle et al.
ACS CHEMICAL BIOLOGY (2015)
Targeting Cullin-RING E3 ubiquitin ligases for drug discovery: structure, assembly and small-molecule modulation
Emil Bulatov et al.
BIOCHEMICAL JOURNAL (2015)
Promises and Challenges of Smac Mimetics as Cancer Therapeutics
Simone Fulda
CLINICAL CANCER RESEARCH (2015)
Structure-Guided Design and Optimization of Small Molecules Targeting the Protein Protein Interaction between the von Hippel- Lindau (VHL) E3 Ubiquitin Ligase and the Hypoxia Inducible Factor (HIF) Alpha Subunit with in Vitro Nanomolar Affinities
Carles Galdeano et al.
JOURNAL OF MEDICINAL CHEMISTRY (2014)
IAP proteins as targets for drug development in oncology
Laurence Dubrez et al.
ONCOTARGETS AND THERAPY (2013)
Targeting IAP proteins for therapeutic intervention in cancer
Simone Fulda et al.
NATURE REVIEWS DRUG DISCOVERY (2012)
Smac Mimetics Activate the E3 Ligase Activity of cIAP1 Protein by Promoting RING Domain Dimerization
Rebecca Feltham et al.
JOURNAL OF BIOLOGICAL CHEMISTRY (2011)
Antagonists Induce a Conformational Change in cIAP1 That Promotes Autoubiquitination
Erin C. Dueber et al.
SCIENCE (2011)
IAP antagonists induce autoubiquitination of c-IAPs, NF-κB activation, and TNFα-dependent apoptosis
Eugene Varfolomeev et al.
CELL (2007)
IAP antagonists target cIAP1 to induce TNFα- dependent apoptosis
James E. Vince et al.
CELL (2007)
Autocrine TNFα signaling renders human cancer cells susceptible to smac-mimetic-induced apoptosis
Sean L. Petersen et al.
CANCER CELL (2007)
Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer
TK Oost et al.
JOURNAL OF MEDICINAL CHEMISTRY (2004)
Pharmaceutical profiling method for lipophilicity and integrity using liquid chromatography-mass spectrometry
EH Kerns et al.
JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES (2003)
Fast gradient HPLC method to determine compounds binding to human serum albumin. Relationships with octanol/water and immobilized artificial membrane lipophilicity
K Valko et al.
JOURNAL OF PHARMACEUTICAL SCIENCES (2003)
IAP proteins: Blocking the road to death's door
GS Salvesen et al.
NATURE REVIEWS MOLECULAR CELL BIOLOGY (2002)
Structural basis for binding of Smac/DIABLO to the XIAP BIR3 domain
ZH Liu et al.
NATURE (2000)
Structural basis of IAP recognition by Smac/DIABLO
G Wu et al.
NATURE (2000)
Structural and biochemical basis of apoptotic activation by Smac/DIABLO
JJ Chai et al.
NATURE (2000)
Smac, a mitochondrial protein that promotes cytochrome c-dependent caspase activation by eliminating IAP inhibition
CY Du et al.
CELL (2000)
Identification of DIABLO, a mammalian protein that promotes apoptosis by binding to and antagonizing IAP proteins
AM Verhagen et al.
CELL (2000)