ABC Transporters and Multidrug Resistance (Wiley Series in by Ahcene Boumendjel, Jean Boutonnat, Jacques Robert

By Ahcene Boumendjel, Jean Boutonnat, Jacques Robert

A complete evaluate of the most up-tp-date clinical learn on ABC transporters and multidrug resistanceATP-binding cassette transporter genes (ABC transporters) are identified to play a very important position within the improvement of multidrug resistance (MDR). MDR is the power of pathologic cells, akin to tumors, to resist chemical substances designed to focus on and break such cells. In MDR, sufferers who're on medicine ultimately boost resistance not to in basic terms the drug they're taking, yet to numerous types of drugs.ABC Transporters and Multidrug Resistance deals a vital source for pharmaceutical researchers who're operating to find medicinal drugs to counteract multidrug resistance in illnesses comparable to melanoma. in a single complete quantity, this publication encompasses a selection of the most up-tp-date wisdom at the involvement of ABC transporters in drug delivery and resistance.This accomplished quantity offers an outline at the description of the constitution, the genome, basic tissue expression, physiological point, and mechanism of motion of the ABC protein. The specialist participants discover the expression, detection, and implications of ABC proteins in hematological malignancies and reliable tumors and ABC proteins and pathogenic microorganisms. This quantity additionally explains MDR modulation via inhibition of ABC transporters and the layout of inhibitors and mechanism of motion. moreover, the e-book deals crucial details at the organic and medical element of multidrug resistance.

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Inhibition of N-linked glycosylation of P-glycoprotein by tunicamycin results in a reduced multidrug resistance phenotype. Br J Cancer 71: 670–675. 85. Zhang Z, Wu JY, Hait WN, and Yang JM. 2004. Regulation of the stability of P-glycoprotein by ubiquitination. Mol Pharmacol 66: 395–403. 86. Gribar JJ, Ramachandra M, Hrycyna CA, Dey S, and Ambudkar SV. 2000. Functional characterization of glycosylation-deficient human P-glycoprotein using a vaccinia virus expression system. J Membr Biol 173: 203–214.

Thus, P-gp activity is particularly sensitive to its lipid environment. In some cases, P-gp appears to be within specialized raft-like membrane microdomains, where its ATPase activity is five times higher than in crude membranes (159, 160). These observations remain controversial (161). More generally, P-gp retains its function in liquid-ordered cholesterol and sphingolipid model membranes, and P-gp activity requires a microenvironment of raft microdomains or intermediate-density domains (162, 163).

Biochem Biophys Res Commun 368: 930–936. 102. de Grouw EP, Raaijmakers MH, Boezeman JB, van der Reijden BA, Van de Locht LT, and de Witte TJ. 2006. Preferential expression of a high number of ATP binding cassette transporters in both normal and leukemic CD34 + CD38- cells. Leukemia 20: 750–754. 103. Chaudhary PM and Roninson IB. 1991. Expression and activity of P-glycoprotein, a multidrug efflux pump, in human hematopoietic stem cells. Cell 66: 85–94. 104. Dean M, Fojo T, and Bates S. 2005. Tumour stem cells and drug resistance.

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