TY - JOUR
T1 - The renal type H+/peptide symporter PEPT2
T2 - Structure-affinity relationships
AU - Biegel, A.
AU - Knütter, I.
AU - Hartrodt, B.
AU - Gebauer, S.
AU - Theis, S.
AU - Luckner, P.
AU - Kottra, G.
AU - Rastetter, M.
AU - Zebisch, K.
AU - Thondorf, I.
AU - Daniel, H.
AU - Neubert, K.
AU - Brandsch, M.
PY - 2006/8
Y1 - 2006/8
N2 - The H+/peptide cotransporter PEPT2 is expressed in a variety of organs including kidney, lung, brain, mammary gland, and eye. PEPT2 substrates are di- and tripeptides as well as peptidomimetics, such as β-lactam antibiotics. Due to the presence of PEPT2 at the bronchial epithelium, the aerosolic administration of peptide-like drugs might play a major role in future treatment of various pulmonary and systemic diseases. Moreover, PEPT2 has a significant influence on the in vivo disposition and half-life time of peptide-like drugs within the body, particularly in kidney and brain. PEPT2 is known to have similar but not identical structural requirements for substrate recognition and transport compared to PEPT1, its intestinal counterpart. In this review we compiled available affinity constants of 352 compounds, measured at different mammalian tissues and expression systems and compare the data whenever possible with those of PEPT1.
AB - The H+/peptide cotransporter PEPT2 is expressed in a variety of organs including kidney, lung, brain, mammary gland, and eye. PEPT2 substrates are di- and tripeptides as well as peptidomimetics, such as β-lactam antibiotics. Due to the presence of PEPT2 at the bronchial epithelium, the aerosolic administration of peptide-like drugs might play a major role in future treatment of various pulmonary and systemic diseases. Moreover, PEPT2 has a significant influence on the in vivo disposition and half-life time of peptide-like drugs within the body, particularly in kidney and brain. PEPT2 is known to have similar but not identical structural requirements for substrate recognition and transport compared to PEPT1, its intestinal counterpart. In this review we compiled available affinity constants of 352 compounds, measured at different mammalian tissues and expression systems and compare the data whenever possible with those of PEPT1.
KW - Dipeptides
KW - Drug-delivery
KW - Drugs
KW - PEPT1
KW - PEPT2
KW - Peptide transport
KW - Peptidomimetics
KW - Tripeptides
KW - β-Lactam antibiotics
UR - http://www.scopus.com/inward/record.url?scp=33745807413&partnerID=8YFLogxK
U2 - 10.1007/s00726-006-0331-0
DO - 10.1007/s00726-006-0331-0
M3 - Article
C2 - 16868651
AN - SCOPUS:33745807413
SN - 0939-4451
VL - 31
SP - 137
EP - 156
JO - Amino Acids
JF - Amino Acids
IS - 2
ER -