TY - JOUR
T1 - Inhibitors of multidrug resistance (MDR) have affinity for MDR substrates
AU - Zloh, Mire
AU - Kaatz, G.W.
AU - Gibbons, S.
N1 - MEDLINE® is the source for the MeSH terms of this document.
PY - 2004/2/23
Y1 - 2004/2/23
N2 - Multidrug-resistance (MDR) occurs in many bacterial species and tumour cells. MDR functions by membrane proteins which export drugs from cells, resulting in a low ineffective concentration of the drug. We have shown by molecular modelling that inhibitors of MDR have affinity for substrates of MDR transporters. This affinity may facilitate drug entry into cells and a large inhibitor-drug complex may be a poorer substrate for the MDR mechanism. This complex would effectively 'cloak' the drug rendering it unavailable for efflux.
AB - Multidrug-resistance (MDR) occurs in many bacterial species and tumour cells. MDR functions by membrane proteins which export drugs from cells, resulting in a low ineffective concentration of the drug. We have shown by molecular modelling that inhibitors of MDR have affinity for substrates of MDR transporters. This affinity may facilitate drug entry into cells and a large inhibitor-drug complex may be a poorer substrate for the MDR mechanism. This complex would effectively 'cloak' the drug rendering it unavailable for efflux.
UR - http://www.scopus.com/inward/record.url?scp=0842302984&partnerID=8YFLogxK
U2 - 10.1016/j.bmcl.2003.12.015
DO - 10.1016/j.bmcl.2003.12.015
M3 - Article
AN - SCOPUS:0842302984
SN - 0960-894X
VL - 14
SP - 881
EP - 885
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
IS - 4
ER -