Caco-2 cell monolayers as a model for drug transport across the intestinal mucosa

AR Hilgers, RA Conradi, PS Burton - Pharmaceutical research, 1990 - Springer
Human colon adenocarcinoma (Caco-2) cells, when grown on semipermeable filters,
spontaneously differentiate in culture to form confluent monolayers which both structurally and …

The influence of peptide structure on transport across Caco-2 cells

RA Conradi, AR Hilgers, NFH Ho, PS Burton - Pharmaceutical research, 1991 - Springer
… PS Burton, RB Hill, and RA Conradi, Metabolism and transport of peptides across the …
AR Hilgers, RA Conradi, and PS Burton. Caco-2 cell monolayers as a model for drug transport …

How structural features influence the biomembrane permeability of peptides

PS Burton, RA Conradi, NFH Ho, AR Hilgers… - Journal of …, 1996 - Elsevier
Successful drug development requires not only optimization of specific and potent pharmacological
activity at the target site, but also efficient delivery to that site. Many promising new …

The influence of peptide structure on transport across Caco-2 cells. II. Peptide bond modification which results in improved permeability

RA Conradi, AR Hilgers, NFH Ho, PS Burton - Pharmaceutical research, 1992 - Springer
In order to study the influence of hydrogen bonding in the amide backbone of a peptide on
permeability across a cell membrane, a series of tetrapeptide analogues was prepared from D…

Predictive relationships in the water solubility of salts of a nonsteroidal anti-inflammatory drug

BD Anderson, RA Conradi - Journal of pharmaceutical sciences, 1985 - Elsevier
A number of metal and amine salts of the nonsteroidal anti-inflammatory drug 2-(2-fluoro-4-biphenylyl)propionic
acid (flurbiprofen) (1) were synthesized, and the water solubilities of …

Physicochemical determinants of passive membrane permeability: role of solute hydrogen-bonding potential and volume

JT Goodwin, RA Conradi, NFH Ho… - Journal of medicinal …, 2001 - ACS Publications
The relationship of solute structure with cellular permeability was probed. Two series of
dipeptide mimetics consisting of glycine, alanine, valine, leucine, phenylalanine, and …

Small molecule peptidomimetics containing a novel phosphotyrosine bioisostere inhibit protein tyrosine phosphatase 1B and augment insulin action

…, XY Wang, DP Thompson, RA Conradi… - Biochemistry, 2001 - ACS Publications
Protein tyrosine phosphatase 1B (PTP1B) attenuates insulin signaling by catalyzing
dephosphorylation of insulin receptors (IR) and is an attractive target of potential new drugs for …

(B) Mechanisms of peptide and protein absorption:(2) Transcellular mechanism of peptide and protein absorption: passive aspects

PS Burton, RA Conradi, AR Hilgers - Advanced drug delivery reviews, 1991 - Elsevier
A major factor contributing to the poor bioavailability of peptides and proteins after non-parenteral
administration is thought to be inefficient transport across cellular barriers. While the …

Evidence for a polarized efflux system for peptides in the apical membrane of Caco-2 cells

PS Burton, RA Conradi, AR Hilgers, NFH Ho - Biochemical and biophysical …, 1993 - Elsevier
The transport of two model peptides across confluent monolayers of human colon adenocarcinoma
(Caco-2) cells was studied. In the case of AcPhe(NMePhe) 2 NH 2 , transport in the …

Piperazinyl oxazolidinone antibacterial agents containing a pyridine, diazene, or triazene heteroaromatic ring

…, CW Ford, GE Zurenko, RA Conradi… - Journal of medicinal …, 1998 - ACS Publications
Oxazolidinones are a novel class of synthetic antibacterial agents active against gram-positive
organisms including methicillin-resistant Staphylococcus aureus as well as selected …