Publications by authors named "Gary Probst"

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Transcriptional repression of estrogen receptor alpha by YAP reveals the Hippo pathway as therapeutic target for ER breast cancer.
Shenghong Ma, Tracy Tang, Gary Probst, Andrei Konradi, Chunyu Jin

Nat Commun· February 2022

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Antibody-Drug Conjugates (ADCs) Derived from Interchain Cysteine Cross-Linking Demonstrate Improved Homogeneity and Other Pharmacological Properties over Conventional Heterogeneous ADCs.
Christopher R Behrens, Edward H Ha, Lawrence L Chinn, Simeon Bowers, Gary Probst

Mol Pharm· November 2015

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Thermodynamic and kinetic characterization of hydroxyethylamine β-secretase-1 inhibitors.
Kalyani Mondal, Karin Regnstrom, Winse Morishige, Robin Barbour, Gary Probst

Biochem Biophys Res Commun· November 2013

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Design and synthesis of hydroxyethylamine (HEA) BACE-1 inhibitors: prime side chromane-containing inhibitors.
Raymond A Ng, Minghua Sun, Simeon Bowers, Roy K Hom, Gary D Probst

Bioorg Med Chem Lett· August 2013

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Discovery of (R)-4-cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro-1H-pyrazolo[4,3-c]quinoline (ELND006) and (R)-4-cyclopropyl-8-fluoro-5-(6-(trifluoromethyl)pyridin-3-ylsulfonyl)-4,5-dihydro-2H-pyrazolo[4,3-c]quinoline (ELND007): metabolically stable γ-secretase Inhibitors that selectively inhibit the production of amyloid-β over Notch.
Gary Probst, Danielle L Aubele, Simeon Bowers, Darren Dressen, Albert W Garofalo

J Med Chem· July 2013

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Discovery of 4-alkylamino-7-aryl-3-cyanoquinoline LRRK2 kinase inhibitors.
Albert W Garofalo, Marc Adler, Danielle L Aubele, Elizabeth F Brigham, David Chian, Gary D Probst

Bioorg Med Chem Lett· April 2013

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Triazolopyridazine LRRK2 kinase inhibitors.
Maurizio Franzini, Xiaocong M Ye, Marc Adler, Danielle L Aubele, Albert W Garofalo, Gary D Probst

Bioorg Med Chem Lett· April 2013

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Structure-based design of novel dihydroisoquinoline BACE-1 inhibitors that do not engage the catalytic aspartates.
Simeon Bowers, Ying-zi Xu, Shendong Yuan, Gary D Probst, Roy K Hom

Bioorg Med Chem Lett· April 2013

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Discovery of a novel [3.2.1] benzo fused bicyclic sulfonamide-pyrazoles as potent, selective and efficacious γ-secretase inhibitors.
Xiaocong M Ye, Andrei W Konradi, Minghua Sun, Shendong Yuan, Danielle L Aubele, Gary D Probst

Bioorg Med Chem Lett· February 2013

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Novel cinnoline-based inhibitors of LRRK2 kinase activity.
Albert W Garofalo, Marc Adler, Danielle L Aubele, Simeon Bowers, Maurizio Franzini, Gary D Probst

Bioorg Med Chem Lett· January 2013

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Small-molecule BACE1 inhibitors: a patent literature review (2006 - 2011).
Gary Probst, Ying-zi Xu

Expert Opin Ther Pat· May 2012

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Design, synthesis and structure-activity relationship of novel [3.3.1] bicyclic sulfonamide-pyrazoles as potent γ-secretase inhibitors.
Danielle L Aubele, Anh P Truong, Darren B Dressen, Gary D Probst, Simeon Bowers

Bioorg Med Chem Lett· October 2011

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Design and synthesis of brain penetrant selective JNK inhibitors with improved pharmacokinetic properties for the prevention of neurodegeneration.
Simeon Bowers, Anh P Truong, R Jeffrey Neitz, Roy K Hom, Jennifer M Sealy, Gary D Probst

Bioorg Med Chem Lett· September 2011

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Design and synthesis of a novel, orally active, brain penetrant, tri-substituted thiophene based JNK inhibitor.
Simeon Bowers, Anh P Truong, R Jeffrey Neitz, Martin Neitzel, Gary D Probst

Bioorg Med Chem Lett· March 2011

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Highly selective c-Jun N-terminal kinase (JNK) 2 and 3 inhibitors with in vitro CNS-like pharmacokinetic properties prevent neurodegeneration.
Gary D Probst, Simeon Bowers, Jennifer M Sealy, Anh P Truong, Roy K Hom

Bioorg Med Chem Lett· January 2011

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Design and synthesis of disubstituted thiophene and thiazole based inhibitors of JNK.
Roy K Hom, Simeon Bowers, Jennifer M Sealy, Anh P Truong, Gary D Probst

Bioorg Med Chem Lett· December 2010

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Design of an orally efficacious hydroxyethylamine (HEA) BACE-1 inhibitor in a preclinical animal model.
Anh P Truong, Gergley Tóth, Gary D Probst, Jennifer M Sealy, Simeon Bowers

Bioorg Med Chem Lett· November 2010

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Design and synthesis of hydroxyethylamine (HEA) BACE-1 inhibitors: structure-activity relationship of the aryl region.
Gary D Probst, Simeon Bowers, Jennifer M Sealy, Brian Stupi, Darren Dressen

Bioorg Med Chem Lett· October 2010

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Improving the permeability of the hydroxyethylamine BACE-1 inhibitors: structure-activity relationship of P2' substituents.
Anh P Truong, Gary D Probst, Jose Aquino, Larry Fang, Louis Brogley

Bioorg Med Chem Lett· August 2010

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N-Bridged bicyclic sulfonamides as inhibitors of gamma-secretase.
Simeon Bowers, Gary D Probst, Anh P Truong, Roy K Hom, Andrei W Konradi

Bioorg Med Chem Lett· December 2009

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Design and synthesis of cell potent BACE-1 inhibitors: structure-activity relationship of P1' substituents.
Jennifer M Sealy, Anh P Truong, Luke Tso, Gary D Probst, Jose Aquino

Bioorg Med Chem Lett· November 2009

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Design, synthesis, and structure-activity relationship of novel orally efficacious pyrazole/sulfonamide based dihydroquinoline gamma-secretase inhibitors.
Anh P Truong, Danielle L Aubele, Gary D Probst, Martin L Neitzel, Chris M Semko

Bioorg Med Chem Lett· September 2009

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Discovery of betrixaban (PRT054021), N-(5-chloropyridin-2-yl)-2-(4-(N,N-dimethylcarbamimidoyl)benzamido)-5-methoxybenzamide, a highly potent, selective, and orally efficacious factor Xa inhibitor.
Penglie Zhang, Wenrong Huang, Lingyan Wang, Liang Bao, Zhaozhong J Jia, Gary D Probst

Bioorg Med Chem Lett· April 2009

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The role and significance of unconventional hydrogen bonds in small molecule recognition by biological receptors of pharmaceutical relevance.
Gergely Tóth, Simeon G Bowers, Anh P Truong, Gary Probst

Curr Pharm Des· February 2008

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A formal synthesis of (-)-mycalamide A.
Barry M Trost, Hanbiao Yang, Gary D Probst

J Am Chem Soc· January 2004

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