Memorial Sloan Kettering Cancer Center

Rutgers, the State University of New Jersey

The Rockefeller University

University of Bonn

University of Copenhagen

Dinshaw J Patel

Thomas Tuschl

Gunther Hartmann

Roger A Jones

Manuel Ascano, Jr

Winfried Barchet

Thomas Zillinger

Pu Gao

Barbara L Gaffney

Yang Wu

Yizhou Liu

Toshihiro Imaeda

Liang Deng

Yasutomi Asano

Weiyi Wang

Taku Kamei

Jumpei Aida

Rei Okamoto

Mayako Michino

Takanobu Kuroita

J Fraser Glickman

Michael Miller

Anja Groth

Giulia Saredi

Shogo Hashizume

Hongda Huang

Colin Hammond

Lodoe Lama

Daisuke Tomita

Roger Jones

JFraser Glickman

Taku Kamel

1-(3,4-Dihydro-1H-pyrido[4, 3-b]indol-2(5H)-yl)-2-hydroxyethanones are disclosed. The compounds are inhibitors of human cGAS in interferon-producing cell types. They are thus useful as therapeutic agents for treating cGAS-related autoimmune diseases in humans.

Substituted pyrido[4,3-b]indoles and azepino[4,5-b]indoles as inhibitors of cGAS

The present disclosure provides, among other things, compounds comprising cyclic dinucleotides containing a 2',5' linkage useful in the design of research tools, as research tools, and as therapeutic modalities such as enzyme modulators.

Compositions and methods for altering second messenger signaling

The present invention relates to small molecules interfering with the conformational space of the TONSL ARD occupied by the histone H4 tail. These small molecules targets the binding pocket of TONSL encompassing the H4 residues K12-R23 and act by preventing or disrupting the binding of the H4 tail K12-R23 with the TONSL ARD via direct competition or via allosteric disruption of the binding pocket.

Small molecules blocking histone reader domains

The invention relates to compositions, methods, kits, and assays related to the use and/or exploitation of isomers of cGAMP as well as the structure of the enzyme cGAS.

The present invention provides STING crystals. The present invention also provides STING modulators that interact with sites present in and/or defined by such crystals. The present invention also provides methods of making and using such crystals and modulators. Other aspects and/or features of the present invention will be apparent to those skilled in the art, reading the present specification.

STING crystals and modulators

The present disclosure provides, among other things, novel cyclic-GMP-AMP (cGAMP) analogs, mimics, mimetics and variants, and compositions and kits thereof; methods of using the compounds as described herein for treating cancer, and immune disease, disorders, or conditions; methods of using the compounds as described herein for modulating cGAS and STING; and methods of designing or characterizing a cGAS modulator.

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Dobbs Ferry, NY, United States of America

Dinshaw J Patel