TBXT Ligands for Chordoma: Covalent Inhibitors Targeting CYS122 Part B: Quinazolines

In this blog post, I will discuss the progress made on improving the binding affinity of new covalent quinazolines targeting CYS122, as well as some of the directions we are taking to further improve binding affinity to TBXT and reduce binding affinity towards EGFR. The synthetic work has been primarily driven by Zach and our Read More …

Baculovirus expression of FIGLA to characterize as a Non-Hormonal Contraceptive Target

Background The Bill and Melinda Gates Foundation awarded the Structural Genomics Consortium with the SGC Women’s and Children’s Health Initiative in September 2021.  The initiative targets a group of proteins for effective non-hormonal contraceptive agents.  Each target protein will be purified and characterized to screen for possible chemical probes and drug candidates. SGC-UNC was assigned Read More …

Assessing PATL2 as a Non-hormonal Contraceptive Target

For clearer figures, please see this post at: https://zenodo.org/record/6993848#.Yv6Kwj3MI2w   Introduction   Project Proposal The Structural Genomics Consortium (SGC) has recently embarked on its first research project in reproductive biology as a part of the SGC’s new open science Women’s and Children’s Health Program (WCHP). This program, which was generously funded by the Bill & Read More …

A promising target for non-hormonal contraception – The α/β Hydrolase Domain 2

The Background In the scope of the SGC’s (Structural Genomics Consortium) Women’s and Children’s Health Initiative, a group of proteins that are potential targets for new, safe, and effective non-hormonal contraceptives will be characterized. These will then used as a template to screen for possible chemical probes and drug candidates. A group of postdoctoral researchers Read More …