Design, Synthesis, and Pharmacological Evaluation of Multisubstituted Pyrido[4,3-d]pyrimidine Analogues Bearing Deuterated Methylene Linkers as Potent KRASG12D Inhibitors

Feedback activation of EGFR/wild-type RAS signaling axis limits KRASG12D inhibitor efficacy in KRASG12D-mutated colorectal cancer

(2023) Juanjuan Feng et al.   ONCOGENE

Drugging the Next Undruggable KRAS Allele-Gly12Asp

(2022) Qinheng Zheng et al.   JOURNAL OF MEDICINAL CHEMISTRY

Expanding the Reach of Precision Oncology by Drugging All KRAS Mutants

(2022) Marco H. Hofmann et al.   Cancer Discovery

A Structure Is Worth a Thousand Words: New Insights for RAS and RAF Regulation

(2022) Dhirendra K. Simanshu et al.   Cancer Discovery

KRAS(G12D) can be targeted by potent inhibitors via formation of salt bridge

(2022) Zhongwei Mao et al.   Cell Discovery

Discovery of Thieno[2,3-d]pyrimidine-based KRAS G12D inhibitors as potential anticancer agents via combinatorial virtual screening

(2022) Ling Li et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

KRAS is vulnerable to reversible switch-II pocket engagement in cells

(2022) James D. Vasta et al.   Nature Chemical Biology

Classification of KRAS-Activating Mutations and the Implications for Therapeutic Intervention

(2022) Christian Johnson et al.   Cancer Discovery

Anti-tumor efficacy of a potent and selective non-covalent KRASG12D inhibitor

(2022) Jill Hallin et al.   NATURE MEDICINE

KRAS G12D targeted therapies for pancreatic cancer: Has the fortress been conquered?

(2022) Sahar F. Bannoura et al.   Frontiers in Oncology

BCL6 confers KRAS-mutant non–small-cell lung cancer resistance to BET inhibitors

(2021) Jiawei Guo et al.   JOURNAL OF CLINICAL INVESTIGATION

Design, Synthesis, and Pharmacological Evaluation of Biaryl-Containing PD-1/PD-L1 Interaction Inhibitors Bearing a Unique Difluoromethyleneoxy Linkage

(2021) Zilan Song et al.   JOURNAL OF MEDICINAL CHEMISTRY

Identification of MRTX1133, a Noncovalent, Potent, and Selective KRASG12D Inhibitor

(2021) Xiaolun Wang et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

RAS-targeted therapies: is the undruggable drugged?

(2020) Amanda R. Moore et al.   NATURE REVIEWS DRUG DISCOVERY

Small-Molecule Inhibitors Directly Targeting KRAS as Anticancer Therapeutics

(2020) Hao Chen et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

Targeting KRAS Mutant Cancers with a Covalent G12C-Specific Inhibitor

(2018) Matthew R. Janes et al.   CELL

Therapeutic strategies to target RAS-mutant cancers

(2018) Meagan B. Ryan et al.   Nature Reviews Clinical Oncology

Drugging RAS: Know the enemy

(2017) Bjoern Papke et al.   SCIENCE

Drugging the undruggable RAS: Mission Possible?

(2014) Adrienne D. Cox et al.   NATURE REVIEWS DRUG DISCOVERY