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

By Ahcene Boumendjel, Jean Boutonnat, Jacques Robert

ISBN-10: 0470227346

ISBN-13: 9780470227343

A accomplished assessment of the most up-tp-date clinical learn on ABC transporters and multidrug resistanceATP-binding cassette transporter genes (ABC transporters) are recognized to play an important position within the improvement of multidrug resistance (MDR). MDR is the power of pathologic cells, comparable to tumors, to resist chemical substances designed to focus on and break such cells. In MDR, sufferers who're on drugs ultimately increase resistance not to in simple terms the drug they're taking, yet to a number of types of drugs.ABC Transporters and Multidrug Resistance deals a necessary source for pharmaceutical researchers who're operating to find medicines to counteract multidrug resistance in ailments similar to melanoma. in a single accomplished quantity, this publication features a number of the most up-tp-date wisdom at the involvement of ABC transporters in drug delivery and resistance.This complete quantity presents an outline at the description of the constitution, the genome, general 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. furthermore, the booklet deals crucial details at the organic and scientific point of multidrug resistance.

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Rohlff C and Glazer RI. 1998. Regulation of the MDR1 promoter by cyclic AMP-dependent protein kinase and transcription factor Sp1. Int J Oncol 12: 383–386. 31. Bargou RC, Jurchott K, Wagener C, Bergmann S, Metzner S, Bommert K et al. 1997. Nuclear localization and increased levels of transcription factor YB-1 in primary human breast cancers are associated with intrinsic MDR1 gene expression. Nat Med 3: 447–450. 32. Ogretmen B and Safa AR. 2000. Identification and characterization of the MDR1 promoter-enhancing factor 1 (MEF1) in the multidrug resistant HL60/VCR human acute myeloid leukemia cell line.

1999. Mechanism of inhibition of P-glycoprotein-mediated drug transport by protein kinase C blockers. Biochem Pharmacol 58: 1723–1733. Sachs CW, Chambers TC, and Fine RL. 1999. Differential phosphorylation of sites in the linker region of P-glycoprotein by protein kinase C isozymes alpha, betaI, betaII, gamma, delta, epsilon, eta, and zeta. Biochem Pharmacol 58: 1587–1592. Szabó K, Bakos E, Welker E, Müller M, Goodfellow HR, Higgins CF et al. 1997. Phosphorylation site mutations in the human multidrug transporter modulate its drug-stimulated ATPase activity.

The linker region also plays an important role in P-gp function. Its flexible secondary structure is sufficient for the coordinate functioning of both halves of P-gp, which are likely required for the proper interaction of the two ATP-binding sites. Both NBDs of P-gp can bind and hydrolyse ATP. There is great evidence that for efficient ATP hydrolysis, the two NBDs have to interact by forming a sandwich dimer so that the LSGGQ motif of one NBD comes into contact with the loop of the other NBD to form the nucleotide-binding pocket (66).

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


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