Mechanistic elucidation guided by covalent inhibitors for the development of anti-diabetic PPARγ ligands-Reference-Cited by-同舟云学术

Mechanistic elucidation guided by covalent inhibitors for the development of anti-diabetic PPARγ ligands

Published:2016 Issue:8 Volume:7 Page:5523-5529
ISSN:2041-6520
Container-title:Chemical Science
language:en
Short-container-title:Chem. Sci.

Author:

Bae Hwan¹²³⁴,Jang Jun Young¹²³⁴,Choi Sun-Sil⁵⁶⁷⁴,Lee Jae-Jin⁸⁹¹⁰⁴,Kim Heejun¹²³⁴,Jo Ala¹²³⁴,Lee Kong-Joo⁸⁹¹⁰⁴,Choi Jang Hyun⁵⁶⁷⁴,Suh Se Won¹²³⁴¹¹,Park Seung Bum¹²³⁴¹¹^ORCID

Affiliation:

1. Department of Chemistry

2. Seoul National University

3. Seoul 151-747

4. Korea

5. Department of Biological Science

6. Ulsan National Institute of Science and Technology

7. Ulsan 689-798

8. Graduate School of Pharmaceutical Sciences and College of Pharmacy

9. Ewha Womans University

10. Seoul 120-750

11. Department of Biophysics and Chemical Biology

Abstract

We revealed the X-ray structure of PPARγ co-crystallized with SR1664 bound to the alternate binding site of PPARγ and confirmed that this blocks the phosphorylation of Ser273.

Funder

National Research Foundation of Korea

Publisher

Royal Society of Chemistry (RSC)

Subject

General Chemistry

Link

http://pubs.rsc.org/en/content/articlepdf/2016/SC/C6SC01279E

Reference24 articles.

1. Insulin signalling and the regulation of glucose and lipid metabolism

2. An Antidiabetic Thiazolidinedione Is a High Affinity Ligand for Peroxisome Proliferator-activated Receptor γ (PPARγ)

3. The Many Faces of PPARγ