相关参考文献
注意：仅列出部分参考文献，下载原文获取全部文献信息。Chemoproteomic-Driven Discovery of Covalent PROTACs
Yiqing Zhou et al.
BIOCHEMISTRY (2020)
Design, Synthesis, and Biological Evaluation of MEK PROTACs
Stefan Vollmer et al.
JOURNAL OF MEDICINAL CHEMISTRY (2020)
Optical Control of Small Molecule-Induced Protein Degradation
Yuta Naro et al.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2020)
PHOTACs enable optical control of protein degradation
Martin Reynders et al.
SCIENCE ADVANCES (2020)
Antibody-PROTAC Conjugates Enable HER2-Dependent Targeted Protein Degradation of BRD4
Maria Maneiro et al.
ACS CHEMICAL BIOLOGY (2020)
Azo-PROTAC: Novel Light-Controlled Small-Molecule Tool for Protein Knockdown
Yu-Hui Jin et al.
JOURNAL OF MEDICINAL CHEMISTRY (2020)
Enhancing intracellular accumulation and target engagement of PROTACs with reversible covalent chemistry
Wen-Hao Guo et al.
NATURE COMMUNICATIONS (2020)
Potent and Selective Mitogen-Activated Protein Kinase Kinase 1/2 (MEK1/2) Heterobifunctional Small-molecule Degraders
Jianping Hu et al.
JOURNAL OF MEDICINAL CHEMISTRY (2020)
A caged E3 ligase ligand for PROTAC-mediated protein degradation with light
Cyrille S. Kounde et al.
CHEMICAL COMMUNICATIONS (2020)
Covalent Ligand Screening Uncovers a RNF4 E3 Ligase Recruiter for Targeted Protein Degradation Applications
Carl C. Ward et al.
ACS CHEMICAL BIOLOGY (2019)
Pomalidomide hybrids act as proteolysis targeting chimeras: Synthesis, anticancer activity and B-Raf degradation
Hong Chen et al.
BIOORGANIC CHEMISTRY (2019)
Design and Characterization of SGK3-PROTAC1, an Isoform Specific SGK3 Kinase PROTAC Degrader
Hannah Tovell et al.
ACS CHEMICAL BIOLOGY (2019)
Reversible Spatiotemporal Control of Induced Protein Degradation by Bistable PhotoPROTACs
Patrick Pfaff et al.
ACS CENTRAL SCIENCE (2019)
Triazol: a privileged scaffold for proteolysis targeting chimeras
Li-Wen Xia et al.
FUTURE MEDICINAL CHEMISTRY (2019)
Discovery of a First-in-Class Mitogen-Activated Protein Kinase Kinase 1/2 Degrader
Jieli Wei et al.
JOURNAL OF MEDICINAL CHEMISTRY (2019)
Light-Induced Protein Degradation with Photocaged PROTACs
Gang Xue et al.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2019)
Targeted protein degradation: expanding the toolbox
Matthieu Schapira et al.
NATURE REVIEWS DRUG DISCOVERY (2019)
The PROTAC technology in drug development
Yutian Zou et al.
CELL BIOCHEMISTRY AND FUNCTION (2019)
PROTAC-Mediated Degradation of Bruton's Tyrosine Kinase Is Inhibited by Covalent Binding
Christopher P. Tinworth et al.
ACS CHEMICAL BIOLOGY (2019)
MEK inhibitors under development for treatment of non-small-cell lung cancer
Chul Kim et al.
EXPERT OPINION ON INVESTIGATIONAL DRUGS (2018)
Identification and Characterization of Von Hippel-Lindau-Recruiting Proteolysis Targeting Chimeras (PROTACs) of TANK-Binding Kinase 1
Andrew P. Crew et al.
JOURNAL OF MEDICINAL CHEMISTRY (2018)
Targeting the C481S Ibrutinib-Resistance Mutation in Bruton's Tyrosine Kinase Using PROTAC-Mediated Degradation
Alexandru D. Buhimschi et al.
BIOCHEMISTRY (2018)
Proteolysis Targeting Chimeras (PROTACs) of Anaplastic Lymphoma Kinase (ALK)
Chengwei Zhang et al.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2018)
DNA-encoded chemical libraries - achievements and remaining challenges
Nicholas Favalli et al.
FEBS LETTERS (2018)
Molecular mechanisms of drug resistance in ovarian cancer
Leyla Norouzi-Barough et al.
JOURNAL OF CELLULAR PHYSIOLOGY (2018)
Plasticity in binding confers selectivity in ligand-induced protein degradation
Radoslaw P. Nowak et al.
NATURE CHEMICAL BIOLOGY (2018)
Encorafenib and Binimetinib: First Global Approvals
Matt Shirley
DRUGS (2018)
Overcoming Resistance to Targeted Anticancer Therapies through Small-Molecule-Mediated MEK Degradation
Jessie Peh et al.
CELL CHEMICAL BIOLOGY (2018)
Lessons in PROTAC Design from Selective Degradation with a Promiscuous Warhead
Daniel P. Bondeson et al.
CELL CHEMICAL BIOLOGY (2018)
Induced protein degradation: an emerging drug discovery paradigm
Ashton C. Lai et al.
NATURE REVIEWS DRUG DISCOVERY (2017)
Molecular recognition of ternary complexes: a new dimension in the structure-guided design of chemical degraders
Scott J. Hughes et al.
STRUCTURE-BASED DRUG DESIGN: INSIGHTS FROM ACADEMIA AND INDUSTRY (2017)
Focal necrotizing myopathy with 'dropped-head syndrome' induced by cobimetinib in metastatic melanoma
Marie-Lea Gauci et al.
MELANOMA RESEARCH (2017)
Structural basis of PROTAC cooperative recognition for selective protein degradation
Morgan S. Gadd et al.
NATURE CHEMICAL BIOLOGY (2017)
The Ubiquitin Code in the Ubiquitin-Proteasome System and Autophagy
Yong Tae Kwon et al.
TRENDS IN BIOCHEMICAL SCIENCES (2017)
Cardiovascular Effects of the MEK Inhibitor, Trametinib: A Case Report, Literature Review, and Consideration of Mechanism
Mary Banks et al.
CARDIOVASCULAR TOXICOLOGY (2017)
Targeted Protein Degradation: from Chemical Biology to Drug Discovery
Philipp M. Cromm et al.
CELL CHEMICAL BIOLOGY (2017)
Modular PROTAC Design for the Degradation of Oncogenic BCR-ABL
Ashton C. Lai et al.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2016)
Small-Molecule PROTACS: New Approaches to Protein Degradation
Momar Toure et al.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2016)
Chemical Space of DNA-Encoded Libraries
Raphael M. Franzini et al.
JOURNAL OF MEDICINAL CHEMISTRY (2016)
Discovery of Bifunctional Oncogenic Target Inhibitors against Allosteric Mitogen-Activated Protein Kinase (MEK1) and Phosphatidylinositol 3-Kinase (PI3K)
Martian E. Van Dort et al.
JOURNAL OF MEDICINAL CHEMISTRY (2016)
Cobimetinib combined with vemurafenib in advanced BRAFV600-mutant melanoma (coBRIM): updated efficacy results from a randomised, double-blind, phase 3 trial
Paolo A. Ascierto et al.
LANCET ONCOLOGY (2016)
The Combination of Vemurafenib and Procaspase-3 Activation Is Synergistic in Mutant BRAF Melanomas
Jessie Peh et al.
MOLECULAR CANCER THERAPEUTICS (2016)
Protein Degradation by In-Cell Self-Assembly of Proteolysis Targeting Chimeras
Honorine Lebraud et al.
ACS CENTRAL SCIENCE (2016)
Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4
Michael Zengerle et al.
ACS CHEMICAL BIOLOGY (2015)
Dual inhibition of allosteric mitogen-activated protein kinase (MEK) and phosphatidylinositol 3-kinase (PI3K) oncogenic targets with a bifunctional inhibitor
Marcian E. Van Dort et al.
BIOORGANIC & MEDICINAL CHEMISTRY (2015)
Tetrahydropyrrolo-diazepenones as inhibitors of ERK2 kinase
Jeffrey T. Bagdanoff et al.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2015)
Tunable-Combinatorial Mechanisms of Acquired Resistance Limit the Efficacy of BRAF/MEK Cotargeting but Result in Melanoma Drug Addiction
Gatien Moriceau et al.
CANCER CELL (2015)
Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4
Jing Lu et al.
CHEMISTRY & BIOLOGY (2015)
NSK-01105 inhibits proliferation and induces apoptosis of prostate cancer cells by blocking the Raf/MEK/ERK and PI3K/Akt/mTOR signal pathways
Pengfei Yu et al.
TUMOR BIOLOGY (2015)
MEK1 and MEK2 inhibitors and cancer therapy: the long and winding road
Christopher J. Caunt et al.
NATURE REVIEWS CANCER (2015)
Surface plasmon resonance spectroscopy for characterisation of membrane protein-ligand interactions and its potential for drug discovery
Simon G. Patching
BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES (2014)
Disruption of CRAF-mediated MEK activation is required for effective MEK inhibition in KRAS mutant tumors
Piro Lito et al.
CANCER RESEARCH (2014)
A randomised, double-blind, placebo-controlled trial of trametinib, an oral MEK inhibitor, in combination with gemcitabine for patients with untreated metastatic adenocarcinoma of the pancreas
Jeffrey R. Infante et al.
EUROPEAN JOURNAL OF CANCER (2014)
The clinical development of MEK inhibitors
Yujie Zhao et al.
NATURE REVIEWS CLINICAL ONCOLOGY (2014)
Combined BRAF and MEK Inhibition versus BRAF Inhibition Alone in Melanoma
G. V. Long et al.
NEW ENGLAND JOURNAL OF MEDICINE (2014)
Increased MAPK reactivation in early resistance to dabrafenib/trametinib combination therapy of BRAF-mutant metastatic melanoma
Georgina V. Long et al.
NATURE COMMUNICATIONS (2014)
Targeting RAF kinases for cancer therapy: BRAF-mutated melanoma and beyond
Matthew Holderfield et al.
NATURE REVIEWS CANCER (2014)
Rigosertib Blocks RAS Signaling By Acting As a Small Molecule RAS Mimetic That Binds to the RAS-Binding Domains of RAS Effector Proteins
E. Premkumar Reddy et al.
BLOOD (2014)
Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers
Georgia Hatzivassiliou et al.
NATURE (2013)
Mechanisms of acquired resistance to ERK1/2 pathway inhibitors
A. S. Little et al.
ONCOGENE (2013)
Posttranslational protein knockdown coupled to receptor tyrosine kinase activation with phosphoPROTACs
John Hines et al.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2013)
Discovery of a Novel ERK Inhibitor with Activity in Models of Acquired Resistance to BRAF and MEK Inhibitors
Erick J. Morris et al.
CANCER DISCOVERY (2013)
Concurrent MEK2 Mutation and BRAF Amplification Confer Resistance to BRAF and MEK Inhibitors in Melanoma
Jessie Villanueva et al.
CELL REPORTS (2013)
Discovery of MEK/PI3K dual inhibitor via structure-based virtual screening
Hwangseo Park et al.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2012)
Enhanced Apoptosis and Tumor Growth Suppression Elicited by Combination of MEK (Selumetinib) and mTOR Kinase Inhibitors (AZD8055)
Sarah V. Holt et al.
CANCER RESEARCH (2012)
First-in-Human, Phase I Dose-Escalation Study of the Safety, Pharmacokinetics, and Pharmacodynamics of RO5126766, a First-in-Class Dual MEK/RAF Inhibitor in Patients with Solid Tumors
Maria Martinez-Garcia et al.
CLINICAL CANCER RESEARCH (2012)
ERK Inhibition Overcomes Acquired Resistance to MEK Inhibitors
Georgia Hatzivassiliou et al.
MOLECULAR CANCER THERAPEUTICS (2012)
Activation and Function of the MAPKs and Their Substrates, the MAPK-Activated Protein Kinases (vol 75, pg 50, 2011)
Marie Cargnello et al.
MICROBIOLOGY AND MOLECULAR BIOLOGY REVIEWS (2012)
Combined BRAF and MEK Inhibition in Melanoma with BRAF V600 Mutations
Keith T. Flaherty et al.
NEW ENGLAND JOURNAL OF MEDICINE (2012)
Mechanisms of Resistance to RAF Inhibitors in Melanoma
Andrew E. Aplin et al.
JOURNAL OF INVESTIGATIVE DERMATOLOGY (2011)
Strong negative feedback from Erk to Raf confers robustness to MAPK signalling
Raphaela Fritsche-Guenther et al.
MOLECULAR SYSTEMS BIOLOGY (2011)
Activation and Function of the MAPKs and Their Substrates, the MAPK-Activated Protein Kinases
Marie Cargnello et al.
MICROBIOLOGY AND MOLECULAR BIOLOGY REVIEWS (2011)
Amplification of the Driving Oncogene, KRAS or BRAF, Underpins Acquired Resistance to MEK1/2 Inhibitors in Colorectal Cancer Cells
Annette S. Little et al.
SCIENCE SIGNALING (2011)
Discovery of 3-(2-aminoethyl)-5-(3-phenyl-propylidene)-thiazolidine-2,4-dione as a dual inhibitor of the Raf/MEK/ERK and the PI3K/Akt signaling pathways
Qianbin Li et al.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2010)
Transcriptional Pathway Signatures Predict MEK Addiction and Response to Selumetinib (AZD6244)
Jonathan R. Dry et al.
CANCER RESEARCH (2010)
Phase I Pharmacokinetic and Pharmacodynamic Study of the Oral MAPK/ERK Kinase Inhibitor PD-0325901 in Patients with Advanced Cancers
Patricia M. LoRusso et al.
CLINICAL CANCER RESEARCH (2010)
Impact of Feedback Phosphorylation and Raf Heterodimerization on Normal and Mutant B-Raf Signaling
Daniel A. Ritt et al.
MOLECULAR AND CELLULAR BIOLOGY (2010)
BRAF Gene Amplification Can Promote Acquired Resistance to MEK Inhibitors in Cancer Cells Harboring the BRAF V600E Mutation
Ryan B. Corcoran et al.
SCIENCE SIGNALING (2010)
RDEA119/BAY 869766: A Potent, Selective, Allosteric Inhibitor of MEK1/2 for the Treatment of Cancer
Cory Iverson et al.
CANCER RESEARCH (2009)
MEK1 mutations confer resistance to MEK and B-RAF inhibition
Caroline M. Emery et al.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2009)
Growth-Inhibitory and Antiangiogenic Activity of the MEK Inhibitor PD0325901 in Malignant Melanoma with or without BRAF Mutations
Ludovica Ciuffreda et al.
NEOPLASIA (2009)
BRAF V600E disrupts AZD6244-Induced abrogation of negative feedback pathways between extracellular signal-regulated kinase and Raf proteins
Bret B. Friday et al.
CANCER RESEARCH (2008)
Putative allosteric MEK1 and MEK2 inhibitors
Steve Price
EXPERT OPINION ON THERAPEUTIC PATENTS (2008)
Small-molecule activation of procaspase-3 to caspase-3 as a personalized anticancer strategy
Karson S. Putt et al.
NATURE CHEMICAL BIOLOGY (2006)
BRAF mutation predicts sensitivity to MEK inhibition
DB Solit et al.
NATURE (2006)
The effects of a novel MEK inhibitor PD184161 on MEK-ERK signaling and growth in human liver cancer
Patrick J. Klein et al.
NEOPLASIA (2006)
ON01910, a non-ATP-competitive small molecule inhibitor of Plk1, is a potent anticancer agent
K Gumireddy et al.
CANCER CELL (2005)
Regulation of raf-1 by direct feedback phosphorylation
MK Dougherty et al.
MOLECULAR CELL (2005)
Chemical genetic control of protein levels: Selective in vivo targeted degradation
JS Schneekloth et al.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2004)
Overexpression of caspase-3 in hepatocellular carcinomas
R Persad et al.
MODERN PATHOLOGY (2004)
The Raf/MEK inhibitor PD98059 enhances ERK1/2 phosphorylation mediated by peroxynitrite via enforced mitochondrial formation of reactive oxygen species
L Cerioni et al.
FEBS LETTERS (2003)
Development of protacs to target cancer-promoting proteins for ubiquitination and degradation
KM Sakamoto et al.
MOLECULAR & CELLULAR PROTEOMICS (2003)
Mutations of the BRAF gene in human cancer
H Davies et al.
NATURE (2002)
Elevated procaspase levels in human melanoma
D Fink et al.
MELANOMA RESEARCH (2001)
Immunohistochemical expression of caspase-3 as an adverse indicator of the clinical outcome in human breast cancer
L Nakopoulou et al.
PATHOBIOLOGY (2001)
分享论文
