Complex interplay between the P-glycoprotein multidrug efflux pump and the membrane: its role in modulating protein function

FJ Sharom - Frontiers in oncology, 2014 - frontiersin.org
Multidrug resistance in cancer is linked to expression of the P-glycoprotein multidrug
transporter (Pgp, ABCB1), which exports many structurally diverse compounds from cells …

[HTML][HTML] Comparison of mechanistic transport cycle models of ABC exporters

D Szöllősi, D Rose-Sperling, UA Hellmich… - Biochimica et Biophysica …, 2018 - Elsevier
ABC (ATP binding cassette) transporters, ubiquitous in all kingdoms of life, carry out
essential substrate transport reactions across cell membranes. Their transmembrane …

Molecular docking characterizes substrate-binding sites and efflux modulation mechanisms within P-glycoprotein.

RJ Ferreira, MJU Ferreira… - Journal of chemical …, 2013 - ACS Publications
P-Glycoprotein (Pgp) is one of the best characterized ABC transporters, often involved in the
multidrug-resistance phenotype overexpressed by several cancer cell lines. Experimental …

Molecular basis of the polyspecificity of P-glycoprotein (ABCB1): recent biochemical and structural studies

EE Chufan, HM Sim, SV Ambudkar - Advances in cancer research, 2015 - Elsevier
Abstract ABCB1 (P-glycoprotein/P-gp) is an ATP-binding cassette transporter well known for
its association with multidrug resistance in cancer cells. Powered by the hydrolysis of ATP, it …

Structure–activity relationships, ligand efficiency, and lipophilic efficiency profiles of benzophenone-type inhibitors of the multidrug transporter P-glycoprotein

I Jabeen, K Pleban, U Rinner, P Chiba… - Journal of medicinal …, 2012 - ACS Publications
The drug efflux pump P-glycoprotein (P-gp) has been shown to promote multidrug
resistance (MDR) in tumors as well as to influence ADME properties of drug candidates …

Ligand and structure-based classification models for prediction of P-glycoprotein inhibitors

F Klepsch, P Vasanthanathan… - Journal of chemical …, 2014 - ACS Publications
The ABC transporter P-glycoprotein (P-gp) actively transports a wide range of drugs and
toxins out of cells, and is therefore related to multidrug resistance and the ADME profile of …

The role of the degenerate nucleotide binding site in type I ABC exporters

T Stockner, R Gradisch, L Schmitt - FEBS letters, 2020 - Wiley Online Library
ATP‐binding cassette (ABC) transporters are fascinating molecular machines that are
capable of transporting a large variety of chemically diverse compounds. The energy …

ATP-dependent substrate transport by the ABC transporter MsbA is proton-coupled

H Singh, S Velamakanni, MJ Deery, J Howard… - Nature …, 2016 - nature.com
ATP-binding cassette transporters mediate the transbilayer movement of a vast number of
substrates in or out of cells in organisms ranging from bacteria to humans. Current …

Exhaustive sampling of docking poses reveals binding hypotheses for propafenone type inhibitors of P-glycoprotein

F Klepsch, P Chiba, GF Ecker - PLoS computational biology, 2011 - journals.plos.org
Overexpression of the xenotoxin transporter P-glycoprotein (P-gp) represents one major
reason for the development of multidrug resistance (MDR), leading to the failure of antibiotic …

Naphthoquinone derivatives as P-glycoprotein inducers in inflammatory bowel disease: 2D monolayers, 3D spheroids, and in vivo models

N Mahmoud, MEF Hegazy, W Wadie… - Pharmacological …, 2022 - Elsevier
Inflammatory bowel disease (IBD) represents a chronic inflammation of the gastrointestinal
tract characterized by an overreaction of immune responses and damage at the intestinal …