Results 101 to 110 of about 1,152,460 (369)

Solid-Phase Synthesis of Arylpiperazine Derivatives and Implementation of the Distributed Drug Discovery (D3) Project in the Search for CNS Agents

Molecules, 2011
We have successfully implemented the concept of Distributed Drug Discovery (D3) in the search for CNS agents. Herein, we demonstrate, for the first time, student engagement from different sites around the globe in the development of new biologically ...
William L. Scott, Ziniu Zhou, Martin J. O’Donnell, Grzegorz Satała, Andrzej J. Bojarski, Jean Martinez, Gaël Nomezine, Maciej Pawłowski, Gilles Subra, Katarzyna Grychowska, Joanna Król, Paweł Zajdel   +11 more
doaj   +1 more source

Mechanistic basis for inhibition of the extended‐spectrum β‐lactamase GES‐1 by enmetazobactam and tazobactam

FEBS Letters, EarlyView.
Antimicrobial resistance (AMR) is of huge importance, resulting in over 1 million deaths each year. Here, we describe how a new drug, enmetazobactam, designed to help fight resistant bacterial diseases, inhibits a key enzyme (GES‐1) responsible for AMR. Our data show it is a more potent inhibitor than the related tazobactam, with high‐level computation
Michael Beer, Philip Hinchliffe, Marko Hanževački, Christopher R. Bethel, Catherine L. Tooke, Marc W. Van der Kamp, Krisztina M. Papp‐Wallace, Robert A. Bonomo, Stuart Shapiro, Adrian J. Mulholland, James Spencer   +10 more
wiley   +1 more source

Heterologous Expression and Biochemical Characterization of a Novel Lytic Polysaccharide Monooxygenase from Chitinilyticum aquatile CSC-1

Microorganisms
Lytic polysaccharide monooxygenases (LPMOs) are copper-dependent enzymes that catalyze the oxidative cleavage of recalcitrant polysaccharides. There are limited reports on LPMOs capable of concurrently catalyzing the oxidative cleavage of both cellulose ...
Xuezhi Shao, Hongliang Fang, Tao Li, Liyan Yang, Dengfeng Yang, Lixia Pan   +5 more
doaj   +1 more source

Rapid Discovery of Illuminating Peptides for Instant Detection of Opioids in Blood and Body Fluids

Molecules, 2019
The United States is currently experiencing an opioid crisis, with more than 47,000 deaths in 2017 due to opioid overdoses. Current approaches for opioid identification and quantification in body fluids include immunoassays and chromatographic methods (e.
Shabnam Jafari, Yann Thillier, Yousif H. Ajena, Diedra Shorty, Jiannan Li, Jonathan S. Huynh, Bethany Ming-Choi Pan, Tingrui Pan, Kit S. Lam, Ruiwu Liu   +9 more
doaj   +1 more source

Novel and unscrutinized immune entities of the zebrafish gut

FEBS Letters, EarlyView.
Understudied cells of the zebrafish immune system include bona fide immune cells and epithelial (‐derived) cells with immune functions. Research focusing on zebrafish cells which demonstrate similarities to mammalian immune cell counterparts may help us understand the pathologies in which they are implicated. Currently available and advanced tools make
Audrey Inge Schytz Andersen‐Civil, Marine Mantel, Julia Soh, Serge Mostowy, Sylvia Brugman, Gilles Claude Vanwalleghem   +5 more
wiley   +1 more source

Library Design

CHIMIA, 2003
This review aims at giving a short introduction to the most important areas of library design. The description of compounds by descriptors and fingerprints, and similarity-based clustering techniques are illustrated in the context of untargeted ...
Friederike Stoll
doaj   +1 more source

Comb-e-Chem: an e-science research project

, 2002
The background to the Comb-e-Chem e-Science pilot project funded under the UK-Science Programme is presented and the areas being addresses within chemistry and more specifically combinatorial chemistry are discussed.
Frey, Jeremy G.
core   +1 more source

Rational, computer-aided design of multi-target ligands : poster presentation from 6th German Conference on Chemoinformatics, GCC 2010, Goslar, Germany. 7-9 November 2010 [PDF]

, 2011
Over the past two decades the “one drug – one target – one disease” concept became the prevalent paradigm in drug discovery. The main idea of this approach is the identification of a single protein target whose inhibition leads to a successful treatment ...
Achenbach, Janosch, Proschak, Ewgenij
core  

From lactation to malignancy: A comparison between healthy and cancerous breast gland at single‐cell resolution reveals new issues for tumorigenesis

FEBS Letters, EarlyView.
Single‐cell RNA sequencing reveals an opposite role of SLPI in basal tumors based on metastatic spread, along with shared activation of specific regulons in cancer cells and mature luminal lactocytes, as well as downregulation of MALAT1 and NEAT1 in the latter.
Pietro Ancona, Carlo M. Bergamini, Carlo Ferrari, Stefano Volinia, Nicoletta Bianchi   +4 more
wiley   +1 more source

Imeglimin attenuates liver fibrosis by inhibiting vesicular ATP release from hepatic stellate cells

FEBS Letters, EarlyView.
Imeglimin, at clinically relevant concentrations, inhibits vesicular ATP accumulation and release from hepatic stellate cells, thereby attenuating purinergic signaling and reducing fibrogenic activation. This mechanism reveals a newly identified antifibrotic action of imeglimin beyond glycemic control.
Seiji Nomura, Lixiang Wang, Nao Hasuzawa, Ayako Nagayama, Sawako Moriyama, Kenji Ashida, Yoshinori Moriyama, Masatoshi Nomura, Ken Yamamoto   +8 more
wiley   +1 more source