Zobrazeno 1 - 10
of 866
pro vyhledávání: '"covalent inhibitor"'
Autor:
Jinsai Shang, Douglas J Kojetin
Publikováno v:
eLife, Vol 13 (2024)
Peroxisome proliferator-activated receptor gamma (PPARγ) is a nuclear receptor transcription factor that regulates gene expression programs in response to ligand binding. Endogenous and synthetic ligands, including covalent antagonist inhibitors GW9
Externí odkaz:
https://doaj.org/article/fb8838a62f4b4e72936073ad314cfa87
Publikováno v:
Molecules, Vol 29, Iss 20, p 4870 (2024)
Glycoside hydrolases have been implicated in a wide range of human conditions including lysosomal storage diseases. Consequently, many researchers have directed their efforts towards identifying new classes of glycoside hydrolase inhibitors, both syn
Externí odkaz:
https://doaj.org/article/b22d705092f045858673c53a8b27fbd2
Akademický článek
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Tetrandrine inhibits aldosterone synthesis by covalently targeting CYP11A1 to attenuate hypertension
Publikováno v:
Frontiers in Pharmacology, Vol 15 (2024)
IntroductionTetrandrine (Tet) is the main pharmacological component of Stephania tetrandra S. Moore, which is a well-documented traditional Chinese medicine known for its diuretic and antihypertensive properties. Unraveling the specific targets and m
Externí odkaz:
https://doaj.org/article/c850244bc67249d7bf3be8efec69c5d1
Autor:
Kanzal Iman, Muhammad Usman Mirza, Fazila Sadia, Matheus Froeyen, John F. Trant, Safee Ullah Chaudhary
Publikováno v:
Viruses, Vol 16, Iss 8, p 1250 (2024)
The emergence of drug-resistance-inducing mutations in Hepatitis C virus (HCV) coupled with genotypic heterogeneity has made targeting NS3/4A serine protease difficult. In this work, we investigated the mutagenic variations in the binding pocket of G
Externí odkaz:
https://doaj.org/article/5012ef92da2b40af9dddc0f0eba8f9f7
Autor:
Anirban Ghoshal, Álvaro F. Magalhães, Kesatebrhan Haile Asressu, Mohammad Anwar Hossain, Matthew H. Todd, Timothy M. Willson
Publikováno v:
Pharmaceuticals, Vol 17, Iss 7, p 836 (2024)
Optimized syntheses of (E)-5-(2-ethoxyphenyl)-N-(3-(methylsulfonyl)allyl)-1H-pyrazole-3-carboxamide (RA-0002034, 1), a promising antiviral covalent cysteine protease inhibitor lead, were developed. The syntheses avoid the contamination of 1 with the
Externí odkaz:
https://doaj.org/article/87f8f130ef43418e9874a8e9b8ca2984
Autor:
Anni Hu, Hang Wang, Qianqian Xu, Yuqi Pan, Zeyu Jiang, Sheng Li, Yi Qu, Yili Hu, Hao Wu, Xinzhi Wang
Publikováno v:
Redox Biology, Vol 68, Iss , Pp 102959- (2023)
Colorectal cancer (CRC) is a common and deadly disease of the digestive system, but its targeted therapy is hampered by the lack of reliable and specific biomarkers. Hence, discovering new therapeutic targets and agents for CRC is an urgent and chall
Externí odkaz:
https://doaj.org/article/88844f04209a4906bbe3f806d741b1db
Autor:
Lisa Hong, Dennis C. Braden, Yaoning Zhao, John J. Skoko, Fei Chang, Steven R. Woodcock, Crystall Uvalle, Allison Casey, Katherine Wood, Sonia R. Salvatore, Alparslan Asan, Trey Harkness, Adeola Fagunloye, Mortezaali Razzaghi, Adam Straub, Maria Spies, Daniel D. Brown, Adrian V. Lee, Francisco Schopfer, Bruce A. Freeman, Carola A. Neumann
Publikováno v:
Redox Biology, Vol 66, Iss , Pp 102856- (2023)
Nitro fatty acids (NO2-FAs) are endogenously generated lipid signaling mediators from metabolic and inflammatory reactions between conjugated diene fatty acids and nitric oxide or nitrite-derived reactive species. NO2-FAs undergo reversible Michael a
Externí odkaz:
https://doaj.org/article/74e2d4a459964b33908f0fc33cbe7493
Autor:
Diego Benítez, Jaime Franco, Florencia Sardi, Alejandro Leyva, Rosario Durán, Gahee Choi, Gyongseon Yang, Taehee Kim, Namyoul Kim, Jinyeong Heo, Kideok Kim, Honggun Lee, Inhee Choi, Constantin Radu, David Shum, Joo Hwan No, Marcelo A. Comini
Publikováno v:
Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 37, Iss 1, Pp 912-929 (2022)
Trypanothione synthetase (TryS) catalyses the synthesis of N1,N8-bis(glutathionyl)spermidine (trypanothione), which is the main low molecular mass thiol supporting several redox functions in trypanosomatids. TryS attracts attention as molecular targe
Externí odkaz:
https://doaj.org/article/d6287e9bbb0746028794672207991f63
Akademický článek
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