The backbone constitution drives passive permeability independent of side chains in depsipeptide and peptide macrocycles inspired by <i>ent</i>-verticilide-Reference-Cited by-同舟云学术

The backbone constitution drives passive permeability independent of side chains in depsipeptide and peptide macrocycles inspired by ent-verticilide

Published:2024 Issue: Volume: Page:
ISSN:2041-6520
Container-title:Chemical Science
language:en
Short-container-title:Chem. Sci.

Author:

Thorpe Madelaine P.¹^ORCID,Smith Abigail N.¹^ORCID,Blackwell Daniel J.²^ORCID,Hopkins Corey R.³^ORCID,Knollmann Bjorn C.²^ORCID,Akers Wendell S.⁴,Johnston Jeffrey N.¹^ORCID

Affiliation:

1. Department of Chemistry, Vanderbilt Institute of Chemical Biology, Vanderbilt University, Nashville, TN 37235-1822, USA

2. Department of Medicine, Vanderbilt Center for Arrhythmia Research and Therapeutics (VanCART), Vanderbilt University Medical Center, Medical Research Bldg IV, Room 1265, 2215B Garland Ave, Nashville, TN 37232-0575, USA

3. Department of Pharmaceutical Sciences, College of Pharmacy, University of Nebraska Medical Center, Omaha, NE 68198, USA

4. Pharmaceutical Sciences Research Center, College of Pharmacy, Lipscomb University, Nashville, TN 37204, USA

Abstract

The number of peptide-like scaffolds found in late-stage drug development is increasing, but a critical unanswered question in the field is whether substituents (side chains) or the backbone drive passive permeability.

Funder

National Heart, Lung, and Blood Institute

Pharmaceutical Research and Manufacturers of America Foundation

National Institutes of Health

Publisher

Royal Society of Chemistry (RSC)

Link

http://pubs.rsc.org/en/content/articlepdf/2024/SC/D4SC02758B

Reference45 articles.

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4. Macrocyclic Drugs and Clinical Candidates: What Can Medicinal Chemists Learn from Their Properties?

5. Beyond 20 in the 21st Century: Prospects and Challenges of Non-canonical Amino Acids in Peptide Drug Discovery