Phospholipase C zeta 1 (PLCζ1): a promising target as a non-hormonal contraceptive

Background 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 Read More …

Characterization and Assessment of KCNU1/SLO3 as a Potential Non-hormonal Contraceptive Target

Characterization and Assessment of KCNU1/SLO3 as a Potential Non-hormonal Contraceptive Target 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 …

Assessing Ovastacin and Fetuin B as a Non-Hormonal Contraceptive Targets

Background: Ovastacin is an oocyte-specific protease involved in sperm adhesion and fertilization. Research into the ovastacin’s protease function suggest it acts on the post-fertilization cleavage of ZP2 via cortical granule exocytosis1. Cleaved ZP2 then causes hardening of the zona pellucida and is then unable to support further sperm binding2. Zona pellucida regulation is critical for Read More …

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 …

TBXT Ligands for Chordoma: Priority series molecules

Our chordoma research focused on developing small reversible molecules targeting the transcription factor TBXT which codes for the brachyury protein. Brachyury contains several shallow pockets, and through an x-ray crystallography fragment based approach we previously identified several series of small fragments bound to it (TBXT Fragment Hits). Our medicinal chemistry project aimed to grow the Read More …

TBXT Ligands for Chordoma: Covalent Inhibitors Targeting CYS122 Part A: Benzamides

By Zachary Davis-Gilbert, Anwar Hossain, and David H. Drewry* In conjunction with our efforts to target TBXT via non-covalent small molecules, we have also been developing covalent compounds that bind to CYS122, which has previously been shown to be accessible by afatinib (pdb code 6ZU8). In this blog post, I will discuss the progress made Read More …

In vivo characterization of antibodies directed against TREAT-AD target proteins in mouse model of AD pathology

In vivo characterization of antibodies directed against TREAT-AD target proteins in mouse model of AD pathology Suzanne Doolen, Riham Ayoubi, Carl Laflamme, Ranjita Betarbet, Elizabeth Zoeller, Sean-Paul G. Williams and Stacey J. Sukoff Rizzo https://doi.org/10.5281/zenodo.6612215 Our goal in support of the Emory-Sage-Structural Genomics Consortium (SGC) TREAT-AD Center is to develop and identify high-quality tools to Read More …