Using a Function-First “Scout Fragment”-Based Approach to Develop Allosteric Covalent Inhibitors of Conformationally Dynamic Helicase Mechanoenzymes-Reference-Cited by-同舟云学术

Using a Function-First “Scout Fragment”-Based Approach to Develop Allosteric Covalent Inhibitors of Conformationally Dynamic Helicase Mechanoenzymes

Published:2023-12-22 Issue:1 Volume:146 Page:62-67
ISSN:0002-7863
Container-title:Journal of the American Chemical Society
language:en
Short-container-title:J. Am. Chem. Soc.

Author:

Ramsey Jared R.¹²^ORCID,Shelton Patrick M. M.²,Heiss Tyler K.²,Olinares Paul Dominic B.³,Vostal Lauren E.¹²^ORCID,Soileau Heather¹²^ORCID,Grasso Michael²,Casebeer Sara W.²,Adaniya Stephanie⁴,Miller Michael⁵,Sun Shan⁵,Huggins David J.⁵⁶,Myers Robert W.⁵^ORCID,Chait Brian T.³,Vinogradova Ekaterina V.¹⁴,Kapoor Tarun M.¹²^ORCID

Affiliation:

1. Tri-Institutional PhD Program in Chemical Biology, New York, New York 10021, United States

2. Laboratory of Chemistry and Cell Biology, The Rockefeller University, New York, New York 10065, United States

3. Laboratory of Mass Spectrometry and Gaseous Ion Chemistry, The Rockefeller University, New York, New York 10065, United States

4. Laboratory of Chemical Immunology and Proteomics, The Rockefeller University, New York, New York 10065, United States

5. Sanders Tri-Institutional Therapeutics Discovery Institute, New York, New York 10065, United States

6. Department of Physiology and Biophysics, Weill Cornell Medicine, New York, New York 10021, United States

Funder

Takeda Pharmaceutical Company

Achelis and Bodman Foundation

Stavros Niarchos Foundation

Rockefeller University

National Institute of General Medical Sciences

Robertson Foundation

Publisher

American Chemical Society (ACS)

Subject

Colloid and Surface Chemistry,Biochemistry,General Chemistry,Catalysis

Link

https://pubs.acs.org/doi/pdf/10.1021/jacs.3c10581

Reference43 articles.

1. Discovering New Medicines Targeting Helicases

2. Viral and cellular RNA helicases as antiviral targets

3. Translocation and Unwinding Mechanisms of RNA and DNA Helicases

4. Three conformational snapshots of the hepatitis C virus NS3 helicase reveal a ratchet translocation mechanism

5. Selective inhibitors of SARM1 targeting an allosteric cysteine in the autoregulatory ARM domain

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