New paper out in Cell Chemical Biology!

We are thrilled to share a story emerging from our androgen receptor program is now available for download at Cell Chemical Biology!

This work, co-led by Dr. Andre Richters and Dr. Shelby Doyle, has been a long-running effort from our team focused on prostate cancer, who discovered KI-ARv-03, a selective CDK9 inhibitor with potent activity in castration resistant prostate cancer models. The initial discovery was supported through a partnership with Janssen Pharmaceuticals and validated in collaboration with the lab of Dr. Steven Balk through the Koch Institute and Dana-Farber/Harvard Cancer Center (DF/HCC) Bridge Project. More recently this project grew to collaborative effort between our lab, colleagues at the Therapeutic Innovation Center at Baylor College of Medicine, and Kronos Bio, Inc., who optimized KI-ARv-03 to produce KB-0742.

We are grateful to the entire team of authors and extend congratulations to all!

REFERENCE: *André Richters, *Shelby K. Doyle, David B. Freeman, Christina Lee, Becky S. Leifer, Sajjeev Jagannathan, Florian Kabinger, Jošt Vrabič Koren, Nicholas B. Struntz, Julie Urgiles, Ryan A. Stagg, Brice H. Curtin, Deep Chatterjee, Sebastian Mathea, Peter J. Mikochik, Tamara D. Hopkins, Hua Gao, Jonathan Branch, Hong Xin, Lori Westover, Gilles C. Bignan, Brent A. Rupnow, Kristen L. Karlin, Calla M. Olson, Thomas F. Westbrook, Joseph Vacca, Chris M. Wilfong, B. Wesley Trotter, Douglas C. Saffran, Norbert Bischofberger, Stefan Knapp, Joshua W. Russo, Ian Hickson, James R. Bischoff, Marco M. Gottardis, Steven P. Balk, Charles Y. Lin, Marius S. Pop, Angela N. Koehler. “Modulating Androgen Receptor-Driven Transcription in Prostate Cancer with Selective CDK9 Inhibitors.” Cell Chemical Biology. Open Access Published: October 20, 2020 DOI:https://doi.org/10.1016/j.chembiol.2020.10.001

New paper on our Max-directed chemical probe is out in Cell Chemical Biology!

We are very excited to finally share in long-form the story of KI-MS2-008, a Max-directed small molecule probe that attenuates Myc-driven transcription, which is now available for download at Cell Chemical Biology!

This work has been a highly collaborative team effort—originating in the work of many Koehler lab alumni and affiliates; greatly enhanced by the contributions of collaborators at Stanford University, Baylor College of Medicine, Brigham and Women’s Hospital, and Dana-Farber Cancer Institute; and championed by lead authors Nick Struntz and Andrew Chen. We are grateful to the team and extend congratulations to all!

Graphical abstract from our most recent publication on KI-MS2-008 in Cell Chemical Biology.

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For a non-technical description of this project and its impact, please see our feature on MIT News.

For the short form specifications on the chemical probe and its discovery, please see our new pages for KI-MS2-008 and Max on our probe and target pages, respectively.

To request access to the compound, please visit our contact page.
The compound is not currently available from commercial sources; however, we intend to make the probe available to any colleagues unable to synthesize the molecule who wish to leverage the molecule for their own studies.