Gary Schiltz

Novel PROTACs targeting tissue transglutaminase (TG2) suppress tumorigenicity of ovarian cancer cells Tissue transglutaminase (TG2), a multifunctional enzyme involved in protein crosslinking through transamidation, fibronectin–integrin interactions and…

Excitingly, our most promising new compound (P374) shows in vivo activity at reducing omentum colonization of ovarian cancer cells and significantly reduced tumor weights, tumor volumes, and the number of ovarian tumors.

www.sciencedirect.com/science/arti...

Happy to share our latest work in collaboration with Dr. Daniela Matei, Dr. Joshua Zhu, and Purav Vagadia. We developed new TG2 protein degraders to treat ovarian cancer that block both enzymatic and non-enzymatic activities of multi-functional TG2 even though they do not bind the catalytic site.

Discovery of Potent and Selective MNK Kinase Inhibitors for the Treatment of Leukemia MNK activity is regulated by the p38 and Erk MAPK pathways. Phosphorylation of MNK leads to its activation and binding to the eIF4G/eIF4E complex. MNK then phosphorylates eIF4E at Ser209, whose activa...

Happy to share a new paper from my team. Chemistry was led by talented medicinal chemist Purav Vagadia collaborating with @leonidasplatan1.bsky.social

Discovery of Potent and Selective MNK Kinase Inhibitors for the Treatment of Leukemia | Journal of Medicinal Chemistry pubs.acs.org/doi/10.1021/...

Rational Design and Optimization of a Potent IDO1 Proteolysis Targeting Chimera (PROTAC) Indoleamine 2,3-dioxygenase 1 (IDO1) is an immunosuppressive protein that inhibits antitumor immunity through both tryptophan metabolism and nonenzymatic functions. Drugs targeting IDO1 enzyme activit...

Happy to share my latest work developing IDO1 degraders. This is the result of a fantastic collaboration with @dwainwright-phd.bsky.social and his group. The medicinal chemistry was led by an amazing postdoctoral fellow Dr. Paige Monsen (now at Foghorn Therapeutics).

pubs.acs.org/doi/10.1021/...