Recent Experiments

PLCζ1: a promising target for non-hormonal contraceptives

The Structural Genomics Consortium (SGC) has been funded by the Bill & Melinda Gates Foundation to research Women’s and Children’s Health, focusing on the advancement of drug discovery in reproductive biology and disease, child development, and childhood diseases. The SGC plans to generate protein reagents and chemical probes for several potential drug targets for new, Read More …

PATL2: A Potential Contraceptive Target August 2023 Update

PATL2: A Potential Contraceptive Target A promising protein target for NHCs is Protein Associated with Topoisomerase II Homolog 2 (PATL2), a highly conserved, oocyte-specific mRNA-binding protein that represses translation1. For consanguineous families, the inheritance pattern for PATL2 is recessive; thus, infertility is often caused by homozygous mutations in the gene2. Although some mutations in PATL2 Read More …

GRC Poster: Identification of SARS-CoV-2 helicase inhibitors by large-scale virtual screening

by Mohammad Anwar Hossain1, Konstantin Popov2, Sumera Perveen3, Kesatebrhan Haile Asressu1, Kenneth Hugh Pearce Jr.2, Cheryl Arrowsmith3, Peter Brown1, Alexander Tropsha4, Tim Willson1 1Structural Genomics Consortium, The University of North Carolina at Chapel Hill, Chapel Hill, NC, USA; 2CICBDD, UNC Eshelman School of Pharmacy; 3The Structural Genomics Consortium, University of Toronto, Canada; 4CBMC, UNC Eshelman Read More …

A systematic review of drug-like ligands bound to helicases in the PDB

Introduction A current focus in the field of antiviral drug discovery are helicases, which are motor enzymes responsible for ATP-dependent nucleic acid duplex unwinding. Helicases of all superfamilies (SF) have stretches of amino acids called motifs, that are conserved within an SF and similar across SFs. For this reason, established helicase inhibitors interacting with these Read More …

Release of The Kinase Chemogenomic Set 2.0 (KCGS2.0)

Introduction Situation Kinases are useful for drug discovery – many opportunities! Kinase by kinase probe development is important, but it will take too long to discover a probe for each kinase Disease relevant phenotypic assays need smart compounds sets Numerous high quality kinase inhibitors exist in the literature and in company collections Kinases are “connected” Read More …