Enzymatic Synthesis Assisted Discovery of Proline‐Rich Macrocyclic Peptides in Marine Sponges
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DOI: 10.1002/cbic.202100275
Abstract: Proline‐rich macrocyclic peptides (PRMPs) are natural products present in geographically and phylogenetically dispersed marine sponges. The large diversity and low abundance of PRMPs in sponge metabolomes precludes isolation and structure elucidation of each individual PRMP… read more here.
Keywords: enzymatic synthesis; macrocyclic peptides; marine sponges; rich macrocyclic ... See more keywords
Bacterially Secretable Single‐Chain Tandem Macrocyclic Peptides for High Affinity and Inhibitory Activity
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DOI: 10.1002/cbic.202200599
Abstract: The inhibition of protein‐protein interactions (PPIs) is an effective approach for therapy. Owing to their large binding surface areas to target proteins, macrocyclic peptides are suitable molecules for PPI inhibition. In this study, we developed… read more here.
Keywords: chain tandem; macrocyclic peptides; inhibitory activity; single chain ... 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
Discovery of Functional Macrocyclic Peptides by Means of the RaPID System.
Sign Up to like & getrecommendations! Published in 2019 at "Methods in molecular biology"
DOI: 10.1007/978-1-4939-9504-2_14
Abstract: Flexizymes, highly flexible tRNA aminoacylation ribozymes, have enabled charging of virtually any amino acid (including non-proteogenic ones) onto tRNA molecules. Coupling to a custom-made in vitro translation system, namely the flexible in vitro translation (FIT)… read more here.
Keywords: rapid system; system; functional macrocyclic; macrocyclic peptides ... See more keywords
Designing Cell-Permeable Macrocyclic Peptides.
Sign Up to like & getrecommendations! Published in 2019 at "Methods in molecular biology"
DOI: 10.1007/978-1-4939-9504-2_3
Abstract: Peptides provide an attractive modality for targeting challenging drug targets such as intracellular protein-protein interactions. Unfortunately, peptides are generally impermeable to the cell membrane and inherently susceptible to proteolytic degradation in vivo. Macrocyclization of peptides… read more here.
Keywords: designing cell; cell permeable; macrocyclic peptides; cell penetrating ... See more keywords
Tiered analytics for purity assessment of macrocyclic peptides in drug discovery: Analytical consideration and method development
Sign Up to like & getrecommendations! Published in 2017 at "Journal of Pharmaceutical and Biomedical Analysis"
DOI: 10.1016/j.jpba.2017.01.056
Abstract: &NA; Synthetic macrocyclic peptides with natural and unnatural amino acids have gained considerable attention from a number of pharmaceutical/biopharmaceutical companies in recent years as a promising approach to drug discovery, particularly for targets involving protein–protein… read more here.
Keywords: tiered analytics; macrocyclic peptides; drug; drug discovery ... See more keywords
Accelerated Identification of Cell Active KRAS Inhibitory Macrocyclic Peptides using Mixture Libraries and Automated Ligand Identification System (ALIS) Technology
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Medicinal Chemistry"
DOI: 10.1021/acs.jmedchem.2c00154
Abstract: Macrocyclic peptides can disrupt previously intractable protein–protein interactions (PPIs) relevant to oncology targets such as KRAS. Early hits often lack cellular activity and require meticulous improvement of affinity, permeability, and metabolic stability to become viable… read more here.
Keywords: identification system; macrocyclic peptides; ligand identification; identification ... See more keywords
Design, Synthesis, and Optimization of Macrocyclic Peptides as Species-Selective Antimalaria Proteasome Inhibitors.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c00611
Abstract: With over 200 million cases and close to half a million deaths each year, malaria is a threat to global health, particularly in developing countries. Plasmodium falciparum, the parasite that causes the most severe form… read more here.
Keywords: design synthesis; macrocyclic peptides; species selective; proteasome inhibitors ... See more keywords
Peptide-to-Small Molecule: A Pharmacophore-Guided Small Molecule Lead Generation Strategy from High-Affinity Macrocyclic Peptides.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c00919
Abstract: Recent technological innovations have led to the development of methods for the rapid identification of high-affinity macrocyclic peptides for a wide range of targets; however, it is still challenging to achieve the desired activity and… read more here.
Keywords: small molecule; macrocyclic peptides; high affinity; molecule ... See more keywords
A Strategy to Select Macrocyclic Peptides Featuring Asymmetric Molecular Scaffolds as Cyclization Units by Phage Display
Sign Up to like & getrecommendations! Published in 2022 at "Journal of the American Chemical Society"
DOI: 10.1021/jacs.1c12822
Abstract: Macrocyclic peptides (MPs) have positioned themselves as a privileged class of compounds for the discovery of therapeutics and development of chemical probes. Aided by the development of powerful selection strategies, high-affinity binders against biomolecular targets… read more here.
Keywords: phage display; strategy; macrocyclic peptides; cyclization units ... See more keywords
Accessing Diverse Pyridine-Based Macrocyclic Peptides by a Two-Site Recognition Pathway
Sign Up to like & getrecommendations! Published in 2022 at "Journal of the American Chemical Society"
DOI: 10.1021/jacs.2c02824
Abstract: Macrocyclic peptides are sought-after molecular scaffolds for drug discovery, and new methods to access diverse libraries are of increasing interest. Here, we report the enzymatic synthesis of pyridine-based macrocyclic peptides (pyritides) from linear precursor peptides.… read more here.
Keywords: macrocyclic peptides; pyridine based; region; site ... See more keywords