Pharmaceutical and pharmacological importance of peptide transporters

M Brandsch, I Knütter… - Journal of Pharmacy …, 2008 - Wiley Online Library
Peptide transport is currently a prominent topic in membrane research. The transport
proteins involved are under intense investigation because of their physiological importance …

Intestinal solute carriers: an overview of trends and strategies for improving oral drug absorption

B Steffansen, CU Nielsen, B Brodin, AH Eriksson… - European journal of …, 2004 - Elsevier
A large amount of absorptive intestinal membrane transporters play an important part in
absorption and distribution of several nutrients, drugs and prodrugs. The present paper …

Prodrugs of nucleoside analogues for improved oral absorption and tissue targeting

F Li, H Maag, T Alfredson - Journal of pharmaceutical sciences, 2008 - Elsevier
Nucleoside analogues are widely used for the treatment of antiviral infections and
anticancer chemotherapy. However, many nucleoside analogues suffer from poor oral …

Intestinal barrier dysfunction: implications for chronic inflammatory conditions of the bowel

WM Miner-Williams, PJ Moughan - Nutrition research reviews, 2016 - cambridge.org
The intestinal epithelium of adult humans acts as a differentially permeable barrier that
separates the potentially harmful contents of the lumen from the underlying tissues. Any …

Human PEPT1 pharmacophore distinguishes between dipeptide transport and binding

BS Vig, TR Stouch, JK Timoszyk, Y Quan… - Journal of Medicinal …, 2006 - ACS Publications
The human intestinal oligopeptide transporter (PEPT1) facilitates the absorption of
dipeptides, tripeptides, and many peptidomimetic drugs. In this study, a large number of …

The intestinal H+/peptide symporter PEPT1: structure–affinity relationships

M Brandsch, I Knütter, FH Leibach - European journal of pharmaceutical …, 2004 - Elsevier
Peptide transporter 1, PEPT1, of the mammalian enterocyte is presently under intense
investigation in many laboratories because of its nutritional importance in the absorption of …

Amino acid ester prodrugs of the anticancer agent gemcitabine: synthesis, bioconversion, metabolic bioevasion, and hPEPT1-mediated transport

X Song, PL Lorenzi, CP Landowski, BS Vig… - Molecular …, 2005 - ACS Publications
Gemcitabine, a clinically effective nucleoside anticancer agent, is a polar drug with low
membrane permeability and is administered intravenously. Further, extensive degradation of …

Amino Acid Ester Prodrugs of the Antiviral Agent 2-Bromo-5,6-dichloro-1-(β-d-ribofuranosyl)benzimidazole as Potential Substrates of hPEPT1 Transporter

X Song, BS Vig, PL Lorenzi, JC Drach… - Journal of medicinal …, 2005 - ACS Publications
Amino acid ester prodrugs of 2-bromo-5, 6-dichloro-1-(β-d-ribofuranosyl) benzimidazole
(BDCRB) were synthesized and evaluated for their affinity for hPEPT1, an intestinal …

Chemical properties of antimicrobials and their uniqueness

MJ Macielag - Antibiotic discovery and development, 2011 - Springer
Antibacterial drug discovery has benefitted from the availability of a large number of genome
sequences for target selection and new assay formats for inhibitor identification. Until …

Modeling kinetics of subcellular disposition of chemicals

S Balaz - Chemical Reviews, 2009 - ACS Publications
The effects of low-molecular-weight (< 1000 g/mol) chemicals on biosystems ranging from
membranes to organisms are of interest in medicinal chemistry, chemical biology …