Kamal R. Abdul Azeez

TL;DR: A thorough characterization of the Published Kinase Inhibitor Set is provided and chemical starting points for designing new chemical probes of orphan kinases are identified and the utility of these leads are illustrated by developing a selective inhibitor for the previously untargeted kinases LOK and SLK.

TL;DR: This work shows that salt-inducible kinase 2 (SIK2) is overexpressed in adipocyte-rich metastatic deposits compared with ovarian primary lesions, and identifies SIK2 at the apex of the adipocytes-induced signaling cascades in cancer cells and makes a compelling case for targeting Sik2 for therapy in ovarian cancer.

TL;DR: The first high-resolution structures of kinases AAK1 and BIKE in complex with two drug candidates are reported, allowing a comprehensive structural characterization of the NAK kinase family and provide the basis for rational design of selective NAK inhibitors.

TL;DR: Terpyridines have been developed as α-helix mimetics for the inhibition of such interactions and are the first biologically active, nonpeptidic compounds that block the AKAP binding site of PKA.

TL;DR: The RhoGEF (Rho GTPase guanine-nucleotide-exchange factor) domain of AKAP-Lbc, also known as AKAP13, catalyses nucleotide exchange on RhoA and is involved in the development of cardiac hypertrophy and cancer.