Rigid Peptide Macrocycles from On‐Resin Glaser Stapling
Sign Up to like & getrecommendations! Published in 2018 at "ChemBioChem"
DOI: 10.1002/cbic.201800121
Abstract: Peptide macrocycles are widely utilized in the development of high affinity ligands, including stapled α‐helices. The linear rigidity of a 1,3‐diynyl linkage provides an optimal distance (7 Å) between β‐carbons of the i,i+4 amino acid side… read more here.
Keywords: peptide; peptide macrocycles; macrocycles resin; resin glaser ... See more keywords
Helical Stabilization of Peptide Macrocycles by Stapled Architectures.
Sign Up to like & getrecommendations! Published in 2022 at "Methods in molecular biology"
DOI: 10.1007/978-1-0716-1689-5_21
Abstract: Over the past two decades, significant efforts have invested in the development of strategies for the stabilization of macrocyclic peptides with α-helix structure by stapling their architectures. These strategies can be divided into two categories:… read more here.
Keywords: macrocyclic peptides; peptide macrocycles; helical stabilization; macrocycles stapled ... See more keywords
Shape linear peptides into rigid rings: a sp3 C–H arylation approach to cyclophane-braced peptide macrocycles
Sign Up to like & getrecommendations! Published in 2018 at "Science China Chemistry"
DOI: 10.1007/s11426-018-9288-2
Abstract: Peptide-based therapeutics have attracted increasing attention due to their unique properties in comparison to small molecule drugs and recombinant biologics [1]. With moderate size and suitable surface area, peptides possess enormous potential in drug discovery… read more here.
Keywords: cyclophane braced; peptide macrocycles; braced peptide; arylation ... See more keywords
Development of a Platform To Enable Efficient Permeability Evaluation of Novel Organo-Peptide Macrocycles.
Sign Up to like & getrecommendations! Published in 2019 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.9b00036
Abstract: As more macrocycle structures are utilized to drug intracellular targets, new platforms are needed to facilitate the discovery of cell permeable compounds in this unique chemical space. Herein, a method is disclosed that allows for… read more here.
Keywords: permeability evaluation; novel organo; organo peptide; evaluation novel ... See more keywords
Increasing the bioactive space of peptide macrocycles by thioamide substitution† †Electronic supplementary information (ESI) available. See DOI: 10.1039/c7sc04671e
Sign Up to like & getrecommendations! Published in 2018 at "Chemical Science"
DOI: 10.1039/c7sc04671e
Abstract: Thioamide substitution into macrocyclic peptides increases the conformational rigidity of the backbone resulting in enhanced biological activity and metabolic stability. read more here.
Keywords: space peptide; peptide macrocycles; bioactive space; thioamide substitution ... See more keywords
Streamlined construction of peptide macrocycles via palladium-catalyzed intramolecular S-arylation in solution and on DNA†
Sign Up to like & getrecommendations! Published in 2021 at "Chemical Science"
DOI: 10.1039/d1sc00789k
Abstract: A highly efficient and versatile method for construction of peptide macrocycles via palladium-catalyzed intramolecular S-arylation of alkyl and aryl thiols with aryl iodides under mild conditions is developed. The method exhibits a broad substrate scope… read more here.
Keywords: macrocycles via; construction peptide; palladium catalyzed; catalyzed intramolecular ... See more keywords