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Transcellular transport of a compound is highly dependent on a number of physiological factors, some of which is discussed in this chapter. It also discusses relative importance to overall physiology and the pharmacokinetics/ pharmacodynamics (PK/PD) of potential pharmaceutical substrates. Also, the functional roles of proton- coupled oligopeptide transporter (POT) members to drug screening and renal drug design from an industrial perspective are presented. The chapter explains about molecular and structural characteristics and functional properties of peptide transporters. Oligopeptide transporter research has predominantly been focused on delineating the functional characteristics of each transporter isoform. Factors such as diet, development phase, hormonal influences, pathological conditions and various pharmacological agents have all been demonstrated to regulate peptide transporters 1 (PepT1) expression and are also discussed. In screening compound permeation across cellular barriers, delineation of the key rate-determining steps for controlling absorption needs to be identified.