Results 71 to 80 of about 26,717 (273)

Identification of highly selective type II kinase inhibitors with chiral peptidomimetic tails

open access: yesJournal 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

A Study of Archiving Strategies in Multi-Objective PSO for Molecular Docking [PDF]

open access: yes, 2016
Molecular docking is a complex optimization problem aimed at predicting the position of a ligand molecule in the active site of a receptor with the lowest binding energy. This problem can be formulated as a bi-objective optimization problem by minimizing
A Sandoval-Perez   +15 more
core   +1 more source

Evaluating Cytocompatibility of Corynebacterium glutamicum‐poly Vinyl Alcohol Living Biomaterials for Ocular Use

open access: yesAdvanced Healthcare Materials, EarlyView.
In ophthalmology, living biomaterials such as living contact lenses appear promising for sustained drug delivery or biosensing. The cytocompatibility of Cg‐PVA hydrogels, developed as a model living contact lens, is investigated with the ocular surface, showing their potential translation to the clinic.
Krupansh Desai   +6 more
wiley   +1 more source

Isolation of bis(copper) key intermediates in Cu-catalyzed azide-alkyne "click reaction". [PDF]

open access: yes, 2015
The copper-catalyzed 1,3-dipolar cycloaddition of an azide to a terminal alkyne (CuAAC) is one of the most popular chemical transformations, with applications ranging from material to life sciences.
Bertrand, Guy   +3 more
core   +2 more sources

Peptidomimetic blockade of MYB in acute myeloid leukemia

open access: yesNature Communications, 2017
Aberrant gene expression is a hallmark of acute leukemias. MYB-driven transcriptional coactivation with CREB-binding protein (CBP)/P300 is required for acute lymphoblastic and myeloid leukemias, including refractory MLL-rearranged leukemias.
Kavitha Ramaswamy   +12 more
semanticscholar   +1 more source

Peptomer Linkers Enable Kinetic Control over Co‐Delivery of Multiple Chemotherapeutics

open access: yesAdvanced Healthcare Materials, EarlyView.
A key challenge in combinatorial chemotherapeutic drug delivery is independent control over release kinetics, especially with drugs of similar size and structure. Here, peptoid substitutions to proteolytically degradable peptides enabled the design of fast and slow‐releasing drug linkers.
Carolyn M. Watkins   +3 more
wiley   +1 more source

A cyclic carbo-isosteric penta-depsipeptide: cyclo(Phe1–d-Ala2–Gly3–Phe4–APO5)

open access: yesActa 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

Connexin communication compartments and wound repair in epithelial tissue [PDF]

open access: yes, 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

Structure‐Based Development of Ultra‐Broad‐Spectrum 3C‐Like Protease Inhibitors

open access: yesAdvanced Science, EarlyView.
This study provides an in‐depth analysis of the substrate binding pocket of 3CLpros across all coronavirus species using bioinformatics and structural insights, revealing the critical impact of S2/S4 subsite diversity on the broad‐spectrum activity of approved therapeutics.
Haixia Su   +15 more
wiley   +1 more source

ASTX660, a Novel Non-peptidomimetic Antagonist of cIAP1/2 and XIAP, Potently Induces TNFα-Dependent Apoptosis in Cancer Cell Lines and Inhibits Tumor Growth

open access: yesMolecular Cancer Therapeutics, 2018
Because of their roles in the evasion of apoptosis, inhibitor of apoptosis proteins (IAP) are considered attractive targets for anticancer therapy. Antagonists of these proteins have the potential to switch prosurvival signaling pathways in cancer cells ...
G. Ward   +13 more
semanticscholar   +1 more source

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