Communication between Multiple Drug Binding Sites on P-glycoprotein

2000 ◽  
Vol 58 (3) ◽  
pp. 624-632 ◽  
Author(s):  
Catherine Martin ◽  
Georgina Berridge ◽  
Christopher F. Higgins ◽  
Prakash Mistry ◽  
Peter Charlton ◽  
...  
Keyword(s):  
Binding Sites ◽  
Drug Binding ◽  
Multiple Drug ◽  
P Glycoprotein ◽  
Drug Binding Sites

scholarly journals Systematic exploration of multiple drug binding sites

2017 ◽  
Vol 9 (1) ◽  
Author(s):  
Mónika Bálint ◽  
Norbert Jeszenői ◽  
István Horváth ◽  
David van der Spoel ◽  
Csaba Hetényi
Keyword(s):  
Binding Sites ◽  
Drug Binding ◽  
Multiple Drug ◽  
Systematic Exploration ◽  
Drug Binding Sites

scholarly journals Atomic modelling and systematic mutagenesis identify residues in multiple drug binding sites that are essential for drug resistance in the major Candida transporter Cdr1

2016 ◽  
Vol 1858 (11) ◽  
pp. 2858-2870 ◽  
Author(s):  
Shweta Nim ◽  
Lucia Gonzalez Lobato ◽  
Alexis Moreno ◽  
Vincent Chaptal ◽  
Manpreet Kaur Rawal ◽  
...  
Keyword(s):  
Drug Resistance ◽  
Binding Sites ◽  
Drug Binding ◽  
Multiple Drug ◽  
Drug Binding Sites

scholarly journals Novel features in the structure of P-glycoprotein (ABCB1) in the post-hydrolytic state as determined at 7.9Å resolution

2018 ◽  
Author(s):  
Nopnithi Thonghin ◽  
Richard F. Collins ◽  
Alessandro Barbieri ◽  
Talha Shafi ◽  
Alistair Siebert ◽  
...  
Keyword(s):  
Binding Sites ◽  
Drug Binding ◽  
Multi Drug Resistance ◽  
Binding Domains ◽  
Atp Binding Cassette Transporter ◽  
P Glycoprotein ◽  
Head Groups ◽  
Related Drug ◽  
Drug Binding Sites

AbstractP-glycoprotein (ABCB1) is a ATP-binding cassette transporter that plays an important role in the removal of drugs and xenobiotic compounds from the cell. It is also associated with multi-drug resistance in cancer. Here we report novel features of the cryo-EM-derived structure of P-glycoprotein in the post-hydrolytic state: The cytosolic nucleotide-binding domains (NBDs) are separated despite ADP remaining bound to the NBDs. Gaps in the TMDs that connect to the inner hydrophilic cavity are back-filled by detergent head-groups from the annular detergent micelle and are close to two regions predicted to delineate two pseudo-symmetry-related drug-binding sites. In this conformation, the (newly-resolved) N-terminal extension, NBD-TMD linker region and gap-filling detergents all appear to impede NBD dimerisation. We propose a model for the mechanism of action of the exporter where ATP will be bound to the protein for most of the time, consistent with the high physiological ATP concentrationsin vivo.

A New Paclitaxel Photoaffinity Analog with a 3-(4-Benzoylphenyl)propanoyl Probe for Characterization of Drug-Binding Sites on Tubulin and P-Glycoprotein

1995 ◽  
Vol 38 (20) ◽  
pp. 3891-3894 ◽  
Author(s):  
Iwao Ojima ◽  
Olivier Duclos ◽  
Gyorgy Dorman ◽  
Bruno Simonot ◽  
Glenn D. Prestwich ◽  
...  
Keyword(s):  
Binding Sites ◽  
Drug Binding ◽  
P Glycoprotein ◽  
Drug Binding Sites

Drug Binding Sites on P-Glycoprotein Are Altered by ATP Binding Prior to Nucleotide Hydrolysis†

Biochemistry ◽  
2000 ◽  
Vol 39 (39) ◽  
pp. 11901-11906 ◽  
Author(s):  
Catherine Martin ◽  
Georgina Berridge ◽  
Prakash Mistry ◽  
Christopher Higgins ◽  
Peter Charlton ◽  
...  
Keyword(s):  
Binding Sites ◽  
Drug Binding ◽  
Atp Binding ◽  
Nucleotide Hydrolysis ◽  
P Glycoprotein ◽  
Drug Binding Sites
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