Fragment Optimization of Reversible Binding to the Switch II Pocket on KRAS Leads to a Potent, In Vivo Active KRASG12C Inhibitor
Published 2022 View Full Article
- Home
- Publications
- Publication Search
- Publication Details
Title
Fragment Optimization of Reversible Binding to the Switch II Pocket on KRAS Leads to a Potent, In Vivo Active KRASG12C Inhibitor
Authors
Keywords
-
Journal
Journal of Medicinal Chemistry
Volume 65, Issue 21, Pages 14614-14629
Publisher
American Chemical Society (ACS)
Online
2022-10-27
DOI
10.1021/acs.jmedchem.2c01120
References
Ask authors/readers for more resources
Related references
Note: Only part of the references are listed.- High-Throughput Kinetic Characterization of Irreversible Covalent Inhibitors of KRASG12C by Intact Protein MS and Targeted MRM
- (2022) Ke Sherry Li et al. ANALYTICAL CHEMISTRY
- The path to the clinic: a comprehensive review on direct KRASG12C inhibitors
- (2022) Albert K. Kwan et al. JOURNAL OF EXPERIMENTAL & CLINICAL CANCER RESEARCH
- Conformation-locking antibodies for the discovery and characterization of KRAS inhibitors
- (2022) Christopher W. Davies et al. NATURE BIOTECHNOLOGY
- Expanding the Reach of Precision Oncology by Drugging All KRAS Mutants
- (2022) Marco H. Hofmann et al. Cancer Discovery
- Identification of MRTX1133, a Noncovalent, Potent, and Selective KRASG12D Inhibitor
- (2021) Xiaolun Wang et al. JOURNAL OF MEDICINAL CHEMISTRY
- The Frequency of Ras Mutations in Cancer
- (2020) Ian A. Prior et al. CANCER RESEARCH
- Identification of the Clinical Development Candidate MRTX849, a Covalent KRASG12C Inhibitor for the Treatment of Cancer
- (2020) Jay B. Fell et al. JOURNAL OF MEDICINAL CHEMISTRY
- Drugging all RAS isoforms with one pocket
- (2020) Dirk Kessler et al. Future Medicinal Chemistry
- RAS-targeted therapies: is the undruggable drugged?
- (2020) Amanda R. Moore et al. NATURE REVIEWS DRUG DISCOVERY
- BI-3406, a potent and selective SOS1::KRAS interaction inhibitor, is effective in KRAS-driven cancers through combined MEK inhibition
- (2020) Marco H Hofmann et al. Cancer Discovery
- Drugging an undruggable pocket on KRAS
- (2019) Dirk Kessler et al. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
- The clinical KRAS(G12C) inhibitor AMG 510 drives anti-tumour immunity
- (2019) Jude Canon et al. NATURE
- The KRASG12C Inhibitor MRTX849 Provides Insight toward Therapeutic Susceptibility of KRAS-Mutant Cancers in Mouse Models and Patients
- (2019) Jill Hallin et al. Cancer Discovery
- Discovery of a Covalent Inhibitor of KRASG12C (AMG 510) for the Treatment of Solid Tumors
- (2019) Brian A. Lanman et al. JOURNAL OF MEDICINAL CHEMISTRY
- Expanding the Armory: Predicting and Tuning Covalent Warhead Reactivity
- (2017) Richard Lonsdale et al. Journal of Chemical Information and Modeling
- Allele-specific inhibitors inactivate mutant KRAS G12C by a trapping mechanism
- (2016) P. Lito et al. SCIENCE
- Intrinsic reactivity profile of electrophilic moieties to guide covalent drug design: N-α-acetyl-l-lysine as an amine nucleophile
- (2016) Upendra P. Dahal et al. MedChemComm
- Selective Inhibition of Oncogenic KRAS Output with Small Molecules Targeting the Inactive State
- (2016) M. P. Patricelli et al. Cancer Discovery
- A method for the second-site screening of K-Ras in the presence of a covalently attached first-site ligand
- (2014) Qi Sun et al. JOURNAL OF BIOMOLECULAR NMR
- K-Ras(G12C) inhibitors allosterically control GTP affinity and effector interactions
- (2013) Jonathan M. Ostrem et al. NATURE
- Using chemical shift perturbation to characterise ligand binding
- (2013) Mike P. Williamson PROGRESS IN NUCLEAR MAGNETIC RESONANCE SPECTROSCOPY
- Discovery of Small Molecules that Bind to K-Ras and Inhibit Sos-Mediated Activation
- (2012) Qi Sun et al. ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
- Small-molecule ligands bind to a distinct pocket in Ras and inhibit SOS-mediated nucleotide exchange activity
- (2012) T. Maurer et al. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
Find the ideal target journal for your manuscript
Explore over 38,000 international journals covering a vast array of academic fields.
SearchCreate your own webinar
Interested in hosting your own webinar? Check the schedule and propose your idea to the Peeref Content Team.
Create Now