2-Aminopyridine Analogs Inhibit Both Enzymes of the Glyoxylate Shunt in Pseudomonas aeruginosa

Autor: Mahmud Kajbaf, Päivi Tammela, Viviana Gatta, David R. Spring, Sean Bartlett, Alyssa C. McVey, Annalisa Pellacani, Martin Welch

Publikováno v: International Journal of Molecular Sciences, Vol 21, Iss 2490, p 2490 (2020)
International Journal of Molecular Sciences
Volume 21
Issue 7

Pseudomonas aeruginosa is an opportunistic pathogen responsible for many hospital-acquired infections. P. aeruginosa can thrive in diverse infection scenarios by rewiring its central metabolism. An example of this is the production of biomass from C2

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c65cf324330ec4e0b61e98b2a3f0f379
http://hdl.handle.net/10138/317973

1,2,4-Triazolyl 5-Azaspiro[2.4]heptanes: Lead Identification and Early Lead Optimization of a New Series of Potent and Selective Dopamine D3 Receptor Antagonists

Autor: Aldo Feriani, Laura Zonzini, Laura Castelletti, Selena Nola, Michele Dal Cin, Teresa Semeraro, Sylvie Gehanne, Silvia Tomelleri, Filippo Visentini, Palmina Cavallini, Susanna Cremonesi, Annalisa Pellacani, Anna Sava, Alessia Bacchi, Andrea Wong, Simone Braggio, Luca Tarsi, Mahmud Kajbaf, Paolo Cavanni, Elisabetta Perdona, Christian Heidbreder, Luciano Marchiò, Beatrice Oliosi, Fabrizio Micheli

Publikováno v: Journal of Medicinal Chemistry. 59:8549-8576

A novel series of 1,2,4-triazolyl 5-azaspiro[2.4]heptanes with high affinity and selectivity at the dopamine (DA) D3 receptor (D3R) is described. Some of these compounds also have high selectivity over the hERG channel and were characterized with res

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3e92639ff81d14ff2d424ab7f16b988a
https://doi.org/10.1021/acs.jmedchem.6b00972

Evaluation of Cytochrome P450 Inhibition Assays Using Human Liver Microsomes by a Cassette Analysis /LC-MS/MS

Autor: Stefano Fontana, Mahmud Kajbaf, Serenella Zambon

Publikováno v: Drug Metabolism Letters. 4:120-128

In vitro inhibition assays are used to screen new chemical entities (NCEs) for inhibition studies by using human liver microsomes. High-throughput inhibition assays using pooling methods have been developed to keep pace with screening requirements at

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1c9d3c396f4292dfc04b63b042a7a024
https://doi.org/10.2174/187231210791698483

Development of a Rapid and Cost Effective Assay for the Screening of Reversible Cytochrome P450 Inhibition in Parallel with Cyp3a4 Metabolism-Dependent Inhibition Using Recombinant Proteins

Autor: Mahmud Kajbaf, Stefano Fontana, Raffaele Longhi, Serenella Zambon

Publikováno v: Pharmaceutica Analytica Acta.

In the present study we have developed a high quality, rapid and cost effective CYP450 inhibition assay that does have the ability to detect both reversible and CYP3A4 metabolism-dependent inhibition (MDI), using recombinantly expressed P450 isoforms

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::74bf030f87e1363e01edcedd71e10c20
https://doi.org/10.4172/2153-2435.1000389

Contribution of rat intestinal metabolism to the xenobiotics clearance

Autor: Serenella Zambon, Mahmud Kajbaf, Stefano Fontana, Raffaella Ricci

Publikováno v: European journal of drug metabolism and pharmacokinetics. 38(1)

Michaelis–Menten constants K m and V max values were determined by product formation and substrate depletion at several substrate concentrations of 4-methylumbelliferone using rat intestinal microsomes. K m and V max values determined by measuring

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ff2c0c47473c216796c8c6c400fe984c
https://pubmed.ncbi.nlm.nih.gov/22714869