Results 21 to 30 of about 47,963 (298)

Quantitative Determination of 5-Aminoisoquinoline, a PARP-1 Inhibitor by UPLC-MS/MS: In Silico ADME Profile and In Vitro Metabolic Stability Study

Applied Sciences, 2022
5-Aminoisoquinoline (5-AIQ) is a water-soluble, potent and selective Poly (ADP-ribose) polymerase 1 (PARP-1) inhibitor, widely used as a biochemical and pharmacological tool to study the inhibitory effect of PARPs enzyme.
Muzaffar Iqbal, Essam A. Ali, Mohd Abul Kalam, Sheikh F. Ahmad, Rashad Al-Salahi   +4 more
doaj   +1 more source

Manipulation of Chemistry and Biology with Visible Light Using Tetra‐ortho‐Substituted Azobenzenes and Azonium Ions

Angewandte Chemie, EarlyView.
Tetra‐ortho‐Azobenzenes (TOABs) in broad daylight: in recent years, TOAB photoswitches became indispensable tools for all‐visible‐light manipulation of chemistry, biology and materials. This review explores their unique photochemical properties, design and synthetic approaches, offering support in choosing a TOAB for a given application.
Francesca Cardano, Rosa Márquez García, Wiktor Szymanski   +2 more
wiley   +2 more sources

The ATM Kinase Inhibitor AZD0156 Is a Potent Inhibitor of Plasmodium Phosphatidylinositol 4‐Kinase (PI4Kβ) and Is an Attractive Candidate for Medicinal Chemistry Optimization Against Malaria

Angewandte Chemie, EarlyView.
AZD0156, an ATM kinase inhibitor in clinical development, shows promising multistage antiplasmodial activity by targeting Plasmodium falciparum phosphatidylinositol 4‐kinase (PfPI4Kβ). With an improved specificity profile relative to other PfPI4Kβ inhibitors and moderate efficacy in a P.
John G. Woodland, Dina Coertzen, Kathryn J. Wicht, Virginia Franco Hidalgo, Charisse Flerida A. Pasaje, Luiz C. Godoy, Tarrick Qahash, Mmakwena M. Mmonwa, Godwin A. Dziwornu, Lynn Wambua, Sarah Harries, Constance M. Korkor, Mathew Njoroge, Liezl Krugmann, Dale Taylor, Meta Leshabane, Henrico Langeveld, Tayla Rabie, Janette Reader, Mariëtte van der Watt, Nelius Venter, Erica Erlank, Ayesha S. Aswat, Lizette L. Koekemoer, Tomas Yeo, Jin H. Jeon, David A. Fidock, Francisco Javier Gamo, Sergio Wittlin, Jacquin C. Niles, Manuel Llinas, Lauren B. Coulson, Lyn‐Marié Birkholtz, Kelly Chibale   +33 more
wiley   +2 more sources

Relationship between NAFLD and coronary artery disease: A Mendelian randomization study

Hepatology, EarlyView., 2022
Abstract Background and Aims There is an ongoing debate on whether NAFLD is an active contributor or an innocent bystander in the pathogenesis of coronary artery disease (CAD). The aim of the present study was to assess the causal relationship between NAFLD and CAD.
Zhewen Ren, Pomme I. H. G. Simons, Anke Wesselius, Coen D. A. Stehouwer, Martijn C. G. J. Brouwers   +4 more
wiley   +1 more source

Oxidative Rearrangements of the Alkaloid Intermediate Geissoschizine

Angewandte Chemie, EarlyView.
19E‐geissoschizine is a key precursor in the biosynthesis of monoterpene indole alkaloids such as strychnine, ibogaine, and vinblastine. Using enzymatic assays and gene silencing, three CYPs were identified from C. roseus that oxidize this compound to four alkaloid scaffolds: strychnos, sarpagan, akuammiline, and mavacurane. Mutational analysis reveals
Mohamed O. Kamileen, Benke Hong, Klaus Gase, Maritta Kunert, Lorenzo Caputi, Benjamin R. Lichman, Sarah E. O'Connor   +6 more
wiley   +2 more sources

Intestinal peroxisome proliferator‐activated receptor α‐fatty acid‐binding protein 1 axis modulates nonalcoholic steatohepatitis

Hepatology, EarlyView., 2022
Abstract Background and Aims Peroxisome proliferator‐activated receptor α (PPARα) regulates fatty acid transport and catabolism in liver. However, the role of intestinal PPARα in lipid homeostasis is largely unknown. Here, intestinal PPARα was examined for its modulation of obesity and NASH. Approach and Results Intestinal PPARα was activated and fatty
Tingting Yan, Yuhong Luo, Nana Yan, Keisuke Hamada, Nan Zhao, Yangliu Xia, Ping Wang, Changdong Zhao, Dan Qi, Shoumei Yang, Lulu Sun, Jie Cai, Qiong Wang, Changtao Jiang, Oksana Gavrilova, Kristopher W. Krausz, Daxesh P. Patel, Xiaoting Yu, Xuan Wu, Haiping Hao, Weiwei Liu, Aijuan Qu, Frank J. Gonzalez   +22 more
wiley   +1 more source

3‐Oxabicyclo[3.1.1]heptane as an Isostere of meta‐Benzene

Angewandte Chemie, EarlyView.
3‐Oxabicyclo[3.1.1]heptanes were designed as saturated isosteres of meta‐benzene. Crystallographic analysis revealed that these structures and meta‐benzene have identical geometric properties. Replacement of the central benzene ring in the anticancer drug Sonidegib with 3‐oxabicyclo[3.1.1]heptane provided a patent‐free analogue with a nanomolar potency,
Dmitry Dibchak, Pavel K. Mykhailiuk
wiley   +2 more sources

Elucidation of Arctigenin Pharmacokinetics and Tissue Distribution after Intravenous, Oral, Hypodermic and Sublingual Administration in Rats and Beagle Dogs: Integration of In Vitro and In Vivo Findings

Frontiers in Pharmacology, 2017
Although arctigenin (AG) has diverse bioactivities, such as anti-oxidant, anti-inflammatory, anti-cancer, immunoregulatory and neuroprotective activities, its pharmacokinetics have not been systematically evaluated.
Jie Li, Jie Li, Jie Li, Xin Li, Xin Li, Xin Li, Yu-Shan Ren, Yu-Shan Ren, Yuan-Yuan Lv, Yuan-Yuan Lv, Yuan-Yuan Lv, Jun-Sheng Zhang, Jun-Sheng Zhang, Jun-Sheng Zhang, Xiao-Li Xu, Xiao-Li Xu, Xiao-Li Xu, Xian-Zhen Wang, Xian-Zhen Wang, Xian-Zhen Wang, Jing-Chun Yao, Jing-Chun Yao, Jing-Chun Yao, Gui-Min Zhang, Gui-Min Zhang, Zhong Liu, Zhong Liu   +26 more
doaj   +1 more source

NAFLD‐related hepatocellular carcinoma: The growing challenge

Hepatology, EarlyView., 2022
Risk and protective factors for NAFLD‐related hepatocellular carcinoma Abstract Hepatocellular carcinoma (HCC) is a common cause of cancer‐related mortality and morbidity worldwide. With the obesity pandemic, NAFLD‐related HCC is contributing to the burden of disease exponentially.
Pir Ahmad Shah, Rashmee Patil, Stephen A. Harrison   +2 more
wiley   +1 more source

Loss of hepatic SMLR1 causes hepatosteatosis and protects against atherosclerosis due to decreased hepatic VLDL secretion

Hepatology, EarlyView., 2022
The role of SMLR1 in lipid metabolism (high fat + cholesterol diet in mice) Abstract Background and Aims The assembly and secretion of VLDL from the liver, a pathway that affects hepatic and plasma lipids, remains incompletely understood. We set out to identify players in the VLDL biogenesis pathway by identifying genes that are co‐expressed with the ...
Willemien van Zwol, Antoine Rimbert, Justina C. Wolters, Marieke Smit, Vincent W. Bloks, Niels J. Kloosterhuis, Nicolette C. A. Huijkman, Mirjam H. Koster, Umesh Tharehalli, Simon M. de Neck, Colin Bournez, Marceline M. Fuh, Jeroen Kuipers, Sujith Rajan, Alain de Bruin, Henry N. Ginsberg, Gerard J. P. van Westen, M. Mahmood Hussain, Ludger Scheja, Joerg Heeren, Philip Zimmerman, Bart van de Sluis, Jan Albert Kuivenhoven   +22 more
wiley   +1 more source