University of Michigan

Kura Oncology, Inc.

Other

Vanderbilt University

University of Virginia Patent Foundation

Tomasz Cierpicki

Jolanta Grembecka

Dmitry Borkin

Szymon Klossowski

Pingda Ren

Liansheng Li

Tao Wu

Jonathan Pollock

EunGi Kim

Hongzhi Miao

Hao Li

Jing Deng

Yi Liu

Jun Feng

Duxin Sun

Trupta Purohit

Jay L Hess

Yi Wang

Xiaoqin Li

Dong Chen

Wenbing Chen

Felicia Gray

Huang Huang

Qingjie Zhao

Sergei Zari

Hyo Je Cho

Mykhaylo Potopnyk

Sergii Dudkin

Yassir Adam

Christina Howard

Weijiang Ying

Yiwu Yao

Shaun R Stauffer

Kevin Lloyd Greenman

Rocco D Gogliotti

Mohamed Ibrahim

Deanna Montgomery

Artem Plekhov

Marta Krotoska

Zhuang Jin

David Rogawski

Dymytrii Listunov

Alyssa Winkler

Brian Linhares

Timothy J Senter

Sunil Kumar Upadhyay

Jin Zhuang

Marta Szewczyk

Provided herein are small molecule inhibitors of Polycomb Repressive Complex 1 (PRC1) activity, and methods of use thereof for the treatment of disease, including leukemia and other cancers, as well as other diseases dependent on the activity of PRC1.

PRC1 inhibitors and methods of treatment therewith

Provided herein are small molecule inhibitors of NSD1, NSD2 and/or NSD3 activity, and methods of use thereof for the treatment of disease, including leukemia, breast cancer, osteosarcoma, lung and prostate cancers and other solid tumors as well as other diseases dependent on the activity of NSD1, NSD2 and/or NSD3.

NSD family inhibitors and methods of treatment therewith

Provided herein are small molecules comprising a first domain that binds to ASH1L and a second domain that facilitates ASH1L degradation. In particular, ASH1L-targeting proteolysis targeting chimeras (PROTACs) and methods of use thereof for the treatment of disease (e.g., acute leukemia, solid cancers and other diseases dependent on activity of ASH1L) are provided.

ASH1L degraders and methods of treatment therewith

Provided herein are small molecule inhibitors of ASH1L activity and small molecules that facilitate ASH1L degradation and methods of use thereof for the treatment of disease, including acute leukemia, solid cancers and other diseases dependent on activity of ASH1L.

ASH1L inhibitors and methods of treatment therewith

Provided herein are small molecules that bind to GAS41 and inhibit GAS41 activity, and methods of use thereof for the treatment of cancer.

GAS41 inhibitors and methods of use thereof

Provided herein are small molecules that bind to ASH1L and inhibit ASH1L activity, and methods of use thereof for the treatment of disease, including acute leukemia, solid cancers and other diseases dependent on activity of ASH1L.

The present disclosure provides compounds and methods for inhibiting the interaction of menin with its upstream or downstream signaling molecules including but not limited to MLL1, MLL2 and MLL-fusion oncoproteins. Compounds of the disclosure may be used in methods for the treatment of a wide variety of cancers and other diseases associated with one or more of MLL1, MLL2, MLL fusion proteins, and menin.

Thienopyrimidine and thienopyridine compounds and methods of use thereof

The present disclosure provides methods of inhibiting the interaction of menin with MLL1, MLL2 and MLL-fusion oncoproteins with compositions of Formula (II-A). The methods are useful for the treatment of leukemia, solid cancers, diabetes and other diseases dependent on activity of MLL1, MLL2, MLL fusion proteins, and/or menin. Compositions of Formula (II-A) for use in these methods are also provided. 

Substituted inhibitors of menin-MLL and methods of use

The present disclosure provides compounds of Formula (I-A) for inhibiting the interaction of menin with MLL1, MLL2 and MLL-fusion oncoproteins. The compounds are useful for the treatment of leukemia, solid cancers, diabetes and other diseases dependent on activity of MLL1, MLL2, MLL fusion proteins, and/or menin. 

Bridged bicyclic inhibitors of menin-MLL and methods of use

The present disclosure provides compositions and methods of use to inhibit the interaction of menin with MLL1, MLL2 and MLL-fusion oncoproteins. The compositions and methods of use are useful for the treatment of leukemia, solid cancers, diabetes and other diseases dependent on activity of MLL1, MLL2, MLL fusion proteins, and/or menin.

Methods and compositions for inhibiting the interaction of menin with MLL proteins

Growing community of inventors

Ann Arbor, MI, United States of America

Tomasz Cierpicki