Novel p-Arylthio Cinnamides as Antagonists of Leukocyte Function-Associated Antigen-1/Intracellular Adhesion Molecule-1 Interaction. 2. Mechanism of Inhibition …

…, GF Okasinski, SW Fesik, TW von Geldern - Journal of medicinal …, 2001 - ACS Publications
The interaction between leukocyte function-associated antigen-1 (LFA-1) and intracellular
adhesion molecule-1 (ICAM-1) has been implicated in inflammatory and immune diseases. …

Discovery of Novel p-Arylthio Cinnamides as Antagonists of Leukocyte Function-Associated Antigen-1/Intracellular Adhesion Molecule-1 Interaction. 1. Identification …

…, GF Okasinski, TW von Geldern… - Journal of medicinal …, 2000 - ACS Publications
The interaction between leukocyte function-associated antigen-1 (LFA-1), a member of the
β 2 -integrin family of adhesion molecules, and intracellular adhesion molecule ICAM-1 (cd54…

Pharmacology of endothelin receptor antagonists ABT-627, ABT-546, A-182086 and A-192621: ex vivo and in vivo studies

…, KC Marsh, M Winn, HS Jae, TW GELDERN… - 2002 - portlandpress.com
Endothelins (ETs), 21-amino-acid peptides involved in the pathogenesis of various diseases,
bind to ET A and ET B receptors to initiate their effects. Based on the same core structure, …

Analogues of fenarimol are potent inhibitors of Trypanosoma cruzi and are efficacious in a murine model of Chagas disease

…, E Chatelain, TW von Geldern… - Journal of medicinal …, 2012 - ACS Publications
We report the discovery of nontoxic fungicide fenarimol (1) as an inhibitor of Trypanosoma
cruzi ( T. cruzi ), the causative agent of Chagas disease, and the results of structure–activity …

Preclinical development of an oral anti-Wolbachia macrolide drug for the treatment of lymphatic filariasis and onchocerciasis

MJ Taylor, TW von Geldern, L Ford… - Science translational …, 2019 - science.org
There is an urgent global need for a safe macrofilaricide drug to accelerate elimination of
the neglected tropical diseases onchocerciasis and lymphatic filariasis. From an anti-infective …

Hepatic glucocorticoid receptor antagonism is sufficient to reduce elevated hepatic glucose output and improve glucose control in animal models of type 2 diabetes

PB Jacobson, TW von Geldern, L Öhman… - … of Pharmacology and …, 2005 - ASPET
Glucocorticoids amplify endogenous glucose production in type 2 diabetes by increasing
hepatic glucose output. Systemic glucocorticoid blockade lowers glucose levels in type 2 …

Discovery and structure− activity relationships of piperidinone-and piperidine-constrained phenethylamines as novel, potent, and selective dipeptidyl peptidase IV …

Z Pei, X Li, TW von Geldern… - Journal of medicinal …, 2007 - ACS Publications
Dipeptidyl peptidase IV (DPP4) inhibitors are emerging as a new class of therapeutic agents
for the treatment of type 2 diabetes. They exert their beneficial effects by increasing the …

2,4-Diarylpyrrolidine-3-carboxylic AcidsPotent ETA Selective Endothelin Receptor Antagonists. 1. Discovery of A-127722

M Winn, TW von Geldern, TJ Opgenorth… - Journal of medicinal …, 1996 - ACS Publications
We have discovered a novel class of endothelin (ET) receptor antagonists through pharmacophore
analysis of the existing non-peptide ET antagonists. On the basis of this analysis, we …

Discovery, structure− activity relationship, and pharmacological evaluation of (5-substituted-pyrrolidinyl-2-carbonyl)-2-cyanopyrrolidines as potent dipeptidyl peptidase …

…, X Li, K Longenecker, TW von Geldern… - Journal of medicinal …, 2006 - ACS Publications
A series of (5-substituted pyrrolidinyl-2-carbonyl)-2-cyanopyrrolidine (C5-Pro-Pro) analogues
was discovered as dipeptidyl peptidase IV (DPPIV) inhibitors as a potential treatment of …

Liver-selective glucocorticoid antagonists: a novel treatment for type 2 diabetes

TW von Geldern, N Tu, PR Kym, JT Link… - Journal of medicinal …, 2004 - ACS Publications
Hepatic blockade of glucocorticoid receptors (GR) suppresses glucose production and thus
decreases circulating glucose levels, but systemic glucocorticoid antagonism can produce …