An allosteric site on MKP5 reveals a strategy for small-molecule inhibition-Reference-Cited by-同舟云学术

An allosteric site on MKP5 reveals a strategy for small-molecule inhibition

Published:2020-08-25 Issue:646 Volume:13 Page:
ISSN:1945-0877
Container-title:Science Signaling
language:en
Short-container-title:Sci. Signal.

Author:

Gannam Zachary T. K.¹^ORCID,Min Kisuk¹^ORCID,Shillingford Shanelle R.¹²^ORCID,Zhang Lei¹,Herrington James³,Abriola Laura³^ORCID,Gareiss Peter C.³,Pantouris Georgios¹,Tzouvelekis Argyrios⁴,Kaminski Naftali⁵^ORCID,Zhang Xinbo⁶,Yu Jun⁷^ORCID,Jamali Haya²^ORCID,Ellman Jonathan A.²^ORCID,Lolis Elias¹^ORCID,Anderson Karen S.¹⁸^ORCID,Bennett Anton M.¹⁹^ORCID

Affiliation:

1. Department of Pharmacology, Yale University School of Medicine, New Haven, CT 06520, USA.

2. Department of Chemistry, Yale University, New Haven, CT 06511, USA.

3. Yale Center for Molecular Discovery, Yale West Campus, West Haven, CT 06516, USA.

4. “Alexander Fleming” Biomedical Sciences Research Center, 16672 Vari, Greece.

5. Section of Pulmonary, Critical Care and Sleep Medicine, Department of Internal Medicine, Yale University School of Medicine, New Haven, CT 06520, USA.

6. Department of Medicine, Temple University Lewis Katz School of Medicine, Philadelphia, PA 19140, USA.

7. Center for Metabolic Disease Research and Department of Physiology, Temple University Lewis Katz School of Medicine, Philadelphia, PA 19140, USA.

8. Department of Molecular Biophysics and Biochemistry, New Haven, CT 06520, USA.

9. Program in Integrative Cell Signaling and Neurobiology of Metabolism, Department of Comparative Medicine, Yale University School of Medicine, New Haven, CT 06520, USA.

Abstract

A small-molecule inhibitor of the phosphatase MKP5 identifies an allosteric site that enables specific targeting.

Funder

National Institute of General Medical Sciences

National Institute of Allergy and Infectious Diseases

National Institute of Arthritis and Musculoskeletal and Skin Diseases

Blavatnik Innovations Award

Program in Innovative Therapeutics for Connecticut’s Health

Publisher

American Association for the Advancement of Science (AAAS)

Subject

Cell Biology,Molecular Biology,Biochemistry