Results 31 to 40 of about 35,596 (239)

Targeting the Spliceosomal Protein USP39 Through Allosteric Ligands and PROTAC‐Induced Degradation

Angewandte Chemie International Edition, EarlyView.
Proteolysis‐targeting chimeras (PROTACs) enable degradation of proteins previously considered undruggable by harnessing the cellular ubiquitin–proteasome system. In this study, Schäfer et al. identify thiazole‐based small molecules that allosterically bind the zinc finger domain of ubiquitin‐specific protease 39 (USP39), a non‐enzymatic scaffold ...
Daniel Schäfer, Cristian Prieto‐Garcia, Jianhui Wang, Marcel Heinz, Vigor Matkovic, Pavel Kielkowski, Sebastian Hasselbeck, Varun Jayeshkumar Shah, Stefan Knapp, Gerhard Hummer, Ivan Dikic, Xinlai Cheng   +11 more
wiley   +1 more source

Thromboembolic and neurologic sequelae of discontinuation of an antihyperlipidemic drug during ongoing warfarin therapy [PDF]

, 2017
Warfarin and antihyperlipidemics are commonly co-prescribed. Some antihyperlipidemics may inhibit warfarin deactivation via the hepatic cytochrome P450 system.
Bilker, Warren B., Brensinger, Colleen M., Hennessy, Sean, Kimmel, Stephen E., Leonard, Charles E., Whitaker, Heather J.   +5 more
core   +2 more sources

Uptake of DPYD and UGT1A1 testing in Italy and adherence to pharmacogenetic guidelines: A 5‐year perspective from an EQA provider

British Journal of Clinical Pharmacology, EarlyView.
Aims Pharmacogenetic implementation requires awareness of the state‐of‐the‐art practice of laboratories providing pharmacogenetic testing. This study investigated how pharmacogenetic guidelines and recommendations have been implemented over time by Italian laboratories participating in the external quality assessment (EQA) Pharmaco‐scheme established ...
Rossana Roncato, Samantha Perfler, Diletta Pasin, Elena Peruzzi, Michael Woodcock, Henry Thomas, Rebecca Goodall, Simon J. Patton, Erika Cecchin   +8 more
wiley   +1 more source

Pharmacokinetic profiles of sertraline in pregnancy as a predictor of postpartum depressive symptoms

British Journal of Clinical Pharmacology, EarlyView.
Aim To characterize pharmacokinetic changes of sertraline and its metabolite during pregnancy and postpartum, and their relationship to maternal postpartum depressive symptoms. Methods This was a prospective observational, longitudinal study of pregnant women with a major depressive disorder treated with sertraline (N = 185 women, 205 pregnancies ...
Sílvia M. Illamola, Zachary N. Stowe, Marc L. Kalin, Michael D. Evans, Catherine M. Sherwin, Maged M. Costantine, D. Jeffrey Newport, James C. Ritchie, Angela K. Birnbaum   +8 more
wiley   +1 more source

Studies on Regioselective Binding Mode of Steroid Molecules in Homology Modeled Cytochrome P450-2C11 [PDF]

, 2009
In this study, we investigated the regioselective binding mode of steroid molecules and structure requirements for steroid molecules for 16[alpha]-hydroxylation by Cytochrome P450-2C11.
Eiichi Akaho, Hamed I. Ali, Hukihisa Fujita, Morio Yamada   +3 more
core   +1 more source

Regulation of human CYP2C9 expression by electrophilic stress involves AP-1 activation and DNA looping [PDF]

, 2014
CYP2C9 and CYP2C19 are important human enzymes that metabolize therapeutic drugs, environmental chemicals and physiologically important endogenous compounds.
Goldstein, J. A., Makia, N. L., Monostory, K., Prough, R. A., Surapureddi, S.   +4 more
core   +1 more source

GenoStaR: An R Package for Genotype to Star Allele Conversion for Major Cytochrome P450 Family of Genes. [PDF]

Clin Pharmacol Ther
Pharmacogenomics enables the personalization of drug therapy by linking genetic variations to differences in drug metabolism, efficacy, and risk of adverse reactions. Genetic polymorphisms within cytochrome P450 (CYP) genes significantly affect enzyme activity, influencing drug plasma levels, responses, and safety.
Coulter AJ, Thamilselvan M, Kennedy JL, Zai CC, Tiwari AK.   +4 more
europepmc   +2 more sources

Population pharmacokinetics of artemether–lumefantrine plus amodiaquine in patients with uncomplicated Plasmodium falciparum malaria

British Journal of Clinical Pharmacology, EarlyView.
Aims Resistance to the artemisinins and the artemisinin‐based combination therapy (ACT) partner drugs has developed in Southeast Asia, and artemisinin resistance has also emerged in eastern Africa. Triple ACTs (triple artemisinin‐based combination therapies, TACT), consisting of two partner drugs with different mechanisms of action and similar ...
Junjie Ding, Richard M. Hoglund, Rob W. van der Pluijm, James J. Callery, Thomas J. Peto, Rupam Tripura, Sukanta Das, Nguyễn Hoàng Châu, Cholrawee Promnarate, Mavuto Mukaka, Lek Dysoley, Caterina Fanello, Marie A. Onyamboko, Anupkumar R. Anvikar, Mayfong Mayxay, Frank Smithuis, Lorenz von Seidlein, Mehul Dhorda, Chanaki Amaratunga, M. Abul Faiz, Ho Dang Trung Nghia, Nicholas J. White, Nicholas P. J. Day, Arjen M. Dondorp, Joel Tarning   +24 more
wiley   +1 more source

Effect of enzalutamide on anticoagulant therapy with edoxaban in patients with prostate cancer

British Journal of Clinical Pharmacology, EarlyView.
Aims Treatment with enzalutamide in prostate cancer is challenging due to its high potential for drug–drug interactions, particularly in the typically older population of patients with frequent comorbidities treated with multiple drugs, such as anticoagulants.
Catharina J. P. Op 't Hoog, Niven Mehra, Anouk van Kleef, Diederik M. Somford, Inge M. van Oort, Alex L. T. Imholz, Paul Hamberg, Nielka P. van Erp, Emmy Boerrigter   +8 more
wiley   +1 more source

Low‐dose cannabidiol increases plasma concentrations of amitriptyline: A clinical drug–drug interaction study

British Journal of Clinical Pharmacology, EarlyView.
Abstract Aims Cannabidiol (CBD), the main non‐intoxicating compound from the cannabis plant, is regularly used by patients with chronic pain who also take analgesics. CBD has previously been shown to inhibit CYP‐mediated drug metabolism. This study aimed to characterize the potential pharmacokinetic interaction of CBD with amitriptyline and tramadol ...
Andriy A. Gorbenko, Titiaan E. Post, Pamela K. Strugala, Erica S. Klaassen, Linda E. Klumpers, Saco J. de Visser, Cristina Sempio, Jost Klawitter, Jules A. A. C. Heuberger, Geert J. Groeneveld   +9 more
wiley   +1 more source