Project Grant R16GM165398
- The National Institute of General Medical Sciences awarded New York Institute of Technology $204,907 on July 1, 2026, under the Biomedical Research and Research Training program (CFDA 93.859) to design, synthesize, and biologically evaluate potent and selective pyruvate carboxylase (PC) inhibitors for studying cancer cell metabolism. The project employs structure-based drug discovery to generate small molecule inhibitors targeting PC, an enzyme at the convergence of central metabolic pathways...
- The National Institute of General Medical Sciences awarded the Research Foundation of The City University of New York $154,500 on July 17, 2026, under the Biomedical Research and Research Training program (CFDA 93.859) to develop and validate next-generation allosteric PRC2 inhibitors for cancer epigenetics. The research optimizes a lead compound, DAB003-8C, a stapled peptide targeting the SANT1L domain of EZH2 to inhibit polycomb repressive complex 2 through an allosteric mechanism distinct...
- The National Institute of General Medical Sciences awarded St. John's University $249,574 on July 1, 2026, under the Biomedical Research and Research Training program (CFDA 93.859) to acquire a Shimadzu LCMS-8045RX triple quadrupole liquid chromatography-mass spectrometry (LC-MS/MS) instrument with Nexera XS ultra-high-performance liquid chromatography and associated accessories. The instrument supports pharmaceutical and biomedical research in the Department of Pharmaceutical Sciences, enabling...
- The National Institute of General Medical Sciences, part of the Department of Health and Human Services National Institutes of Health, awarded The Johns Hopkins University $559,800 on July 1, 2026, under the Biomedical Research and Research Training program (CFDA 93.859) to develop rapafucin-based chemical probes and drug leads targeting undruggable protein interactions. The award funds mechanistic investigation and structural optimization of four rapafucin compounds: rapaprotin, a novel...
- The National Cancer Institute awarded Albert Einstein College of Medicine $692,197 on May 1, 2026, under the Cancer Treatment Research program (CFDA 93.395) to develop MTAP transition state analog inhibitors for synthetic-lethal cancer therapy. The award funds research into methylthioadenosine phosphorylase (MTAP) inhibitors designed to convert MTAP-positive tumors to an MTAP-deleted phenotype, rendering them sensitive to existing MAT2A and PRMT5 inhibitors in clinical trials. Current MAT2A...
- The National Cancer Institute awarded the University of Pittsburgh $435,788 on April 1, 2026, under the Cancer Treatment Research program (CFDA 93.395) to develop active site-directed inhibitors and bifunctional degraders targeting mutant isocitrate dehydrogenase enzymes (IDH1 and IDH2). The project addresses acquired resistance to FDA-approved allosteric IDH inhibitors (ivosidenib and enasidenib) that has emerged in cancer patients with IDH mutations in gliomas and hematological malignancies....
- This Project Grant from the National Science Foundation's Division of Molecular and Cellular Biosciences, under the Biological Sciences program (CFDA 47.074), provides $804,836 to the Van Andel Research Institute to study the role of poly(ADP-ribose) polymerase 1 (PARP1) in regulating RNA polymerase II elongation and mRNA splicing. The award aims to advance understanding of PARP1's function in RNA biogenesis through large-scale genomics and gene-specific approaches to map PARP1's genetic and...
- The National Institute of General Medical Sciences awarded The Research Foundation For The State University of New York $434,892 on September 1, 2026, under the Biomedical Research and Research Training program (CFDA 93.859) to support structural and biosynthetic research on natural product enzymes. The award funds investigation of nonribosomal peptide synthetases (NRPSs) and NRPS-independent siderophore biosynthetic pathways, with focus on the conformational dynamics that NRPSs employ to...
- The National Institute of General Medical Sciences awarded The Trustees of Princeton University $451,000 on April 1, 2026, under the Biomedical Research and Research Training program (CFDA 93.859) for discovery and engineering of enzymes that modify amino acids and peptides for use as synthetic tools in biomedical research. The research develops methods to discover, characterize, and engineer enzymes and metabolic pathways involved in amino acid and peptide modification. The work focuses on...
- The National Institute of General Medical Sciences awarded Northeastern University $440,000 on July 1, 2026, under the Biomedical Research and Research Training program (CFDA 93.859) to discover novel antimicrobial molecules from clostridial biosynthesis. The project characterizes cobalamin-dependent radical S-adenosylmethionine enzymes fused with non-ribosomal peptide synthetase adenylation domains found in clostridial genomes. The recipient will conduct biochemical characterization of these...
The National Institute of General Medical Sciences awarded St. John's University, New York, $150,000 on August 1, 2026, under the Biomedical Research and Research Training program (CFDA 93.859) to discover and develop novel pentacyclic indolocyclopentaphthalazinone PARP1 inhibitors for cancer treatment. The research addresses limitations of existing PARP inhibitors, which potently inhibit both PARP1 and PARP2 enzymes and exhibit variable clinical efficacy compromised by dose-limiting toxicities and acquired drug resistance. The project aims to develop a novel class of highly selective PARP1 inhibitors that exhibit moderate PARP1 trapping potency while evading ABC transporter-mediated efflux. The work builds on a published discovery from the recipient's laboratory featuring lead compound 5, which demonstrates single-digit nanomolar potency against PARP1 with greater than 25-fold selectivity over PARP2 and other PARP enzymes. Lead compound 5 shows substantially lower PARP1 trapping compared to talazoparib and favorable oral bioavailability with desirable Caco-2 permeability and efflux ratios, potentially enabling application to brain tumors and combination therapies while mitigating hematologic toxicity. Performance occurs in Jamaica, New York. The period of performance runs from August 1, 2026, through April 30, 2030.
Mod # | Description | ReasonForModification | Federal Obligation | Date |
|---|---|---|---|---|
| Not listed | $150.0k | 7/24/26 |