Results 101 to 110 of about 19,199 (236)

Preparation and Use of a General Solid-Phase Intermediate to Biomimetic Scaffolds and Peptide Condensations [PDF]

open access: yes, 2018
The Distributed Drug Discovery (D3) program develops simple, powerful, and reproducible procedures to enable the distributed synthesis of large numbers of potential drugs for neglected diseases.
Martynow, Jacek G.   +3 more
core   +2 more sources

ADAM17 and its proteolytic targets in disease pathogenesis

open access: yesThe FEBS Journal, EarlyView.
ADAM17 as a multifunctional sheddase with contrasting roles across inflammatory, metabolic, cardiovascular, and neoplastic diseases. Through regulated activation by iRhom, iTAP/FRMD8, and tetraspanins, ADAM17 cleaves diverse membrane ligands and receptors, thereby promoting inflammation, fibrosis, obesity, insulin resistance, and tumor progression ...
Abdulbasit Amin, Marina Badenes
wiley   +1 more source

TREM‐1 Blockade Inhibits Inflammasome Activation and Pyroptosis: Novel Insights on the Role of TREM‐1 and Syk in Monosodium Urate Crystal‐Induced Inflammation

open access: yesImmunology, Volume 178, Issue 2, Page 249-260, June 2026.
Schematic overview of the roles triggering receptor expressed on myeloid cells‐1 (TREM‐1) plays in monosodium urate (MSU) crystal‐induced inflammasome activation and IL‐1β secretion in gout arthritis. The present study provides novel data suggesting that blockade of TREM‐1 by LP17 attenuates MSU‐crystal‐induced inflammation through inhibition of ...
Yair Molad   +2 more
wiley   +1 more source

Stereochemical Behavior of Pyrrolo-Pyrazole Peptidomimetics Promoting Phase-Selective Supramolecular Organogels

open access: yesGels
Supramolecular gels were developed by taking advantage of an assembly of small dipeptides containing pyrrolo-pyrazole scaffolds. The dipeptides were prepared through a robust and ecofriendly synthetic approach from the commercially available starting ...
Enrica Chiesa   +6 more
doaj   +1 more source

Inhibitors Targeting SARS‐CoV‐2 Papain‐Like Protease: Screening, Design, Synthesis, and Biological Evaluation

open access: yesChemMedChem, Volume 21, Issue 9, 14 May 2026.
In our study, we obtained both non‐covalent and covalent PLpro inhibitors. Additionally, the stable protein‐ligand interactions of the active compound were examined using advanced computational docking and molecular dynamics simulations. The non‐covalent inhibitor 2t showed antiviral activity with an EC50 of 2.89 µM, indicating its potential as a ...
Elena‐Oriana Iuga   +11 more
wiley   +1 more source

Fighting the global pest problem: Preface to the special Toxicon issue on insecticidal toxins and their potential for insect pest control [PDF]

open access: yes, 2007
Arthropod pests are responsible for major crop devastation and are vectors for the transmission of new and re-emerging diseases in humans and livestock.
Nicholson, GM
core   +1 more source

Cyclic Peptide Conformational Landscapes Through the Lens of Mass Spectrometry and Orthogonal Spectroscopy

open access: yesJournal of Mass Spectrometry, Volume 61, Issue 5, May 2026.
ABSTRACT Cyclic peptides occupy a structurally dynamic region of chemical space, where function often arises from ensembles rather than a single dominant fold. Closed backbones, frequent N‐methylation, heteroatoms, unnatural amino acids, and a strong propensity for metal coordination create dense conformational and coordination landscapes that ...
Emmanuel Nkyaagye   +2 more
wiley   +1 more source

Structure-Based beta-Secretase (BACE1) Inhibitors [PDF]

open access: yes, 2014
Alois Alzheimer identified first abnormal deformation in the brain of diseased people with mental disorder. The disorder is clinically characterized by a progression from episodic memory problems to a slow global decline of cognitive function, ending ...
Keserű, György Miklós   +1 more
core  

Proapoptotic activity of new glutathione S-transferase inhibitors [PDF]

open access: yes, 2005
Selected 7-nitro-2,1,3-benzoxadiazole derivatives have been recently found very efficient inhibitors of glutathione S-transferase (GST) PI-1,(5) an enzyme which displays antiapoptotic activity and is also involved in the cellular resistance to anticancer
Bullo, A   +11 more
core   +2 more sources

Heterocycles in Peptidomimetics and Pseudopeptides: Design and Synthesis

open access: yesPharmaceuticals, 2012
This minireview provides a brief outline of the peculiar aspects of the preparation of peptidomimetic and pseudopeptidic structures containing heterocycles. In particular novel tricyclic structures are investigated as potential drugs.
Ambra Guarnaccio   +4 more
doaj   +1 more source

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