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

