Abstract: 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.

Abstract: Tri-cyclyl nitrogen-containing heterocyclic compounds 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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. The present inventors have identified and solved the structure of a histone reader domain of TONSL termed the ARD (ankyrin repeat domain).

Abstract: 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.

Abstract: 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.

Abstract: Provided is a computer model generated from a data array, computer readable storage media encoded with the model, and computers comprising the model, wherein the model is derived from atomic structure coordinates of a FMN riboswitch or a lysine riboswitch. Further provided is a pharmacophore having a spatial arrangement of atoms defined by the binding pocket identified in the model, along with a compound defined by the pharmacophore. Also further provided are methods for rational drug design based on the atomic structure data, and compounds identified by the rational drug design process.

Abstract: TAN containing oils, e.g., crudes, are treated by flashing to remove substantially all of the water therefrom, thermally treating the recovered liquid to reduce the naphthenic acid content thereof, and re-combining light gases recovered from the flashing step with the treated liquid.