PMID

Data

Article Title

Organization

Progress in discovery of small-molecule modulators of protein-protein interactions via fragment screening.

Pfizer

Bisphenol A binds to Ras proteins and competes with guanine nucleotide exchange: implications for GTPase-selective antagonists.

Ruhr University Of Bochum

Targeting mutant KRAS for anticancer therapeutics: a review of novel small molecule modulators.

The University Of Arizona

Macrocycles are great cycles: applications, opportunities, and challenges of synthetic macrocycles in drug discovery.

Universite£

Fragment Optimization of Reversible Binding to the Switch II Pocket on KRAS Leads to a Potent, In Vivo Active KRAS

Boehringer Ingelheim Rcv

Discovery of AZD4625, a Covalent Allosteric Inhibitor of the Mutant GTPase KRAS

Astrazeneca

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

Southern Medical University

Efficient targeted oncogenic KRAS

Jinan University

Zinc enzymes in medicinal chemistry.

Hefei University Of Technology

Targeting KRAS mutant cancers by preventing signaling transduction in the MAPK pathway.

Massachusetts College Of Pharmacy And Health Sciences University

Drugging the Next Undruggable KRAS Allele-Gly12Asp.

University Of California San Francisco

Accelerated Identification of Cell Active KRAS Inhibitory Macrocyclic Peptides using Mixture Libraries and Automated Ligand Identification System (ALIS) Technology.

Merck

KRAS Inhibitors and Target Engagement Technology: From Undruggable to Druggable Targets in Cancer Therapeutics.

Usona Institute

Cyclic Peptide Screening Methods for Preclinical Drug Discovery.

University Of Washington

Discovery of novel Quinazoline-based KRAS G12C inhibitors as potential anticancer agents.

Sun Yat-Sen University

Discovery and biological evaluation of 1-{2,7-diazaspiro[3.5]nonan-2-yl}prop-2-en-1-one derivatives as covalent inhibitors of KRAS G12C with favorable metabolic stability and anti-tumor activity.

Astellas Pharma

Targeting a Novel KRAS Binding Site: Application of One-Component Stapling of Small (5-6-mer) Peptides.

Cambridge University

Small-Molecule Inhibitor of the Oncogenic KRAS

Usona Institute

Identification of MRTX1133, a Noncovalent, Potent, and Selective KRAS

Mirati Therapeutics

A Series of Pyrazole Analogs Binding to KRASG12C as Potential Cancer Treatment.

Arrival Discovery

Targeting KRAS G12D Mutant for the Potential Treatment of Pancreatic Cancer.

Usona Institute

Targeting KRAS Mutant Protein Inhibitor for Potential Treatment in Cancer.

Usona Institute

Discovery of a Bicyclic Peptidyl Pan-Ras Inhibitor.

The Ohio State University

Targeting the KRAS G12D Mutant as Potential Therapy in Cancer.

Usona Institute

Dual Inhibition of KRAS G12C and G12D Mutants as a Potential Treatment in Cancer Therapy.

Usona Institute

Small Molecule Inhibitors of KRAS G12C Mutant.

Usona Institute

Small Molecule Inhibitors of KRAS Mutant as a Therapeutic Strategy for the Treatment of Cancer.

Usona Institute

Design, synthesis and pharmacological evaluation of bicyclic and tetracyclic pyridopyrimidinone analogues as new KRAS

Shanghai Institute Of Materia Medica (Simm)

Drugging the undruggable: a computational chemist's view of KRAS

Astrazeneca

De-risking Drug Discovery of Intracellular Targeting Peptides: Screening Strategies to Eliminate False-Positive Hits.

Msd

Chemical Proteomic Characterization of a Covalent KRASG12C Inhibitor.

Lilly Research Laboratories

Fragment-to-Lead Medicinal Chemistry Publications in 2019.

Novartis Institutes For Biomedical Research

Identification of TNO155, an Allosteric SHP2 Inhibitor for the Treatment of Cancer.

TBA

Small-Molecule Inhibitors Directly Targeting KRAS as Anticancer Therapeutics.

Jinan University

Chalcones bearing a 3,4,5-trimethoxyphenyl motif are capable of selectively inhibiting oncogenic K-Ras signaling.

Wright State University

Identification of the Clinical Development Candidate

Array Biopharma

Structure-Based Design and Pharmacokinetic Optimization of Covalent Allosteric Inhibitors of the Mutant GTPase KRAS

Astrazeneca

Inhibitors of G12C Mutant Ras Proteins for the Treatment of Cancers.

Usona Institute

Selective apoptosis-inducing activity of synthetic hydrocarbon-stapled SOS1 helix with d-amino acids in H358 cancer cells expressing KRAS

China Pharmaceutical University

Inhibitors of KRAS May Potentially Provide Effective Cancer Treatment.

Therachem Research Medilab

Discovery of

Amgen

Discovery of a Covalent Inhibitor of KRAS

TBA

Discovery of Tetrahydropyridopyrimidines as Irreversible Covalent Inhibitors of KRAS-G12C with In Vivo Activity.

Array Biopharma

Discovery of covalent enzyme inhibitors using virtual docking of covalent fragments.

University Of Houston

Covalent Guanosine Mimetic Inhibitors of G12C KRAS.

Dana Farber Cancer Institute

New Frontiers in Druggability.

Stony Brook University

Inhibition of Ras-Effector Interaction by Cyclic Peptides.

The Ohio State University

Precedence and Promise of Covalent Inhibitors of EGFR and KRAS for Patients with Non-Small-Cell Lung Cancer.

Pfizer

Crystal Structure of a Human K-Ras G12D Mutant in Complex with GDP and the Cyclic Inhibitory Peptide KRpep-2d.

Takeda Pharmaceutical

Investigation of the structural requirements of K-Ras(G12D) selective inhibitory peptide KRpep-2d using alanine scans and cysteine bridging.

Takeda Pharmaceutical