Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human β-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor-Reference-Cited by-同舟云学术

Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human β-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor

Published:2020-01-31 Issue:6 Volume:63 Page:2986-3003
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

Kumar Kunal¹²,Wang Peng³,Wilson Jessica³,Zlatanic Viktor³,Berrouet Cecilia³,Khamrui Susmita²,Secor Cody²,Swartz Ethan A.³,Lazarus Michael¹²^ORCID,Sanchez Roberto¹²,Stewart Andrew F.³,Garcia-Ocana Adolfo³,DeVita Robert J.¹²^ORCID

Affiliation:

1. Drug Discovery Institute, Icahn School of Medicine at Mount Sinai, New York, New York 10029, United States

2. Department of Pharmacological Sciences, Icahn School of Medicine at Mount Sinai, New York, New York 10029, United States

3. Diabetes, Obesity, and Metabolism Institute, Icahn School of Medicine at Mount Sinai, New York, New York 10029, United States

Funder

National Institute of Diabetes and Digestive and Kidney Diseases

Juvenile Diabetes Research Foundation

National Institute of General Medical Sciences

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Link

https://pubs.acs.org/doi/pdf/10.1021/acs.jmedchem.9b01379

Reference86 articles.

1. The role of DYRK1A in neurodegenerative diseases

2. Recent Advances in the Design, Synthesis, and Biological Evaluation of Selective DYRK1A Inhibitors: A New Avenue for a Disease Modifying Treatment of Alzheimer’s?

3. DYRK1A Kinase Inhibitors with Emphasis on Cancer

4. DYRK1A: the double-edged kinase as a protagonist in cell growth and tumorigenesis

5. A high-throughput chemical screen reveals that harmine-mediated inhibition of DYRK1A increases human pancreatic beta cell replication

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