Substrate transport genes

Transporter (gene) Substrate Km (pmol/l) Distribution Function... 

For other efflux transporters such as BCRP (ABCG2), human pharmacokinetic and pharmacodynamic data are currently rare. However, an investigation of the influence of polymorphisms in ABC-transporter genes on the accumulation of nelfinavir in peripheral blood mononuclear cells (PBMCs) revealed no associations between the polymorphisms in the transporters analyzed and the accumulation of nelfinavir in the PBMCs [151], A second study in patients clearly demonstrated an increase in the AUC of the orally and intravenously administered BCRP substrate topotecan when it is given with GF120918, an inhibitor of P-glycoprotein and BCRP [152],... 

Molecular complexation is a precondition for receptor functions such as substrate selection, substrate transportation, isomeric differentiation, and stereoselective catalysis. Although the investigation of such functions with synthetically derived compounds is a relatively new development in chemistry, they are well known and extensively studied functions in the biological domain. Evolution, gene expression, cell division, DNA replication, protein synthesis, immunological response, hormonal control, ion transportation, and enzymic catalysis are only some of the many examples where molecular complexation is a prerequisite for observing a biological process. 

Transporter Gene name Specificity Substrates Cellular localization... 

Vasudevan G, Ullman B, Landfear SM. 2001. Point mutations in a nucleoside transporter gene from Leishmania dono-vani confer drug resistance and alter substrate selectivity. Proc. Natl. Acad. Sci. USA 98 6092-97... 

Transporter Gene symbol Chromosome Reference accession (m RN A) Amino acids Transmembrane domains Tissue distribution Cellular localization Substrates... 

Transporters genes encode proteins, generally constituted by 12 transmembrane spanning regions. These mediated Na+ or H+ dependent accumulation of small molecules such as neurotransmitters, antibiotics, ions and cationic amino-acid transporters into the cells or organelles. The transport is performed by different mechanisms uniport, substrate-ion sym-port, substrate-ion antiport, substrate-substrate or ion-ion antiport, and ATP-dependent translocation. 

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