TAILIEUCHUNG - Báo cáo khoa học: Multidrug efflux pumps: drug binding – gates or cavity? Emily Crowley and Richard Callaghan

The role of the ATP-binding cassette ABCB1 in mediating the resistance to chemotherapy in many forms of cancer has been well established. The pro-tein is also endogenously expressed in numerous barrier and excretory tissues, thereby regulating or impacting on drug pharmacokinetic profiles. | MINIREVIEW Multidrug efflux pumps drug binding - gates or cavity Emily Crowley and Richard Callaghan Nuffield Department of ClinicalLaboratory Sciences University of Oxford UK Keywords central cavity coupling domain interface drug binding drug resistance drug transport interdomain communication membrane protein multidrug binding P-glycoprotein Correspondence R. Callaghan Nuffield Department of Clinical Laboratory Sciences University of Oxford Level4 Academic Block John Radcliffe Hospital Headley Way Oxford OX3 9DU UK Fax 44 1865 221 834 Tel 44 1865 221110 E-mail Received 22 July 2009 revised 1 October 2009 accepted 5 November 2009 The role of the ATP-binding cassette ABCB1 in mediating the resistance to chemotherapy in many forms of cancer has been well established. The protein is also endogenously expressed in numerous barrier and excretory tissues thereby regulating or impacting on drug pharmacokinetic profiles. Given these prominent roles in health and disease a great deal of biochemical structural and pharmacological research has been directed towards modulating its activity. Despite the effort only a small handful of compounds have reached the later stages of clinical trials. What is responsible for this poor return on the heavy research investment Perhaps the most significant factor is the lack of information on the location physical features and chemical properties of the drug-binding site s in ABCB1. This minireview outlines the various strategies and outcomes of research efforts to pin-point the sites of interaction. The data may be assimilated into two working hypotheses to describe drug binding to ABCB1 a the central cavity and the b domain interface models. doi Properties of drug-binding sites in abCbi P-Glycoprotein also known as ABCB1 mdr1 has long been associated with drug resistance in many cancer types. This protein is a member of the ATP-binding cassette ABC family and is believed .

• Báo cáo khoa học
• Scientific reports
• scientific research
• biochemistry
• drug binding
• hemoglobin
• hormone medicine
• collection of scientific reports
• industry reports philosophy of history reports
• reports in literature
• a scientific b shirt
• presentation of scientific reports
• reports on literature
• philosophy statement
• documents
• studies English language and English language communication and English language commercial
• progress reports at scientific collections
• agronomic reports
• reports in physics
• biology reports
• thematic biological
• induced geometry
• mathematical topics
• quantum mechanics
• physics
• reporting mathematics
• physics reports
• livestock reports
• physical reports
• research physicist
• specializing in physics
• mathematical statements
• mathematical equations
• English pronunciation
• presentation report
• agricultural reports
• technical crops
• bio technology
• English reports
• presentation reports
• mathematical knowledge
• reports of mathematics
• represented
• Wilf on packing distinct
• Tur´n density
• mathematical works
• patterns in a permutation
• statements and documents scientific reports
• reports agronomy
• biotechnology
• plants Vietnam
• specialized biological
• microbiological methods
• presenting the report
• anti bacterial properties of shrimp
• energy exchange
• engineering chicken
• Path counting
• random matrix theory
• Even circuits
• prescribed clockwise parity
• Correspondence between
• algorithmic characterizations
• Finding Induced Acyclic
• Random Digraphs
• Nonexistence results
• Hadamard like matrices
• Voltage Graphs
• Group Presentations
• Cages mathematical knowledge
• Dominance Order
• Graphical Partitions
• On the functions
• values in [α(G
• Box With Translates
• Two Given Rectangular Brick
• On the q analogue
• the sum of cubes