Now showing items 1-10 of 70
Design, synthesis and evaluation against Mycobacterium tuberculosis of azole piperazine derivatives as dicyclotyrosine (cYY) mimics
Three series of azole piperazine derivatives that mimic dicyclotyrosine (cYY), the natural substrate of the essential Mycobacterium tuberculosis cytochrome P450 CYP121A1, were prepared and evaluated for binding affinity ...
Fragment-Based Approaches to the Development of Mycobacterium tuberculosis CYP121 Inhibitors
The essential enzyme CYP121 is a target for drug development against antibiotic resistant strains of Mycobacterium tuberculosis. A triazol-1-yl phenol fragment 1 was identified to bind to CYP121 using a cascade of biophysical ...
QM/MM study of the C-C coupling reaction mechanism of CYP121, an essential Cytochrome p450 of Mycobacterium tuberculosis
Among 20 p450s of Mycobacterium tuberculosis (Mt), CYP121 has received an outstanding interest, not only due to its essentiality for bacterial viability but also because it catalyzes an unusual carbon-carbon coupling ...
Análise do polimorfismo do gene CYP 17 como fator relacionado ao desenvolvimento do leiomioma uterino
(Universidade Federal de São Paulo (UNIFESP), 2009-09-24)
Objective: Uterine leiomyoma is the most common pelvic tumor in women of reproductive age. It has been well established that endogenous sex hormones are involved in the pathogenesis of the disease, and polymorphisms in ...
Food consumption, cytochrome P450 3A4 (CYP3A4) presystemic inhibitors, and bioavailability of saquinavir
(Sociedad Española de Farmacia Hospitalaria (SEFH)ElsevierPromoción y Prevención FarmacéuticaMadrid, España, 2021)
Novel Aryl Substituted Pyrazoles as Small Molecule Inhibitors of Cytochrome P450 CYP121A1: Synthesis and Antimycobacterial Evaluation
Three series of biarylpyrazole imidazole and triazoles are described, which vary in the linker between the biaryl pyrazole and imidazole/triazole group. The imidazole and triazole series with the short -CH2- linker displayed ...
First clinical isolation of an azole-resistant aspergillus fumigatus isolate harboring a TR46 Y121F T289A mutation in South America
(American Society for Microbiology, 2018-10)
One of the most recently described Aspergillus fumigatus CYP51Amediated azole resistance mechanisms is TR46 Y121F T289A. Clinical A. fumigatus strains harboring these substitutions have been reported worldwide, with the ...
Human breast tumor slices: A model for identification of vitamin D regulated genes in the tumor microenvironment
(PERGAMON-ELSEVIER SCIENCE LTD, 2010)
While many studies have addressed the direct effects of 1 alpha,25(OH)(2)D(3) on breast cancer (BC) cells, stromal-epithelial interactions, which are important for the tumor development, have been largely ignored. In ...
Fenotipos metabólicos de CYP2D6 relacionados a efectos adversos y falla terapéutica en pacientes colombianos tratados con tramadol
Introduction: Tramadol is a medication commonly used in clinical practice for the management of moderate to severe pain; This is a prodrug that needs to be metabolized by CYP2D6, to generate its active metabolite ...