Publications by authors named "Wayne Geissler"

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Integrating the Impact of Lipophilicity on Potency and Pharmacokinetic Parameters Enables the Use of Diverse Chemical Space during Small Molecule Drug Optimization.
Randy R Miller, Maria Madeira, Harold B Wood, Wayne M Geissler, Conrad E Raab

J Med Chem· November 2020

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Design and synthesis of novel proline based factor XIa selective inhibitors as leads for potential new anticoagulants.
Zahid Hussain, Andrew J Cooke, Santhosh Neelamkavil, Lindsay Brown, Emma Carswell, Wayne M Geissler

Bioorg Med Chem Lett· August 2020

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Corrigendum to "Discovery of benzofuran propanoic acid GPR120 agonists: From uHTS hit to mechanism-based pharmacodynamic effects" [Bioorg. Med. Chem. Lett. 26 (2016) 5724-5728].
Matthew Lombardo, Kate Bender, Clare London, Michael A Plotkin, Melissa Kirkland, Wayne Geissler

Bioorg Med Chem Lett· March 2017

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Discovery of benzofuran propanoic acid GPR120 agonists: From uHTS hit to mechanism-based pharmacodynamic effects.
Matthew Lombardo, Kate Bender, Clare London, Michael A Plotkin, Melissa Kirkland, Wayne Geissler

Bioorg Med Chem Lett· December 2016

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Definitive Metabolite Identification Coupled with Automated Ligand Identification System (ALIS) Technology: A Novel Approach to Uncover Structure-Activity Relationships and Guide Drug Design in a Factor IXa Inhibitor Program.
Ting Zhang, Yong Liu, Xianshu Yang, Gary E Martin, Huifang Yao, Wayne M Geissler

J Med Chem· March 2016

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Preclinical and translational evaluation of coagulation factor IXa as a novel therapeutic target.
Wendy Ankrom, Harold B Wood, Jiayi Xu, Wayne Geissler, Tom Bateman

Pharmacol Res Perspect· February 2016

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Development of a novel class of potent and selective FIXa inhibitors.
Ting Zhang, Patrick Andre, Thomas J Bateman, Yi-Heng Chen, Kunal Desai, Wayne M Geissler

Bioorg Med Chem Lett· November 2015

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Development of a novel tricyclic class of potent and selective FIXa inhibitors.
Dongfang Meng, Patrick Andre, Thomas J Bateman, Richard Berger, Yi-Heng Chen, Wayne M Geissler

Bioorg Med Chem Lett· November 2015

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Rapid development of two factor IXa inhibitors from hit to lead.
Dann L Parker, Shawn Walsh, Bing Li, Esther Kim, Aurash Sharipour, Wayne Geissler

Bioorg Med Chem Lett· June 2015

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Discovery and optimization of orally active cyclohexane-based prolylcarboxypeptidase (PrCP) inhibitors.
John S Debenham, Thomas H Graham, Andreas Verras, Yong Zhang, Matthew J Clements, Wayne M Geissler

Bioorg Med Chem Lett· December 2013

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A new class of prolylcarboxypeptidase inhibitors, part 1: discovery and evaluation.
Thomas H Graham, Wensheng Liu, Andreas Verras, Iyassu K Sebhat, Yusheng Xiong, Wayne M Geissler

Bioorg Med Chem Lett· April 2012

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A new class of prolylcarboxypeptidase inhibitors, part 2: the aminocyclopentanes.
Thomas H Graham, Wensheng Liu, Andreas Verras, Mikhail Reibarkh, Kelly Bleasby, Wayne M Geissler

Bioorg Med Chem Lett· April 2012

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Discovery of a new class of potent prolylcarboxypeptidase inhibitors derived from alanine.
Zhicai Wu, Cangming Yang, Yusheng Xiong, Zhe Feng, Matthew Lombardo, Wayne Geissler

Bioorg Med Chem Lett· February 2012

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Discovery of benzodihydroisofurans as novel, potent, bioavailable and brain-penetrant prolylcarboxypeptidase inhibitors.
Hong C Shen, Fa-Xiang Ding, Jinlong Jiang, Andreas Verras, Renee M Chabin, Wayne Geissler

Bioorg Med Chem Lett· February 2012

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The discovery of non-benzimidazole and brain-penetrant prolylcarboxypeptidase inhibitors.
Thomas H Graham, Hong C Shen, Wensheng Liu, Yusheng Xiong, Andreas Verras, Wayne M Geissler

Bioorg Med Chem Lett· January 2012

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Discovery of benzimidazole pyrrolidinyl amides as prolylcarboxypeptidase inhibitors.
Hong C Shen, Fa-Xiang Ding, Changyou Zhou, Yusheng Xiong, Andreas Verras, Wayne Geissler

Bioorg Med Chem Lett· March 2011

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Enzymatic preparation of high-specific-activity beta-D-[6,6'-3H]fructose-2,6-bisphosphate: Application to a sensitive assay for fructose-2,6-bisphosphatase.
Robert W Myers, Walter F Baginsky, David J Gattermeir, Wayne M Geissler, Georgianna Harris

Anal Biochem· November 2010

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Design and synthesis of prolylcarboxypeptidase (PrCP) inhibitors to validate PrCP as a potential target for obesity.
Changyou Zhou, Margareta Garcia-Calvo, Shirly Pinto, Matthew Lombardo, Zhe Feng, Wayne M Geissler

J Med Chem· October 2010

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Peptidomic profiling of human cerebrospinal fluid identifies YPRPIHPA as a novel substrate for prolylcarboxypeptidase.
Xuemei Zhao, Katie Southwick, Helene L Cardasis, Yi Du, Michael E Lassman, Wayne M Geissler

Proteomics· August 2010

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Expression, purification and crystallization of human prolylcarboxypeptidase.
Pravien D Abeywickrema, Sangita B Patel, Noel J Byrne, Ronald E Diehl, Dawn L Hall, Wayne M Geissler

Acta Crystallogr Sect F Struct Biol Cryst Commun· June 2010

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Modeling aided design of potent glycogen phosphorylase inhibitors.
Qiaolin Deng, Zhijian Lu, Joann Bohn, Kenneth P Ellsworth, Robert W Myers, Wayne M Geissler

J Mol Graph Model· April 2005

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Selective glucocorticoid receptor nonsteroidal ligands completely antagonize the dexamethasone mediated induction of enzymes involved in gluconeogenesis and glutamine metabolism.
Monica Einstein, Mark Greenlee, Greg Rouen, Ayesha Sitlani, Joe Santoro, Wayne Geissler

J Steroid Biochem Mol Biol· December 2004

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Novel 3,4-dihydroquinolin-2(1H)-one inhibitors of human glycogen phosphorylase a.
Keith G Rosauer, Anthony K Ogawa, Chris A Willoughby, Kenneth P Ellsworth, Wayne M Geissler

Bioorg Med Chem Lett· December 2003

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A new class of glycogen phosphorylase inhibitors.
Zhijian Lu, Joann Bohn, Raynald Bergeron, Qiaolin Deng, Kenneth P Ellsworth, Wayne M Geissler

Bioorg Med Chem Lett· November 2003

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Glucose-lowering in a db/db mouse model by dihydropyridine diacid glycogen phosphorylase inhibitors.
Anthony K Ogawa, Chris A Willoughby, Raynald Bergeron, Kenneth P Ellsworth, Wayne M Geissler

Bioorg Med Chem Lett· October 2003

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