T. V. von Geldern

发表

Benzoxazole benzenesulfonamides as allosteric inhibitors of fructose-1,6-bisphosphatase.

C. Abad-Zapatero, R. Gum, C. Hutchins, 2006, Bioorganic & medicinal chemistry letters.

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

J. Archer, A. Hoerauf, D. Kempf, 2019, Science Translational Medicine.

In vivo kinetics of Wolbachia depletion by ABBV-4083 in L. sigmodontis adult worms and microfilariae

A. Hoerauf, D. Kempf, S. Ward, 2019, PLoS neglected tropical diseases.

Two Analogues of Fenarimol Show Curative Activity in an Experimental Model of Chagas Disease

David M. Shackleford, M. J. Abbott, Paul W. Alexander, 2013, Journal of medicinal chemistry.

Pharmacological characterization of A-127722: an orally active and highly potent ETA-selective receptor antagonist.

S. Magnuson, K. Marsh, J. R. Wu-wong, 1996, The Journal of pharmacology and experimental therapeutics.

Discovery of novel p-arylthio cinnamides as antagonists of leukocyte function-associated antigen-1/intercellular adhesion molecule-1 interaction. 4. Structure-activity relationship of substituents on the benzene ring of the cinnamide.

E B Reilly, J. R. Huth, Z. Xin, 2001, Journal of medicinal chemistry.

The effects of diminishing albumin binding to some Endothelin receptor antagonists.

K. Marsh, J. R. Wu-wong, W. Chiou, 1998, Life sciences.

Selective antagonism of the hepatic glucocorticoid receptor reduces hepatic glucose production.

D. Edgerton, A. Cherrington, D. Beno, 2006, Metabolism: clinical and experimental.

An Essential Myosin Light Chain Peptide Induces Supramaximal Stimulation of Cardiac Myofibrillar ATPase Activity*

R. Solaro, J. R. Wu-wong, T. Opgenorth, 1996, The Journal of Biological Chemistry.

Pyrrolidine-constrained phenethylamines: The design of potent, selective, and pharmacologically efficacious dipeptidyl peptidase IV (DPP4) inhibitors from a lead-like screening hit.

G. L. Hamilton, K. Longenecker, H. Sham, 2007, Bioorganic & medicinal chemistry letters.

“The next big thing” in diabetes: clinical progress on DPP‐IV inhibitors

J. Trevillyan, T. V. von Geldern, 2006 .

Liver-selective glucocorticoid receptor antagonism decreases glucose production and increases glucose disposal, ameliorating insulin resistance.

P. Jacobson, D. Wilcox, B. Zinker, 2007, Metabolism: clinical and experimental.

Hepatic Glucocorticoid Receptor Antagonism Is Sufficient to Reduce Elevated Hepatic Glucose Output and Improve Glucose Control in Animal Models of Type 2 Diabetes

L. Öhman, D. Edgerton, A. Cherrington, 2005, Journal of Pharmacology and Experimental Therapeutics.

Synthesis, activity, metabolic stability, and pharmacokinetics of glucocorticoid receptor modulator-statin hybrids.

M. Emery, S. Fung, Jiahong Wang, 2004, Bioorganic & medicinal chemistry letters.

Xanthine mimetics as potent dipeptidyl peptidase IV inhibitors.

K. Longenecker, H. Sham, K. Stewart, 2006, Bioorganic & medicinal chemistry letters.

Discovery of 2-[4-{{2-(2S,5R)-2-cyano-5-ethynyl-1-pyrrolidinyl]-2-oxoethyl]amino]- 4-methyl-1-piperidinyl]-4-pyridinecarboxylic acid (ABT-279): a very potent, selective, effective, and well-tolerated inhibitor of dipeptidyl peptidase-IV, useful for the treatment of diabetes.

K. Longenecker, J. Segreti, H. Sham, 2006, Journal of medicinal chemistry.

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

K. Marsh, J. R. Wu-wong, B. Dayton, 2002, Clinical science.

2,4-Diarylpyrrolidine-3-carboxylic acids--potent ETA selective endothelin receptor antagonists. 1. Discovery of A-127722.

A. Tasker, K. Marsh, J. R. Wu-wong, 1996, Journal of medicinal chemistry.

Parallel strategies for the preparation and selection of liver-targeted glucocorticoid receptor antagonists.

G. L. Hamilton, B. J. Backes, S. Fung, 2007, Bioorganic & medicinal chemistry letters.

Synthesis and activity of novel bile-acid conjugated glucocorticoid receptor antagonists.

S. Richards, S. Fung, Jiahong Wang, 2006, Bioorganic & medicinal chemistry letters.

Pharmacology of A-216546: a highly selective antagonist for endothelin ET(A) receptor.

K. Marsh, J. Wu-Wong, B. Dayton, 1999, European journal of pharmacology.

Truncated atrial natriuretic factor analogs retain full agonist activity.

D. Pollock, G. Budzik, W. Holleman, 1991, Canadian journal of physiology and pharmacology.

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

A. Tasker, J. R. Wu-wong, M. Winn, 2002, Clinical science.

'Irreversible' endothelin-1 binding does not prohibit ABT-627 from reversing endothelin-1-induced effects.

J. R. Wu-wong, W. Chiou, J. Wessale, 2000, Journal of cardiovascular pharmacology.

Discovery of a series of pyrrolidine-based endothelin receptor antagonists with enhanced ET(A) receptor selectivity.

A. Tasker, K. Marsh, C. Hutchins, 1999, Bioorganic & medicinal chemistry.

Endothelins and endothelin receptor antagonists: binding to plasma proteins.

J. R. Wu-wong, M. Winn, W. Chiou, 1996, Life sciences.

HPLC and PDMS analysis of cleavage products aid in the design of small, stable ANP analogues.

S. Davidsen, W. Holleman, A. Buko, 2009, International journal of peptide and protein research.

A ring-reversed analog of atrial natriuretic peptide retains receptor binding, guanylate cyclase stimulation.

G. Budzik, T. V. von Geldern, T. P. Dillon, 1992, Biochemical and biophysical research communications.

Pyrrolidine-3-carboxylic acids as endothelin antagonists. 2. Sulfonamide-based ETA/ETB mixed antagonists.

K. Marsh, M. Winn, D. Dixon, 1997, Journal of medicinal chemistry.

Discovery of a potent atrial natriuretic peptide antagonist for ANPA receptors in the human neuroblastoma NB-OK-1 cell line.

C. Delporte, J. Winand, T. V. von Geldern, 1992, European journal of pharmacology.

Amino-substituted heterocycles as isosteres of trans-cinnamides: design and synthesis of heterocyclic biaryl sulfides as potent antagonists of LFA-1/ICAM-1 binding.

T. Sowin, Gary T. Wang, R. Gentles, 2005, Bioorganic & medicinal chemistry letters.

Design, structure-activity relationship and in vivo efficacy of piperazine analogues of fenarimol as inhibitors of Trypanosoma cruzi.

David M. Shackleford, Paul W. Alexander, E. Chatelain, 2013, Bioorganic & medicinal chemistry.

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

M. J. Abbott, Paul W. Alexander, E. Chatelain, 2012, Journal of medicinal chemistry.

Small atrial natriuretic peptide analogues: design, synthesis, and structural requirements for guanylate cyclase activation.

S. Davidsen, E. Bush, M. Chu-Moyer, 1992, Journal of medicinal chemistry.

Atrial natriuretic peptide antagonists: biological evaluation and structural correlations.

Y. Kiso, G. Budzik, W. Holleman, 1990, Molecular pharmacology.

Novel p-arylthio cinnamides as antagonists of leukocyte function-associated antigen-1/intracellular adhesion molecule-1 interaction. 2. Mechanism of inhibition and structure-based improvement of pharmaceutical properties.

E B Reilly, J. R. Huth, E. Olejniczak, 2001, Journal of medicinal chemistry.

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

K. Longenecker, H. Sham, Xiaofen Li, 2007, Journal of medicinal chemistry.

Benzoxazole benzenesulfonamides as allosteric inhibitors of fructose-1,6-bisphosphatase.

C. Abad-Zapatero, R. Gum, C. Hutchins, 2006, Bioorganic & medicinal chemistry letters.

New antimitotic agents with activity in multi-drug-resistant cell lines and in vivo efficacy in murine tumor models.

S. Rosenberg, S. L. Gwaltney, R. B. Credo, 2001, Journal of medicinal chemistry.

Discovery of Substituted Di(pyridin-2-yl)-1,2,4-thiadiazol-5-amines as Novel Macrofilaricidal Compounds for the Treatment of Human Filarial Infections

A. Hoerauf, S. Menon, Alexandra Ehrens, 2022, Journal of medicinal chemistry.

Synthesis and biological evaluation of novel, selective, nonsteroidal glucocorticoid receptor antagonists.

I. Akritopoulou‐Zanze, Jyoti R. Patel, P. Kym, 2004, Bioorganic & medicinal chemistry letters.

Pyrrolidine-3-carboxylic acids as endothelin antagonists. 5. Highly selective, potent, and orally active ET(A) antagonists.

K. Marsh, M. Winn, W. Chiou, 2001, Journal of medicinal chemistry.

Discovery of novel p-arylthio cinnamides as antagonists of leukocyte function-associated antigen-1/intracellular adhesion molecule-1 interaction. 1. Identification of an additional binding pocket based on an anilino diaryl sulfide lead.

E B Reilly, K. Marsh, M. Gallatin, 2000, Journal of medicinal chemistry.

Discovery of ((4R,5S)-5-amino-4-(2,4,5- trifluorophenyl)cyclohex-1-enyl)-(3- (trifluoromethyl)-5,6-dihydro- [1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanone (ABT-341), a highly potent, selective, orally efficacious, and safe dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.

K. Longenecker, H. Sham, R. Fryer, 2006, Journal of medicinal chemistry.

Potent and selective non-benzodioxole-containing endothelin-A receptor antagonists.

A. Tasker, K. Marsh, B. Dayton, 1997, Journal of medicinal chemistry.

Discovery of ABBV-4083, a novel analog of Tylosin A that has potent anti-Wolbachia and anti-filarial activity

A. Hoerauf, D. Kempf, S. Ward, 2019, PLoS neglected tropical diseases.

Crystal structures of DPP-IV (CD26) from rat kidney exhibit flexible accommodation of peptidase-selective inhibitors.

Vincent S Stoll, K. Longenecker, V. Stoll, 2006, Biochemistry.

An evaluation of a C-glucuronide as a liver targeting group: conjugate of a glucocorticoid antagonist.

M. Emery, Jiahong Wang, J. Link, 2003, Bioorganic & medicinal chemistry letters.

Selection and optimization of hits from a high-throughput phenotypic screen against Trypanosoma cruzi.

M. J. Abbott, Paul W. Alexander, S. Cornwall, 2013, Future medicinal chemistry.

Stimulation of atrial natriuretic peptide receptor/guanylyl cyclase- A signaling pathway antagonizes the activation of protein kinase C-alpha in murine Leydig cells.

K. Pandey, R. Calle, T. V. von Geldern, 1997, Biochimica et biophysica acta.

Atrial natriuretic peptide and glomerular hyperfiltration during onset of spontaneous diabetes mellitus.

R. Vari, T. Opgenorth, T. V. von Geldern, 1994, American Journal of Physiology.

Pyrrolidine-3-carboxylic acids as endothelin antagonists. 4. Side chain conformational restriction leads to ET(B) selectivity.

A. Tasker, K. Marsh, M. Winn, 1999, Journal of Medicinal Chemistry.

Azole endothelin antagonists. 3. Using delta log P as a tool to improve absorption.

K. Marsh, J. R. Wu-wong, B. Dayton, 1996, Journal of medicinal chemistry.

Design, synthesis, and activity of a series of pyrrolidine-3-carboxylic acid-based, highly specific, orally active ET(B) antagonists containing a diphenylmethylamine acetamide side chain.

K. Marsh, M. Winn, W. Chiou, 1999, Journal of medicinal chemistry.

Expression of atrial natriuretic peptide receptor-A antagonizes the mitogen-activated protein kinases (Erk2 and P38MAPK) in cultured human vascular smooth muscle cells

G. Sharma, R. Gerrity, A. Antonov, 2002, Molecular and Cellular Biochemistry.

Azole endothelin antagonists. 1. A receptor model explains an unusual structure-activity profile.

C. Hutchins, J. R. Wu-wong, W. Chiou, 1996, Journal of medicinal chemistry.

Azole endothelin antagonists. 2. Structure-activity studies.

J. R. Wu-wong, W. Chiou, T. V. Geldern, 1996, Journal of medicinal chemistry.

Antidiabetic activity of passive nonsteroidal glucocorticoid receptor modulators.

Jyoti R. Patel, T. Reisch, Z. Tian, 2005, Journal of medicinal chemistry.

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

H. Sham, Xiaofen Li, D. Beno, 2006, Journal of Medicinal Chemistry.

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

K. Koehler, L. Hagberg, C. Jakob, 2004, Journal of medicinal chemistry.

Benzoxazole benzenesulfonamides are novel allosteric inhibitors of fructose-1,6-bisphosphatase with a distinct binding mode.

Celerino Abad-Zapatero, Chaohong Sun, C. Abad-Zapatero, 2006, Bioorganic & medicinal chemistry letters.

Selection and optimization of hits from a high-throughput phenotypic screen against Trypanosoma cruzi.

Paul W. Alexander, E. Chatelain, S. Charman, 2013, Future medicinal chemistry.

Identification and Profiling of a Novel Diazaspiro[3.4]octane Chemical Series Active against Multiple Stages of the Human Malaria Parasite Plasmodium falciparum and Optimization Efforts.

E. Winzeler, K. Chibale, Dale Taylor, 2021, Journal of medicinal chemistry.