User profiles for Thomas J. Raub

Thomas J Raub

Retired
Verified email at iu.edu
Cited by 8460

Characterization of the human colon carcinoma cell line (Caco-2) as a model system for intestinal epithelial permeability

IJ Hidalgo, TJ Raub, RT Borchardt - Gastroenterology, 1989 - Elsevier
Caco-2 cells develop morphologic characteristics of normal enterocytes when grown on plastic
dishes or nitrocellulose filters. The purpose of this study was to determine whether Caco-…

Quantitative approaches to delineate paracellular diffusion in cultured epithelial cell monolayers

A Adson, TJ Raub, PS Burton, CL Barsuhn… - Journal of …, 1994 - Elsevier
When using cultured cell monolayers to determine the mechanism of transcellular diffusion
of molecules, it may be important to identify the fraction that moves through the paracellular …

Brain exposure of two selective dual CDK4 and CDK6 inhibitors and the antitumor activity of CDK4 and CDK6 inhibition in combination with temozolomide in an …

TJ Raub, GN Wishart, P Kulanthaivel, BA Staton… - Drug Metabolism and …, 2015 - ASPET
Effective treatments for primary brain tumors and brain metastases represent a major unmet
medical need. Targeting the CDK4/CDK6-cyclin D1-Rb-p16/ink4a pathway using a potent …

P-glycoprotein recognition of substrates and circumvention through rational drug design

TJ Raub - Molecular pharmaceutics, 2006 - ACS Publications
It is now well recognized that membrane efflux transporters, especially P-glycoprotein (P-gp;
ABCB1), play a role in determining the absorption, distribution, metabolism, excretion, and …

Discovery of N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide, an Agonist of the α7 Nicotinic Acetylcholine Receptor, for the Potential Treatment …

…, EHF Wong, BA Staton, TJ Raub… - Journal of medicinal …, 2006 - ACS Publications
N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide (14, PHA-543,613), a
novel agonist of the α7 neuronal nicotinic acetylcholine receptor (α7 nAChR), has been …

Determination of the affinity of drugs toward serum albumin by measurement of the quenching of the intrinsic tryptophan fluorescence of the protein

DE Epps, TJ Raub, V Caiolfa, A Chiari… - Journal of Pharmacy …, 1999 - academic.oup.com
Binding of new chemical entities to serum proteins is an issue confronting pharmaceutical
companies during development of potential therapeutic agents. Most drugs bind to the most …

Passive diffusion of weak organic electrolytes across Caco‐2 cell monolayers: Uncoupling the contributions of hydrodynamic, transcellular, and paracellular barriers

A Adson, PS Burton, TJ Raub, CL Barsuhn… - Journal of …, 1995 - Elsevier
A systematic approach was used to demonstrate the quantitative interplay of pH, pK a ,
lipophilicity, charged and uncharged molecular species, molecular size, aqueous diffusivity, and …

[HTML][HTML] How hydrogen bonds impact P-glycoprotein transport and permeability

PV Desai, TJ Raub, MJ Blanco - Bioorganic & medicinal chemistry letters, 2012 - Elsevier
The requirement to cross a biological membrane can be a complex process especially if
multidrug transporters such as P-gp must be considered. Drug partitioning into the lipid …

Permeability of bovine brain microvessel endothelial cells in vitro: barrier tightening by a factor released from astroglioma cells

TJ Raub, SL Kuentzel, GA Sawada - Experimental cell research, 1992 - Elsevier
It has been shown both in vivo and in culture that astrocytes communicate with brain microvessel
endothelial cells (BMECs) to induce many of the blood—brain barrier characteristics …

Design, synthesis, structure–activity relationship, and in vivo activity of azabicyclic aryl amides as α7 nicotinic acetylcholine receptor agonists

…, BA Olson, L Fitzgerald, BA Staton, TJ Raub… - Bioorganic & medicinal …, 2006 - Elsevier
A novel set of azabicyclic aryl amides have been identified as potent and selective agonists
of the α7 nAChR. A two-pronged approach was taken to improve the potential hERG liability …