Results 11 to 20 of about 368,214 (310)

Hit Expansion of a Noncovalent SARS-CoV-2 Main Protease Inhibitor

ACS Pharmacology & Translational Science, 2022
Inhibition of the SARS-CoV-2 main protease (Mpro) is a major focus of drug discovery efforts against COVID-19. Here we report a hit expansion of non-covalent inhibitors of Mpro. Starting from a recently discovered scaffold (The COVID Moonshot Consortium.
J. Glaser, A. Sedova, S. Galanie, D. Kneller, Russell B. Davidson, Elvis Maradzike, Sara Del Galdo, Audrey D. Labbe, Darren J. Hsu, Rupesh Agarwal, D. Bykov, Arnold N. Tharrington, Jerry M. Parks, Dayle M. Smith, I. Daidone, L. Coates, A. Kovalevsky, Jeremy C. Smith   +17 more
semanticscholar   +1 more source

Identification of Theaflavin-3,3’-Digallate as a Novel Zika Virus Protease Inhibitor

Frontiers in Pharmacology, 2020
Mounting evidence indicates that Zika virus (ZIKV) is closely related to neurological disorders such as microcephaly and Guillain-Barré syndrome. There are currently no effective vaccines and FDA-approved inhibitors against ZIKV infection. The flaviviral
Xiangling Cui, Rui Zhou, Chenchao Huang, Rongyu Zhang, Jing Wang, Yongxin Zhang, Jiwei Ding, Xiaoyu Li, Jinming Zhou, S. Cen   +9 more
semanticscholar   +1 more source

Distinct phosphorylation clusters determines the signalling outcome of the free fatty acid receptor FFA4/GPR120 [PDF]

, 2016
It is established that long-chain free fatty acids including ω-3 fatty acids mediate an array of biological responses through members of the free fatty acid receptor family, which includes FFA4.
Alvarez-Curto, Elisa, Butcher, Adrian J., Hudson, Brian D., Miller, Ashley M., Milligan, Graeme, Prihandoko, Rudi, Tobin, Andrew B., Ulven, Trond   +7 more
core   +2 more sources

Pharmacological and therapeutic properties of ritonavir-boosted protease inhibitor therapy in HIV-infected patients [PDF]

Journal of Antimicrobial Chemotherapy, 2003
Boosted protease inhibitor regimens combine ritonavir with a second, 'boosted' protease inhibitor to enhance patient exposure to the latter agent, thereby preventing or overcoming resistance and allowing less frequent dosing, potentially improving adherence.
Robert K, Zeldin, Richard A, Petruschke
openaire   +2 more sources

A Pharmacologic Inhibitor of the Protease Taspase1 Effectively Inhibits Breast and Brain Tumor Growth [PDF]

Cancer Research, 2012
Abstract The threonine endopeptidase Taspase1 has a critical role in cancer cell proliferation and apoptosis. In this study, we developed and evaluated small molecule inhibitors of Taspase1 as a new candidate class of therapeutic modalities.
David Y, Chen, Yishan, Lee, Brian A, Van Tine, Adam C, Searleman, Todd D, Westergard, Han, Liu, Ho-Chou, Tu, Shugaku, Takeda, Yiyu, Dong, David R, Piwnica-Worms, Kyoung J, Oh, Stanley J, Korsmeyer, Ann, Hermone, Richard, Gussio, Robert H, Shoemaker, Emily H-Y, Cheng, James J-D, Hsieh   +16 more
openaire   +2 more sources

Pharmacological dissociation of memory: Anisomycin, a protein synthesis inhibitor, and leupeptin, a protease inhibitor, block different learning tasks [PDF]

Behavioral and Neural Biology, 1985
Inhibition of protein synthesis by anisomycin for a short duration impairs memory of a one-trial inhibitory avoidance task in rats. Memory of escape conditioning involving eight trials is disrupted only if the duration of protein synthesis is prolonged by repeated injections.
Stäubli, U, Faraday, R, Lynch, G
openaire   +3 more sources

TGFβ impairs HNF1α functional activity in Epithelial-to-Mesenchymal Transition interfering with the recruitment of CBP/p300 acetyltransferases [PDF]

, 2019
The cytokine transforming growth factor β (TGFβ) plays a crucial role in the induction of both epithelial-to-mesenchymal transition (EMT) program and fibro-cirrhotic process in the liver, where it contributes also to organ inflammation following several ...
Amicone, Laura, Battistelli, Cecilia, Bisceglia, Francesca, Marchetti, Alessandra, Montaldo, Claudia, Noce, Valeria, Strippoli, Raffaele, Tripodi, Marco, Zammataro, Agatino   +8 more
core   +1 more source

General and Modular Strategy for Designing Potent, Selective, and Pharmacologically Compliant Inhibitors of Rhomboid Proteases [PDF]

Cell Chemical Biology, 2017
Rhomboid-family intramembrane proteases regulate important biological processes and have been associated with malaria, cancer, and Parkinson's disease. However, due to the lack of potent, selective, and pharmacologically compliant inhibitors, the wide therapeutic potential of rhomboids is currently untapped. Here, we bridge this gap by discovering that
Ticha, Anezka, Stanchev, Stancho, Vinothkumar, Kutti R., Mikles, David C., Pachl, Petr, Began, Jakub, Skerle, Jan, Svehlova, Katerina, Nguyen, Minh T.N., Verhelst, Steven, Johnson, Darren C., Bachovchin, Daniel A., Lepsik, Martin, Majer, Pavel, Strisovsky, Kvido   +14 more
openaire   +2 more sources

The p110 delta structure: mechanisms for selectivity and potency of new PI(3)K inhibitors. [PDF]

, 2010
Deregulation of the phosphoinositide-3-OH kinase (PI(3)K) pathway has been implicated in numerous pathologies including cancer, diabetes, thrombosis, rheumatoid arthritis and asthma.
Alex Berndt, Benjamin T Houseman, Christian Rommel, Daniel D Le, Fabrice Gorrec, Jeffrey P Shaw, Joseph I Pacold, Kevan M Shokat, Matthias K Schwarz, Olusegun Williams, Pascale Gaillard, Pingda Ren, Roger L Williams, Simon Miller, Thomas Rückle, Wai-Ching Hon, Yi Liu   +16 more
core   +2 more sources

Nilotinib, an approved leukemia drug, inhibits smoothened signaling in Hedgehog-dependent medulloblastoma. [PDF]

, 2019
Dysregulation of the seven-transmembrane (7TM) receptor Smoothened (SMO) and other components of the Hedgehog (Hh) signaling pathway contributes to the development of cancers including basal cell carcinoma (BCC) and medulloblastoma (MB).
Abagyan, Ruben, Chahal, Kirti Kandhwal, Chen, Clark C, Durden, Donald L, Kufareva, Irina, Li, Jie, Parle, Milind, Wechsler-Reya, Robert J   +7 more
core   +1 more source