Literature DB >> 24900460

Ligand Promiscuity between the Efflux Pumps Human P-Glycoprotein and S. aureus NorA.

Jean Pierre Brincat1, Fabio Broccatelli1, Stefano Sabatini1, Maria Frosini2, Annalisa Neri2, Glenn W Kaatz3, Gabriele Cruciani1, Emanuele Carosati1.   

Abstract

Thirty-two diverse compounds were evaluated for their ability to inhibit both Pgp-mediated efflux in mouse T-lymphoma L5178 MDR1 and NorA-mediated efflux in S. aureus SA-1199B. Only four compounds were strong inhibitors of both efflux pumps. Three compounds were found to inhibit Pgp exclusively and strongly, while seven compounds inhibited only NorA. These results demonstrate that Pgp and NorA inhibitors do not necessarily overlap, opening the way to safer therapeutic use of effective NorA inhibitors.

Entities:  

Keywords:  Multiple drug resistance; NorA; P-glycoprotein; S. aureus; efflux pump inhibitor; promiscuous activity

Year:  2012        PMID： 24900460      PMCID： PMC4025771          DOI： 10.1021/ml200293c

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  29 in total

1.  VolSurf: a new tool for the pharmacokinetic optimization of lead compounds.

Authors:  G Cruciani; M Pastor; W Guba
Journal:  Eur J Pharm Sci       Date:  2000-10       Impact factor: 4.384

2.  From 6-aminoquinolone antibacterials to 6-amino-7-thiopyranopyridinylquinolone ethyl esters as inhibitors of Staphylococcus aureus multidrug efflux pumps.

Authors:  Marco Pieroni; Mirjana Dimovska; Jean Pierre Brincat; Stefano Sabatini; Emanuele Carosati; Serena Massari; Glenn W Kaatz; Arnaldo Fravolini
Journal:  J Med Chem       Date:  2010-06-10       Impact factor: 7.446

3.  Transporter-mediated Efflux Influences CNS Side Effects: ABCB1, from Antitarget to Target.

Authors:  Fabio Broccatelli; Emanuele Carosati; Gabriele Cruciani; Tudor I Oprea
Journal:  Mol Inform       Date:  2010-01-12       Impact factor: 3.353

4.  Passive permeability and P-glycoprotein-mediated efflux differentiate central nervous system (CNS) and non-CNS marketed drugs.

Authors:  Kelly M Mahar Doan; Joan E Humphreys; Lindsey O Webster; Stephen A Wring; Larry J Shampine; Cosette J Serabjit-Singh; Kimberly K Adkison; Joseph W Polli
Journal:  J Pharmacol Exp Ther       Date:  2002-12       Impact factor: 4.030

5.  Use of a genetic approach to evaluate the consequences of inhibition of efflux pumps in Pseudomonas aeruginosa.

Authors:  O Lomovskaya; A Lee; K Hoshino; H Ishida; A Mistry; M S Warren; E Boyer; S Chamberland; V J Lee
Journal:  Antimicrob Agents Chemother       Date:  1999-06       Impact factor: 5.191

6.  Inhibitory potencies of 1,4-dihydropyridine calcium antagonists to P-glycoprotein-mediated transport: comparison with the effects on CYP3A4.

Authors:  M Katoh; M Nakajima; H Yamazaki; T Yokoi
Journal:  Pharm Res       Date:  2000-10       Impact factor: 4.200

7.  Discovery of novel inhibitors of the NorA multidrug transporter of Staphylococcus aureus.

Authors:  Jean Pierre Brincat; Emanuele Carosati; Stefano Sabatini; Giuseppe Manfroni; Arnaldo Fravolini; Jose L Raygada; Diixa Patel; Glenn W Kaatz; Gabriele Cruciani
Journal:  J Med Chem       Date:  2010-12-08       Impact factor: 7.446

8.  From phenothiazine to 3-phenyl-1,4-benzothiazine derivatives as inhibitors of the Staphylococcus aureus NorA multidrug efflux pump.

Authors:  Stefano Sabatini; Glenn W Kaatz; Gian Maria Rossolini; David Brandini; Arnaldo Fravolini
Journal:  J Med Chem       Date:  2008-06-25       Impact factor: 7.446

9.  A novel inhibitor of multidrug efflux pumps in Staphylococcus aureus.

Authors:  Simon Gibbons; Moyosoluwa Oluwatuyi; Glenn W Kaatz
Journal:  J Antimicrob Chemother       Date:  2003-01       Impact factor: 5.790

10.  Effects of NorA inhibitors on in vitro antibacterial activities and postantibiotic effects of levofloxacin, ciprofloxacin, and norfloxacin in genetically related strains of Staphylococcus aureus.

Authors:  J R Aeschlimann; L D Dresser; G W Kaatz; M J Rybak
Journal:  Antimicrob Agents Chemother       Date:  1999-02       Impact factor: 5.191
View more
  1 in total

1.  Chalcone Derivatives as Potential Inhibitors of P-Glycoprotein and NorA: An In Silico and In Vitro Study.

Authors:  Minh-Tri Le; Dieu-Thuong Thi Trinh; Trieu-Du Ngo; Viet-Khoa Tran-Nguyen; Dac-Nhan Nguyen; Tung Hoang; Hoang-Minh Nguyen; Tran-Giang-Son Do; Tan Thanh Mai; Thanh-Dao Tran; Khac-Minh Thai
Journal:  Biomed Res Int       Date:  2022-03-26       Impact factor: 3.411
  1 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.