Work

Development of Narrow Spectrum ATP-competitive Kinase Inhibitors as Probes for BIKE and AAK1

Year: 2016

Type: preprint

Abstract: ABSTRACT Understanding the structural determinants of inhibitor selectivity would facilitate the design and preparation of kinase probes. We describe a pair of matched compounds differing only by one degree of saturation but showing dramatic differential activities at select kinases. We utilized x-ray crystallography and computational analysis to rationalize the basis of the differential activity.

Source: bioRxiv (Cold Spring Harbor Laboratory)

DOI: 10.1101/094631

Authors: Rafael M. Couñago, Alison D. Axtman, Stephen J. Capuzzi, Hátylas Azevedo, David H. Drewry, Jonathan M. Elkins, Opher Gileadi, Cristiano R. W. Guimarães, Alessandra Mascarello, Ricardo A. M. Serafim, Carrow I. Wells, Timothy M. Willson, William J. Zuercher

Institutions: Universidade Estadual de Campinas (UNICAMP), University of North Carolina at Chapel Hill, Aché (Brazil), University of Oxford

Language: English

Topic: Protein Kinase Regulation and GTPase Signaling

Subfield: Molecular Biology

Field: Biochemistry, Genetics and Molecular Biology

Domain: Life Sciences

Open Access status: green

OpenAlex ID: W2581498155

Cites: 41

Cited by: 1

Related to: 10