Thiol-to-amine cyclization reaction enables screening of large libraries of macrocyclic compounds and the generation of sub-kilodalton ligands-Reference-Cited by-同舟云学术

Thiol-to-amine cyclization reaction enables screening of large libraries of macrocyclic compounds and the generation of sub-kilodalton ligands

Published:2019-08-02 Issue:8 Volume:5 Page:
ISSN:2375-2548
Container-title:Science Advances
language:en
Short-container-title:Sci. Adv.

Author:

Kale S. S.¹^ORCID,Bergeron-Brlek M.¹^ORCID,Wu Y.¹^ORCID,Kumar M. G.¹^ORCID,Pham M. V.¹,Bortoli J.²^ORCID,Vesin J.²^ORCID,Kong X.-D.¹^ORCID,Machado J. Franco¹^ORCID,Deyle K.¹^ORCID,Gonschorek P.¹^ORCID,Turcatti G.²^ORCID,Cendron L.³^ORCID,Angelini A.⁴⁵^ORCID,Heinis C.¹^ORCID

Affiliation:

1. Institute of Chemical Sciences and Engineering, Ecole Polytechnique Fédérale de Lausanne (EPFL), CH-1015 Lausanne, Switzerland.

2. Biomolecular Screening Facility, Ecole Polytechnique Fédérale de Lausanne (EPFL), Lausanne, Switzerland.

3. Department of Biology, University of Padova, 35131 Padova, Italy.

4. Department of Molecular Sciences and Nanosystems, Ca’ Foscari University of Venice, Via Torino 155, Venezia Mestre, Venice 30172, Italy.

5. European Centre for Living Technologies (ECLT), Ca’ Bottacin, Dorsoduro 3911, Calle Crosera, Venice 30124, Italy.

Abstract

An efficient cyclization reaction allows for screening of large macrocycle libraries and yields a potent thrombin inhibitor.

Funder

Swiss National Science Foundation

Publisher

American Association for the Advancement of Science (AAAS)

Subject

Multidisciplinary

Reference16 articles.

1. The exploration of macrocycles for drug discovery — An underexploited structural class;Driggers E. M.;Nat. Rev. Drug Discov.,2008

2. Macrocyclic drugs and clinical candidates: What can medicinal chemists learn from their properties?;Giordanetto F.;J. Med. Chem.,2013

3. How proteins bind macrocycles;Villar E. A.;Nat. Chem. Biol.,2014

4. Protein epitope mimetic macrocycles as biopharmaceuticals;Luther A.;Curr. Opin. Chem. Biol.,2017

5. Phage selection of cyclic peptides for application in research and drug development;Deyle K.;Acc. Chem. Res.,2017

Cited by 33 articles. 订阅此论文施引文献订阅此论文施引文献，注册后可以免费订阅5篇论文的施引文献，订阅后可以查看论文全部施引文献

1. Large Libraries of Structurally Diverse Macrocycles Suitable for Membrane Permeation;Angewandte Chemie International Edition;2024-05-24

2. Large Libraries of Structurally Diverse Macrocycles Suitable for Membrane Permeation;Angewandte Chemie;2024-05-24

3. Synthesis of potassium-incorporated caged-ladder-like polyhedral oligomeric silsesquioxane hybrid macromolecules for unique thermal intumescent properties and thermal decomposition studies;European Polymer Journal;2024-05

4. Solid‐phase peptide synthesis in 384‐well plates;Journal of Peptide Science;2024-01-14

5. A facile strategy for the construction of a phage display cyclic peptide library for the selection of functional macrocycles;Chemical Science;2024