Gary Schiltz
@garyeschiltz.bsky.social
Happy to share a new publication with @leonidasplatan1.bsky.social and the @luriecancer.bsky.social where we identified new inhibitors of the mTORC2-specific protein SIN1. These represent novel mTORC2 chemical probes while possessing intriguing anti-cancer activity.
aacrjournals.org/mct/article-...
aacrjournals.org/mct/article-...
Development of a SIN1 Targeting Inhibitor as a Novel Therapeutic Approach for the Treatment of Malignancies
Abstract. The essential role of mTOR in promoting tumorigenesis of many cancers makes it an attractive therapeutic target. However, catalytic mTOR inhibitors, which block both mTORC1 and mTORC2, resul...
aacrjournals.org
January 14, 2026 at 1:25 PM
Happy to share a new publication with @leonidasplatan1.bsky.social and the @luriecancer.bsky.social where we identified new inhibitors of the mTORC2-specific protein SIN1. These represent novel mTORC2 chemical probes while possessing intriguing anti-cancer activity.
aacrjournals.org/mct/article-...
aacrjournals.org/mct/article-...
Excited for this new paper with Dr. Jindan Yu. We describe a set of EZH2 PROTACs that potently and selectively degrade EZH2 and block both enzymatic and non-enzymatic functions. Our degrader shows greater anti-tumor efficacy than EZH2 inhibitor EPZ6438 in a prostate cancer tumor model.
rdcu.be/eYbkG
rdcu.be/eYbkG
January 8, 2026 at 4:43 PM
Excited for this new paper with Dr. Jindan Yu. We describe a set of EZH2 PROTACs that potently and selectively degrade EZH2 and block both enzymatic and non-enzymatic functions. Our degrader shows greater anti-tumor efficacy than EZH2 inhibitor EPZ6438 in a prostate cancer tumor model.
rdcu.be/eYbkG
rdcu.be/eYbkG
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.
October 18, 2025 at 12:16 PM
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.
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/...
Discovery of Potent and Selective MNK Kinase Inhibitors for the Treatment of Leukemia | Journal of Medicinal Chemistry pubs.acs.org/doi/10.1021/...
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...
pubs.acs.org
March 4, 2025 at 3:24 PM
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/...
Discovery of Potent and Selective MNK Kinase Inhibitors for the Treatment of Leukemia | Journal of Medicinal Chemistry pubs.acs.org/doi/10.1021/...
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/...
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...
pubs.acs.org
February 13, 2025 at 7:10 PM
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/...
pubs.acs.org/doi/10.1021/...