Grant ID | RR220012 |
Awarded On | November 18, 2021 |
Title | Recruitment of First-Time, Tenure-Track Faculty Members |
Program | CPRIT Scholar |
Award Mechanism | Recruitment of First-Time, Tenure-Track Faculty Members |
Institution/Organization | Baylor College of Medicine |
Principal Investigator/Program Director | Mingxing Teng |
Cancer Sites | Breast, Lymphoma, Pancreas |
Contracted Amount | $2,000,000 |
Summary of Goals and Objectives |
Global profiling of cysteine reactivity and ligandability in the human proteome has been performed, making most covalent fragment libraries cysteine-focused, leaving the space of other nucleophilic residues such as serine, threonine, tyrosine, and lysine poorly explored. In addition, the cysteine-targeting covalent fragment hits are often either too reactive in the warhead part or too simple in structure, which poses challenges for further optimization and differentiation. Natural products are a rich source of novel chemotypes and electrophilic moieties but are difficult to access by chemical synthesis. The goal of the proposed research is to simplify and modify the natural products into cov... |