نتایج جستجو برای: multi target directed ligand

تعداد نتایج: 1076189  

2014
Andrea Tarozzi Manuela Bartolini Lorna Piazzi Luca Valgimigli Riccardo Amorati Cecilia Bolondi Alice Djemil Francesca Mancini Vincenza Andrisano Angela Rampa

The development of drugs with different pharmacological properties appears to be an innovative therapeutic approach for Alzheimer's disease. In this article, we describe a simple structural modification of AP2238, a first dual function lead, in particular the introduction of the catechol moiety performed in order to search for multi-target ligands. The new compound AP2469 retains anti-acetylcho...

Journal: :Proceedings of the National Academy of Sciences of the United States of America 2000
D A Erlanson A C Braisted D R Raphael M Randal R M Stroud E M Gordon J A Wells

We report a strategy (called "tethering") to discover low molecular weight ligands ( approximately 250 Da) that bind weakly to targeted sites on proteins through an intermediary disulfide tether. A native or engineered cysteine in a protein is allowed to react reversibly with a small library of disulfide-containing molecules ( approximately 1,200 compounds) at concentrations typically used in d...

2018
Zixuan Cang Lin Mu Guo-Wei Wei

This work introduces a number of algebraic topology approaches, including multi-component persistent homology, multi-level persistent homology, and electrostatic persistence for the representation, characterization, and description of small molecules and biomolecular complexes. In contrast to the conventional persistent homology, multi-component persistent homology retains critical chemical and...

Journal: :British Journal of Pharmacology 2010

Journal: :Chemical science 2015
Yousuke Takaoka Yuki Nishikawa Yuki Hashimoto Kenta Sasaki Itaru Hamachi

A rapid and selective ligand-directed chemical reaction was developed for the acylation of proteins in living cells on the basis of ligand-directed chemistry. By fine tuning the reactivity and stability of the phenyl ester derivatives, we successfully identified ortho-dibromophenyl benzoate as the optimal reactive motif. It was sufficiently stable in an aqueous buffer, hydrolyzing less than 10%...

Journal: :Kidney International Reports 2023

Lupus nephritis (LN) occurs in up to 60% of patients with systemic lupus erythematosus (SLE). Despite current development immunosuppressant agents, LN still impairs the survival and quality life SLE patients. Receptor for advanced glycation endproducts (RAGE) is a multi-ligand receptor that belongs immunoglobulin superfamily, which strongly associated innate immune system. In present study, we ...

Journal: :Proceedings of the National Academy of Sciences of the United States of America 2013
Denise Wootten John Simms Laurence J Miller Arthur Christopoulos Patrick M Sexton

Recently, the concept of ligand-directed signaling--the ability of different ligands of an individual receptor to promote distinct patterns of cellular response--has gained much traction in the field of drug discovery, with the potential to sculpt biological response to favor therapeutically beneficial signaling pathways over those leading to harmful effects. However, there is limited understan...

Objective(s): Detection of circulating Mycobacterium tuberculosis (M. tuberculosis) antigens is promising in Tuberculosis (TB) diagnosis. However, not a single antigen marker has been found to be widely expressed in all TB patients. This study is aimed to prepare broadly reactive polyclonal antibodies targeting multiple antigen markers (multi-target antibodies) and evaluate their efficacies in ...

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