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Discovery, design and synthesis of a selective S1P(3) receptor allosteric agonist.
A combination of ligand competition, site-directed mutagenesis and molecular modeling studies showed that the N,N-dicyclohexyl-5-cyclopropylisoxazole-3-carboxamide is an allosteric agonist and binds to the S1P3-R in a manner that does not disrupt the S2P-R-S1P binding. Expand
Abstract C190: Potent and selective inhibition of CDK7 by novel covalent inhibitors
Novel and selective CDK7 covalent inhibitors from two series with desirable drug-like properties, which are being evauated for anti-tumor activity in xenograft models are identified. Expand
Abstract 3070: Potent and selective inhibition of CDK7 by novel covalent inhibitors
Background: Phosphorylation of the RNA polymerase II (RNAPII) in C-terminal domain (CTD) by Cyclin-dependent kinase 7 (CDK7) is an important step in cellular transcription process. HenceExpand
Figure 4, Dose-response curve for ML249
Abstract 2384: Preclinical evaluation of PD and efficacy of novel potent selective and orally bioavailable CDK12 covalent inhibitors in TNBC model
Very potent and highly selective CDK 12 inhibitors have been identified from two distinct chemical series and showed significant anti-proliferative activity in TNBC and other cancer cell lines, which correlated with inhibition of pS2 (RNAP II), a bonafide CDK12 substrate and target engagement. Expand
Abstract LB-317: Identification of a novel preclinical candidate for CDK7 inhibition
Cyclin-dependent kinase 7 (CDK7) is an important constituent of the cellular transcriptional machinery, where it phosphorylates the C-terminal domain (CTD) of RNAP polymerase II (RNAPII). BecauseExpand