Deacylcortivazol-like pyrazole regioisomers reveal a more accommodating expanded binding pocket for the glucocorticoid receptor-Reference-Cited by-同舟云学术

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Deacylcortivazol-like pyrazole regioisomers reveal a more accommodating expanded binding pocket for the glucocorticoid receptor

Published:2021 Issue:2 Volume:12 Page:203-212
ISSN:2632-8682
Container-title:RSC Medicinal Chemistry
language:en
Short-container-title:RSC Med. Chem.

Author:

Zimmerman Jessica A. O.¹²³⁴⁵^ORCID,Fang Mimi¹²³⁴⁵,Doumbia Bintou⁶⁷⁸⁵,Neyman Alexis⁶⁷⁸⁵,Cha Ji Hyeon⁶⁷⁸⁵,Thomas Michael⁶⁷⁸⁵,Hall Bonnie⁹¹⁰⁵,Wu Meng¹²³⁴⁵^ORCID,Wilson Anne M.⁶⁷⁸⁵^ORCID,Pufall Miles A.¹²³⁴⁵^ORCID

Affiliation:

1. Department of Biochemistry

2. Carver College of Medicine

3. University of Iowa

4. Iowa City

5. USA

6. Department of Chemistry

7. Butler University

8. Indianapolis

9. Grand View University

10. Des Moines

Abstract

Ullmann-like synthesis of deacylcortivazol-like regioisomers reveals a broader than expected structure activity relationship for novel glucocorticoids.

Funder

National Science Foundation

National Institutes of Health

National Cancer Institute

Publisher

Royal Society of Chemistry (RSC)

Subject

Organic Chemistry,Drug Discovery,Pharmaceutical Science,Pharmacology,Molecular Medicine,Biochemistry

Link

http://pubs.rsc.org/en/content/articlepdf/2021/MD/D0MD00278J

Reference23 articles.

1. Corticosteroids

2. Regulatory Actions of Glucocorticoid Hormones: From Organisms to Mechanisms

3. Molecular Biology of Glucocorticoid Signaling

4. Dynamic regulation of glucocorticoid signalling in health and disease

5. Structures and mechanism for the design of highly potent glucocorticoids

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1. Identification of global inhibitors of cellular glycosylation;Nature Communications;2023-02-20

2. Cortisol Based Glucocorticoids;SpringerBriefs in Molecular Science;2023

3. Stereoisomers of an Aryl Pyrazole Glucocorticoid Receptor Agonist Scaffold Elicit Differing Anti-inflammatory Responses;ACS Medicinal Chemistry Letters;2022-08-22

4. Potent Anti-Inflammatory, Arylpyrazole-Based Glucocorticoid Receptor Agonists That Do Not Impair Insulin Secretion;ACS Medicinal Chemistry Letters;2021-09-15

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