Results 51 to 60 of about 10,733 (194)

Development of organophosphate hydrolase activity in a bacterial homolog of human cholinesterase

Frontiers in Chemistry, 2014
We applied a combination of rational design and directed evolution (DE) to Bacillus subtilis p-nitrobenzyl esterase (pNBE) with the goal of enhancing organophosphorus acid anhydride hydrolase (OPAAH) activity.
Patricia Marie Legler, Susanne eBoisvert, Jaimee R Compton, Charles B. Millard   +3 more
doaj   +1 more source

Carboxylesterase 1d (Ces1d) does not contribute to cholesteryl ester hydrolysis in the liver

Journal of Lipid Research, 2021
The liver is the central organ regulating cholesterol synthesis, storage, transport, and elimination. Mouse carboxylesterase 1d (Ces1d) and its human ortholog CES1 have been described to possess lipase activity and play roles in hepatic triacylglycerol ...
Jihong Lian, Jelske N. van der Veen, Russell Watts, René L. Jacobs, Richard Lehner   +4 more
doaj   +1 more source

Asymmetric Construction of a Multi-Pharmacophore-Containing Dispirotriheterocyclic Scaffold and Identification of a Human Carboxylesterase 1 Inhibitor [PDF]

, 2018
A catalytic asymmetric [3 + 2] cyclization of novel 4-isothiocyanato pyrazolones and isatin-derived ketimines was developed, delivering a wide range of intriguing dispirotriheterocyclic products in high yield with excellent diastereoselectivity and ...
Shiqiang Wei (1477456), Xiaoze Bao (1490524), Xingkai Qian (5249099), Jingping Qu (556366), Baomin Wang (174006), Liwei Zou (1944679), Guangbo Ge (5249102)   +6 more
core   +1 more source

Simplified assays of lipolysis enzymes for drug discovery and specificity assessment of known inhibitors

Journal of Lipid Research, 2016
Lipids are used as cellular building blocks and condensed energy stores and also act as signaling molecules. The glycerolipid/ fatty acid cycle, encompassing lipolysis and lipogenesis, generates many lipid signals.
Jose Iglesias, Julien Lamontagne, Heidi Erb, Sari Gezzar, Shangang Zhao, Erik Joly, Vouy Linh Truong, Kathryn Skorey, Sheldon Crane, S.R.Murthy Madiraju, Marc Prentki   +10 more
doaj   +1 more source

A Pharmacokinetic and Pharmacodynamic Evaluation of the Anti-Hepatocellular Carcinoma Compound 4-N-Carbobenzoxy-gemcitabine (Cbz-dFdC)

Molecules, 2020
Gemcitabine (dFdC) demonstrates significant effectiveness against solid tumors in vitro and in vivo; however, its clinical application is limited because it tends to easily undergo deamination metabolism.
Yilin Sun, Jiankun Wang, Kun Hao
doaj   +1 more source

Identification of Catalposide Metabolites in Human Liver and Intestinal Preparations and Characterization of the Relevant Sulfotransferase, UDP-glucuronosyltransferase, and Carboxylesterase Enzymes

Pharmaceutics, 2019
Catalposide, an active component of Veronica species such as Catalpa ovata and Pseudolysimachion lingifolium, exhibits anti-inflammatory, antinociceptic, anti-oxidant, hepatoprotective, and cytostatic activities.
Deok-Kyu Hwang, Ju-Hyun Kim, Yongho Shin, Won-Gu Choi, Sunjoo Kim, Yong-Yeon Cho, Joo Young Lee, Han Chang Kang, Hye Suk Lee   +8 more
doaj   +1 more source

Frequency of Pyrethroid Insecticide Resistance kdr Gene and Its Associated Enzyme Modulation in Housefly, Musca domestica L. Populations From Jhang, Pakistan

Frontiers in Environmental Science, 2022
Housefly, Musca domestica, is considered responsible for transmitting a wide variety of human and veterinary diseases. Mostly, insecticides are being used for their control and more commonly, pyrethroid insecticides worldwide.
Bushra Riaz, Muhammad Kashif Zahoor, Kausar Malik, Aftab Ahmad, Humara Naz Majeed, Farhat Jabeen, Muhammad Zulhussnain, Kanwal Ranian   +7 more
doaj   +1 more source

Carboxylesterase-1 Assisted Targeting of HDAC Inhibitors to Mononuclear Myeloid Cells in Inflammatory Bowel Disease [PDF]

, 2022
Background and Aims: Histone deacetylase inhibitors [HDACi] exert potent anti-inflammatory effects. Because of the ubiquitous expression of HDACs, clinical utility of HDACi is limited by off-target effects.
Prinjha, Rab K, van Hamersveld, Patricia H P, Rioja, Inmaculada, Heinsbroek, Sigrid E M, Li Yim, Andrew Y F, Tomlinson, Laura, Bell, Matthew J, Mander, Palwinder K, Wildenberg, Manon E, Welting, Olaf, Rahman, Shafaque, Garcia-Vallejo, Juan J, Elfiky, Ahmed M I, Gregory, Richard, Verhoeff, Jan, de Krijger, Manon, Hageman, Ishtu L, Lewis, Huw D, Ghiboub, Mohammed, Furze, Rebecca C, Admiraal, Iris, de Jonge, Wouter J   +21 more
core   +1 more source

Discovery of lignans as the effective inhibitors of CES1A alleviate lipid droplets formation

Journal of Enzyme Inhibition and Medicinal Chemistry
ER carboxylesterase 1A (CES1A) is an important metabolic enzyme involved in lipid metabolism. Targeting the CES1A is a promising approach for diseases associated with disorders of lipid metabolism therapy.
Jie Mu, Si-Si Chen, Shi-Qing Li, Qiang Jin, Jin Geng, Li-Wei Zou   +5 more
doaj   +1 more source

Fluorine impairs carboxylesterase 1-mediated hydrolysis of T-2 toxin and increases its chondrocyte toxicity

Frontiers in Nutrition, 2022
BackgroundT-2 toxin is recognized as one of the high-risk environmental factors for etiology and pathogenesis of Kashin-Beck disease (KBD). Previous evidence indicates decreased serum fluorine level in KBD patients.
Yumeng Jia, Sirong Shi, Bolun Cheng, Shiqiang Cheng, Li Liu, Peilin Meng, Xuena Yang, Xiaoge Chu, Yan Wen, Feng Zhang, Xiong Guo   +10 more
doaj   +1 more source