Human PEPT1 pharmacophore distinguishes between dipeptide transport and binding.
The results identify key features required for PEPT1 transport in contrast to most previously described pharmacophores, which are based on the inhibition of transport of a known substrate.
Amino acid ester prodrugs of the anticancer agent gemcitabine: synthesis, bioconversion, metabolic bioevasion, and hPEPT1-mediated transport.
- Xueqin Song, P. Lorenzi, C. Landowski, B. Vig, J. Hilfinger, G. Amidon
- Biology, ChemistryMolecular Pharmaceutics
- 16 March 2005
The combined results suggest that the disposition of gemcitabine following oral administration would be controlled by the rate of bioconversion following transport across the intestinal epithelial membrane and that it may be possible to modulate these characteristics by the choice of the amino acid promoiety.
A novel nucleoside prodrug-activating enzyme: substrate specificity of biphenyl hydrolase-like protein.
- Insook Kim, Xueqin Song, G. Amidon
- Biology, ChemistryMolecular Pharmaceutics
- 17 February 2004
The substrate specificity suggests that the substrate-binding pocket of BPHL has a hydrophobic acyl binding site which can accommodate the positively charged alpha-amino group, while having an alcohol leaving group binding site that can accommodate nucleoside analogues with a relatively generous spatial allowance.
Prolidase, a potential enzyme target for melanoma: design of proline-containing dipeptide-like prodrugs.
- S. Mittal, Xueqin Song, G. Amidon
- Biology, ChemistryMolecular Pharmaceutics
- 21 January 2005
Melphalan prodrugs such as prophalan-l that are cleavable by Prolidase offer the potential for enhanced selectivity by facilitating cytotoxic activity only in cells overexpressing prolidase.
Amino acids as promoieties in prodrug design and development.
- B. Vig, K. Huttunen, K. Laine, J. Rautio
- Biology, ChemistryAdvanced Drug Delivery Reviews
- 15 October 2013
Amino acid ester prodrugs of the antiviral agent 2-bromo-5,6-dichloro-1-(beta-D-ribofuranosyl)benzimidazole as potential substrates of hPEPT1 transporter.
- Xueqin Song, B. Vig, P. Lorenzi, J. Drach, L. Townsend, G. Amidon
- Biology, ChemistryJournal of Medicinal Chemistry
- 1 February 2005
Assays of competitive inhibition of [(3)H]glycylsarcosine (Gly-Sar) uptake in HeLa/hPEPT1 cells by the amino acid ester prodrugs of BDCRB suggested their 2- to 4-fold higher affinity for hPepT1 compared to BD CRB.
Assessing the risk of pH-dependent absorption for new molecular entities: a novel in vitro dissolution test, physicochemical analysis, and risk assessment strategy.
- N. Mathias, Yan Xu, K. Raghavan
- BiologyMolecular Pharmaceutics
- 26 September 2013
An API-sparing, two-stage, in vitro microdissolution test was developed to generate drug dissolution, supersaturation, and precipitation kinetic data under conditions that mimic the dynamic pH changes in the gastrointestinal tract, and the hypothesis that physicochemical properties are predictors of clinical pH-effect was explored.
Enhanced Absorption and Growth Inhibition with Amino Acid Monoester Prodrugs of Floxuridine by Targeting hPEPT1 Transporters
A series of amino acid monoester prodrugs of floxuridine was synthesized and evaluated for the improvement of oral bioavailability and the feasibility of target drug delivery via oligopeptide transporters and showed great potential for increased drug absorption and improved tumor selectivity and drug efficacy.
Application of imaging based tools for the characterisation of hollow spray dried amorphous dispersion particles.
- John F. Gamble, A. P. Ferreira, Mike Ashton
- Materials ScienceInternational journal of pharmaceutics
- 25 April 2014
Studies on the antimicrobial substances of sponges. IV. Structure of a bromine-containing compound from a marine sponge.
- G. M. Sharma, B. Vig, P. Burkholder
- ChemistryJournal of Organic Chemistry
- 1 August 1970
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