Results 61 to 70 of about 19,199 (236)
Identification of highly selective type II kinase inhibitors with chiral peptidomimetic tails
Journal of Enzyme Inhibition and Medicinal Chemistry, 2022 Identification of highly selective type II kinase inhibitors is described. Two different chiral peptidomimetic scaffolds were introduced on the tail region of non-selective type II kinase inhibitor GNF-7 to enhance the selectivity.
Seo-Jung Han +16 more
doaj +1 more source
Advanced Science, EarlyView.By leveraging this homodimerization mechanism, molecular glues were rationally designed to induce dysfunctional 3A dimerization, thereby restoring antiviral RNAi. The optimal molecular glue, VTP‐32, demonstrated potent and pan‐enterovirus (groups A, B, D) antiviral effects.
Yuan Fang +13 more
wiley +1 more source
Advanced Science, EarlyView.We introduce a new membrane‐active antifungal design, Gua‐SMACS‐16, that exhibits high potency and single‐species selectivity for C. tropicalis while sparing other close species in the Candida genus. Moreover, when combining with caspofungin, a clinical antifungal drug inhibiting 1,3‐β‐glucan synthase, they exhibit ultra‐strong synergy across a panel ...
Tianjiao Dai +8 more
wiley +1 more source
Directing mesenchymal stem cells to bone to augment bone formation and increase bone mass. [PDF]
, 2012 Aging reduces the number of mesenchymal stem cells (MSCs) that can differentiate into osteoblasts in the bone marrow, which leads to impairment of osteogenesis.
Guan, Min +11 more
core +1 more source
Cilengitide: an RGD pentapeptide ανβ3 and ανβ5 integrin inhibitor in development for glioblastoma and other malignancies [PDF]
, 2011 Cilengitide, a cyclicized arginine-glycine-aspartic acid-containing pentapeptide, potently blocks ανβ3 and ανβ5 integrin activation. Integrins are upregulated in many malignancies and mediate a wide variety of tumor-stroma interactions.
Nabors, L B +5 more
core +1 more source
A cyclic carbo-isosteric penta-depsipeptide: cyclo(Phe1–d-Ala2–Gly3–Phe4–APO5)
Acta Crystallographica Section E: Crystallographic Communications, 2015 The title compound, cyclo(Phe1–d-Ala2–Gly3–Phe4–APO5), C26H32N4O5, is the minor diastereoisomer of a cyclic penta-peptidomimetic analogue containing a novel 2-aminopropyl lactone (APO) motif, which displays the same number of atoms as the native amino ...
Stéphanie M. Guéret, Trixie Wagner
doaj +1 more source
Angewandte 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
Connexin communication compartments and wound repair in epithelial tissue [PDF]
, 2018 Epithelial tissues line the lumen of tracts and ducts connecting to the external environment. They are critical in forming an interface between the internal and external environment and, following assault from environmental factors and pathogens, they ...
Chanson, Marc +4 more
core +4 more sources
Pd(II)‐Catalyzed Strategies for the β‐Arylation of α‐Amino Acids: An Overview
Chemistry – 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
A New Multi-Objective Approach for Molecular Docking Based on RMSD and Binding Energy [PDF]
, 2016 Ligand-protein docking is an optimization problem based on predicting the position of a ligand with the lowest binding energy in the active site of the receptor.
Aldana-Montes, Jose Francisco +4 more
core +1 more source