I. Chau

A resource to enable chemical biology and drug discovery of WDR Proteins

The paper develops a resource for discovering ligands for WDR proteins using experimental and computational methods, leading to the identification of drug-like ligands for 9 out of 20 targets.

Drug Discovery in Low Data Regimes: Leveraging a Computational Pipeline for the Discovery of Novel SARS-CoV-2 Nsp14-MTase Inhibitors

This paper introduces a computational pipeline for identifying SARS-CoV-2 nsp14 inhibitors using virtual screening, identifying seven candidates including NSC620333 and SS148, with experimental validation of binding affinity and structural insights.

Probing the mechanism of Cbl-b inhibition by a small-molecule inhibitor

The paper investigates how a small-molecule inhibitor binds to and inactivates Cbl-b, revealing a structural mechanism that locks the protein in an inactive conformation.

Structure-based discovery of inhibitors of the SARS-CoV-2 Nsp14 N7-methyltransferase

The paper identifies multiple inhibitors of SARS-CoV-2 Nsp14 N7-methyltransferase using docking strategies, with some showing sub-10 M potency and selectivity.

Genetic and immune landscape evolution defines subtypes of MMR deficient colorectal cancer

The paper identifies three subtypes of MMR deficient colorectal cancer based on genetic and immune landscape evolution, linking them to T-cell infiltrates and checkpoint-inhibitor resistance.

Pharmacological targeting of a PWWP domain demonstrates cooperative control of NSD2 localization

The paper develops a chemical probe, UNC6934, that targets the PWWP1 domain of NSD2, revealing cooperative control of NSD2 localization through chromatin reader domains.

Probing the SAM Binding Site of SARS-CoV-2 nsp14 in vitro Using SAM Competitive Inhibitors Guides Developing Selective bi-substrate Inhibitors

This paper identifies SAM competitive inhibitors of SARS-CoV-2 nsp14 methyltransferase and characterizes their mechanism, guiding the development of selective bi-substrate inhibitors.

A First-in-class, Highly Selective and Cell-active AllostericInhibitor of Protein Arginine Methyltransferase 6 (PRMT6)

This paper reports the discovery of a first-in-class, highly selective allosteric inhibitor of PRMT6, SGC6870, with potent activity and selectivity in vitro and in cells.

Mutational processes impact the evolution of anti-EGFR antibody resistance in colorectal cancer

The paper investigates mutational processes in colorectal cancer resistance to anti-EGFR antibodies, finding that mutational Signature 17 predicts resistance evolution and shorter progression-free survival.

Genomic and transcriptomic determinants of therapy resistance and immune landscape evolution during anti-EGFR treatment in colorectal cancer

The paper analyzes genomic and transcriptomic data from CRC patients treated with cetuximab to identify resistance mechanisms and immune landscape changes during anti-EGFR therapy.