Results 81 to 90 of about 130,723 (312)

In vitro and in vivo studies of the trypanocidal properties of WRR-483 against Trypanosoma cruzi. [PDF]

, 2010
BackgroundCruzain, the major cysteine protease of Trypanosoma cruzi, is an essential enzyme for the parasite life cycle and has been validated as a viable target to treat Chagas' disease.
Brinen, Linda S, Chen, Yen Ting, Doyle, Patricia S, Hansell, Elizabeth, Kerr, Iain D, McKerrow, James H, Roush, William R   +6 more
core   +3 more sources

Development of Photo‐Biocatalytic Redox System for Asymmetric Synthesis of Optically Active Amines Using Blue Light and Transaminases. A Case Study Toward Mavacamten

Advanced Synthesis &Catalysis, EarlyView.
Abstract α‐Chiral amines are versatile building blocks for the asymmetric synthesis of optically pure high‐added‐value chemicals, including pharmaceuticals, agrochemicals, and natural products. Herein, we report a one‐pot, two‐step sequential deracemization of racemic sec‐alcohols to optically enriched primary amines throught a photo‐biocatalytic ...
Natalia Antos, Aleksandra Rudzka, Anna Hoser, Tamara Reiter, Wolfgang Kroutil, Paweł Borowiecki   +5 more
wiley   +1 more source

Profile of etravirine for the treatment of HIV infection

Therapeutics and Clinical Risk Management, 2010
Alice Tseng1, Rodger D MacArthur21Toronto General Hospital, Toronto, ON, Canada; 2Division of Infectious Diseases, Wayne State University, Detroit, Michigan, USAAbstract: Etravirine is a second-generation non-nucleoside reverse transcriptase inhibitor ...
Alice Tseng, Rodger D MacArthur
doaj  

Bilirubin Targeting WNK1 to Alleviate NLRP3‐Mediated Neuroinflammation

Advanced Science, EarlyView.
At physiological concentrations, bilirubin binds to the kinase domain of WNK1, thereby augmenting its activity and facilitating the phosphorylation of downstream SPAK/OSR1. This phosphorylation inhibits KCC2 activity, leading to elevate intracellular chloride levels in neurons.
Linfei Mao, Jiayu Lu, Quanjun Yang, Zhenqi Liu, Cuiping Wu, Bingbing Ke, Kaiyan Su, Haolin Yuan, Yaqi Cui, Yao Wang, Richard Salvi, Guang Yang, Shankai Yin, Feng Liu, Chunyan Li   +14 more
wiley   +1 more source

Pharmacokinetic characteristics of telaprevir in healthy Korean male subjects and comparisons with Japanese

Drug Design, Development and Therapy, 2018
Yewon Choi,1 Seonghae Yoon,1 Kyoko Matsumoto,2 Yoshiyasu Ohta,3 SeungHwan Lee,1 Kyung-Sang Yu,1 In-Jin Jang1 1Department of Clinical Pharmacology and Therapeutics, Seoul National University College of Medicine and Hospital, Seoul, Republic of Korea ...
Choi Y, Yoon S, Matsumoto K, Ohta Y, Lee S, Yu KS, Jang IJ   +6 more
doaj  

NaBC1 Boron Transporter Enables Myoblast Response to Substrate Rigidity via Fibronectin‐Binding Integrins

Advanced Science, EarlyView.
Cells transduce the rigidity of the environment into biochemical cues through mechanotransductive cascades that modulate cell behavior. Here, a novel role for the boron transporter NaBC1 is identified as a mechanotransducer involved in regulating cell behavior via specific crosstalk with fibronectin‐binding integrins.
Juan Gonzalez‐Valdivieso, Giuseppe Ciccone, Udesh Dhawan, Tezz Quon, Eva Barcelona‐Estaje, Aleixandre Rodrigo‐Navarro, Rafael R. Castillo, Graeme Milligan, Patricia Rico, Manuel Salmeron‐Sanchez   +9 more
wiley   +1 more source

Fibroblast activation protein (FAP) as a novel metabolic target

Molecular Metabolism, 2016
Objective: Fibroblast activation protein (FAP) is a serine protease belonging to a S9B prolyl oligopeptidase subfamily. This enzyme has been implicated in cancer development and recently reported to regulate degradation of FGF21, a potent metabolic ...
Miguel Angel Sánchez-Garrido, Kirk M. Habegger, Christoffer Clemmensen, Cassie Holleman, Timo D. Müller, Diego Perez-Tilve, Pengyun Li, Archita S. Agrawal, Brian Finan, Daniel J. Drucker, Matthias H. Tschöp, Richard D. DiMarchi, Alexei Kharitonenkov   +12 more
doaj  

Virtual screening of Microalgal compounds as potential inhibitors of Type 2 Human Transmembrane serine protease (TMPRSS2) [PDF]

arXiv, 2021
More than 198 million cases of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has been reported that result in no fewer than 4.2 million deaths globally. The rapid spread of the disease coupled with the lack of specific registered drugs for its treatment pose a great challenge that necessitate the development of therapeutic agents from a ...
arxiv  

Advancing the Identification of Bioactive Molecules and the Construction of a Synergistic Drug Delivery System in Combating Lung Injury

Advanced Science, EarlyView.
Traditional Chinese Medicine (TCM), while holistic and historically esteemed, faces challenges in “miracle cures” due to slow onset, long cycles, and difficulty controlling quality. This study obtains the active ingredients, glabridin (GLA) and puerarin (PUE), from Ge‐Gen Decoction (GGD), developing a safe and effective drug delivery system, GLA‐PUE ...
Jianhong Qi, Yanxia Wang, Huan Chen, Kaitian Wu, Pei Zhou, Yue Dou, Bingqi Xiong, Wei Zhou   +7 more
wiley   +1 more source

A folding inhibitor of the HIV-1 Protease [PDF]

arXiv, 2005
Being the HIV-1 Protease (HIV-1-PR) an essential enzyme in the viral life cycle, its inhibition can control AIDS. The folding of single domain proteins, like each of the monomers forming the HIV-1-PR homodimer, is controlled by local elementary structures (LES, folding units stabilized by strongly interacting, highly conserved, as a rule hydrophobic ...
arxiv