Results 61 to 70 of about 16,050 (209)

Nano‐Gs Protein Peptidomimetics: Rational Design of Gα C‐Terminus‐Derived Peptides Mimicking Key Components of Gs‐β2AR Interactions

open access: yesAngewandte Chemie International Edition, EarlyView.
G protein‐coupled receptors (GPCRs) are major therapeutic targets. Modulating GPCR activity through intracellular sites is evolving. A structure‐ and computation‐assisted approach generated small G protein‐derived peptidomimetics targeting the intracellular binding crevice of the β2 adrenergic receptor mimicking features of the full G protein.
Phuong Thu Tran   +11 more
wiley   +1 more source

Synthesis of acylhydrazino-peptomers, a new class of peptidomimetics, by consecutive Ugi and hydrazino-Ugi reactions

open access: yesBeilstein Journal of Organic Chemistry, 2016
Herein we describe a versatile approach for the synthesis of acylhydrazino-peptomers, a new class of peptidomimetics. The key idea in this approach is based on a simple route using a one-pot hydrazino-Ugi four-component reaction followed by a ...
Angélica de Fátima S. Barreto   +2 more
doaj   +1 more source

Synthesis and antimicrobial activity against Pseudomonas aeruginosa of macrocyclic β-hairpin peptidomimetic antibiotics containing N-methylated amino acids [PDF]

open access: yes, 2016
Antimicrobial resistance among Gram-negative bacteria is a growing problem, fueled by the paucity of new antibiotics that target these microorganisms. One novel family of macrocyclic β-hairpin-shaped peptidomimetics was recently shown to act specifically
Moehle, Kerstin   +2 more
core   +1 more source

Pd(II)‐Catalyzed Strategies for the β‐Arylation of α‐Amino Acids: An Overview

open access: yesChemistry – A European Journal, EarlyView.
The graphical abstract summarizes the review “Pd(II)‐Catalyzed Strategies for the β‐Arylation of α‐Amino Acids: An Overview”, highlighting representative Pd(II)‐catalyzed methods for the β‐arylation of α‐amino acids. Key mechanistic features, substrate diversity, and synthetic relevance of these transformations are showcased. Abstract Metal‐catalyzed C─
Davide Illuminati   +4 more
wiley   +1 more source

C-Terminal Extended Hexapeptides as Potent Inhibitors of the NS2B-NS3 Protease of the ZIKA Virus

open access: yesFrontiers in Medicine, 2022
The Zika virus (ZIKV) protease is an attractive drug target for the design of novel inhibitors to control the ZIKV infection. As the protease substrate-binding site contains acidic residues, inhibitors with basic residues can be beneficial for the ...
Suyash Pant, Nihar R. Jena
doaj   +1 more source

Selective and potent proteomimetic inhibitors of intracellular protein–protein interactions [PDF]

open access: yes, 2015
Inhibition of protein–protein interactions (PPIs) represents a major challenge in chemical biology and drug discovery. α-Helix mediated PPIs may be amenable to modulation using generic chemotypes, termed “proteomimetics”, which can be assembled in a ...
Azzarito   +51 more
core   +4 more sources

Phosphorescent Iridium Hydrazinonicotinic Acid (HYNIC) Complexes That Bind to Prostate Specific Membrane Antigen: Potential Photodynamic Therapy of Prostate Cancer

open access: yesChemistry – A European Journal, EarlyView.
A phosphorescent iridium(III) complex has been prepared with a 6‐hydrazinonicotinic acid (HYNIC) ligand tethered to a lysine‐ureido‐glutamatic acid pharmacophore, which binds to an enzyme, called prostate‐specific membrane antigen (PSMA), which is overexpressed in prostate cancer.
La'El Kimchi   +6 more
wiley   +1 more source

Recent Advances in Amphipathic Peptidomimetics as Antimicrobial Agents to Combat Drug Resistance

open access: yesMolecules
The development of antimicrobial drugs with novel structures and clear mechanisms of action that are active against drug-resistant bacteria has become an urgent need of safeguarding human health due to the rise of bacterial drug resistance. The discovery
Ma Su, Yongxiang Su
doaj   +1 more source

Advances in Development of Antimicrobial Peptidomimetics as Potential Drugs

open access: yesMolecules, 2017
The rapid emergence of multidrug-resistant pathogens has evolved into a global health problem as current treatment options are failing for infections caused by pan-resistant bacteria.
Natalia Molchanova   +2 more
doaj   +1 more source

Non-Conventional Peptide Self-Assembly into a Conductive Supramolecular Rope

open access: yesNanomaterials, 2023
Structures composed of alternating α and β amino acids can give rise to peculiar secondary structural motifs, which could self-assemble into complex structures of controlled geometries.
Nicola Forlano   +7 more
doaj   +1 more source

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