STRUCTURAL BIOLOGY AND FUNCTION OF SOLUTE TRANSPORTERS: IMPLICATIONS FOR IDENTIFYING AND DESIGNING SUBSTRATES

Solute carrier (SLC) proteins have critical physiological roles in nutrient transport and may be utilized as a mechanism to increase drug absorption. However, we have little understanding of these proteins at the molecular level due to the absence of high-resolution crystal structures. Numerous effo...

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Veröffentlicht in:Drug metabolism reviews 2002-01, Vol.34 (4), p.709-750
Hauptverfasser: Zhang, Eric Y., Knipp, Gregory T., Ekins, Sean, Swaan, Peter W.
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container_issue 4
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container_title Drug metabolism reviews
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creator Zhang, Eric Y.
Knipp, Gregory T.
Ekins, Sean
Swaan, Peter W.
description Solute carrier (SLC) proteins have critical physiological roles in nutrient transport and may be utilized as a mechanism to increase drug absorption. However, we have little understanding of these proteins at the molecular level due to the absence of high-resolution crystal structures. Numerous efforts have been made in characterizing the peptide transporter (PepT1) and the apical sodium dependent bile acid transporter (ASBT) that are important for both their native transporter function as well as targets to increase absorption and act as therapeutic targets. In vitro and computational approaches have been applied to gain some insight into these transporters with some success. This represents an opportunity for optimizing molecules as substrates for the solute transporters and providing a further screening system for drug discovery. Clearly the future growth in knowledge of SLC function will be led by integrated in vitro and in silico approaches.
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source MEDLINE; Taylor & Francis Medical Library - CRKN; Taylor & Francis Journals Complete
subjects Amino Acid Sequence - physiology
Animals
Bile acid
Biological and medical sciences
Carrier Proteins - chemical synthesis
Carrier Proteins - chemistry
Carrier Proteins - physiology
Cell physiology
Drug Design
Fundamental and applied biological sciences. Psychology
Humans
Membrane and intracellular transports
Membrane Transport Proteins - chemical synthesis
Membrane Transport Proteins - chemistry
Membrane Transport Proteins - physiology
Molecular and cellular biology
Molecular Sequence Data
P-glycoprotein
Peptide transport
Structure activity
title STRUCTURAL BIOLOGY AND FUNCTION OF SOLUTE TRANSPORTERS: IMPLICATIONS FOR IDENTIFYING AND DESIGNING SUBSTRATES
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