P. Verhoest

发表

Identification of Phosphorylation Consensus Sequences and Endogenous Neuronal Substrates of the Psychiatric Risk Kinase TNIK

M. Ehlers, N. Brandon, Lan Xu, 2016, The Journal of Pharmacology and Experimental Therapeutics.

Moving beyond rules: the development of a central nervous system multiparameter optimization (CNS MPO) approach to enable alignment of druglike properties.

P. Verhoest, Travis T Wager, Xinjun Hou, 2010, ACS chemical neuroscience.

Defining desirable central nervous system drug space through the alignment of molecular properties, in vitro ADME, and safety attributes.

P. Verhoest, Y. Will, Travis T Wager, 2010, ACS chemical neuroscience.

Strategies to optimize the brain availability of central nervous system drug candidates

P. Verhoest, Travis T Wager, Xinjun Hou, 2011, Expert opinion on drug discovery.

Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor.

R. Kurumbail, B. L. Kormos, M. Hayward, 2015, Journal of medicinal chemistry.

Challenges and Opportunities in the Discovery of New Therapeutics Targeting the Kynurenine Pathway.

P. Verhoest, A. Dounay, J. Tuttle, 2015, Journal of medicinal chemistry.

Discovery of hydroxamate bioisosteres as KAT II inhibitors with improved oral bioavailability and pharmacokinetics

J. Pandit, R. Obach, Ji-Young Kim, 2013 .

PF-04859989 as a template for structure-based drug design: identification of new pyrazole series of irreversible KAT II inhibitors with improved lipophilic efficiency.

J. Pandit, Ji-Young Kim, P. Verhoest, 2013, Bioorganic & medicinal chemistry letters.

An oral SARS-CoV-2 Mpro inhibitor clinical candidate for the treatment of COVID-19

K. Gajiwala, A. Kalgutkar, P. Verhoest, 2021, Science.

Kinase domain inhibition of leucine rich repeat kinase 2 (LRRK2) using a [1,2,4]triazolo[4,3-b]pyridazine scaffold.

R. Kurumbail, B. L. Kormos, P. Verhoest, 2014, Bioorganic & medicinal chemistry letters.

Cancers gynécologiques et mammaires dans le département de la Somme: Gynecological and breast cancer in the departement of Somme

P. Verhoest, N. Raverdy, A. Lorriaux, 2004 .

Design and selection parameters to accelerate the discovery of novel central nervous system positron emission tomography (PET) ligands and their application in the development of a novel phosphodiesterase 2A PET ligand.

L. Chen, K. Zasadny, P. Verhoest, 2013, Journal of medicinal chemistry.

Pharmacological Characterization of 2-Methyl- N -((2 (cid:1) -(pyrrolidin-1-ylsulfonyl)biphenyl-4-yl)methyl)propan-1-amine (PF-04455242), a High-Affinity Antagonist Selective for (cid:1) -Opioid Receptors □ S

Anne W. Schmidt, P. Verhoest, S. Grimwood, 2011 .

Discovery of cyclopropyl chromane-derived pyridopyrazine-1,6-dione γ-secretase modulators with robust central efficacy.

Gregory W. Kauffman, David S. Ramirez, L. Pustilnik, 2017, MedChemComm.

Design of Pyridopyrazine-1,6-dione γ-Secretase Modulators that Align Potency, MDR Efflux Ratio, and Metabolic Stability.

Gregory W. Kauffman, L. Pustilnik, A. Stepan, 2015, ACS medicinal chemistry letters.

Central Nervous System Multiparameter Optimization Desirability: Application in Drug Discovery.

Anabella Villalobos, P. Verhoest, Travis T Wager, 2016, ACS chemical neuroscience.

Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia.

Spiros Liras, Anne W. Schmidt, J. Pandit, 2009, Journal of medicinal chemistry.

Design and discovery of 6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one (PF-04447943), a selective brain penetrant PDE9A inhibitor for the treatment of cognitive disorders.

F. Menniti, F. Nelson, C. Proulx-Lafrance, 2012, Journal of medicinal chemistry.

Quantitative Assessment of the Impact of Fluorine Substitution on P-Glycoprotein (P-gp) Mediated Efflux, Permeability, Lipophilicity, and Metabolic Stability.

Gregory W. Kauffman, P. Verhoest, M. Kuhn, 2016, Journal of medicinal chemistry.

Discovery of indole-derived pyridopyrazine-1,6-dione γ-secretase modulators that target presenilin.

Gregory W. Kauffman, L. Pustilnik, A. Stepan, 2015, Bioorganic & medicinal chemistry letters.

Total synthesis of (+)-phorboxazole A exploiting the Petasis-Ferrier rearrangement.

P. Verhoest, M. Schelhaas, K. Minbiole, 2001, Journal of the American Chemical Society.

A general strategy for the synthesis of cyclic N-aryl hydroxamic acids via partial nitro group reduction.

Ji-Young Kim, P. Verhoest, Laura A McAllister, 2011, The Journal of organic chemistry.

Spongistatin synthetic studies. 1. Construction of a C(29–48) subtarget

Mark D. McBriar, P. Verhoest, A. M. Boldi, 1997 .

Total Synthesis of (+)-Phorboxazole A Exploiting the Petasis—Ferrier Rearrangement.

P. Verhoest, M. Schelhaas, K. Minbiole, 2002 .

Phorboxazole synthetic studies. 1. Construction of a C(3-19) subtarget exploiting an extension of the Petasis-Ferrier rearrangement.

P. Verhoest, K. Minbiole, A. Smith, 1999, Organic letters.

Phorboxazole synthetic studies. 2. Construction of a C(20-28) subtarget, a further extension of the Petasis-Ferrier rearrangement.

P. Verhoest, K. Minbiole, A. Smith, 1999, Organic letters.

Total synthesis of (+)-phorboxazole A.

P. Verhoest, M. Schelhaas, K. Minbiole, 1998, Journal of the American Chemical Society.

Structure-Based Design of Irreversible Human KAT II Inhibitors: Discovery of New Potency-Enhancing Interactions.

J. Pandit, Ji-Young Kim, P. Verhoest, 2013, ACS medicinal chemistry letters.

1-(2-Hydroxy-2-methyl-3-phenoxypropanoyl)indoline-4-carbonitrile derivatives as potent and tissue selective androgen receptor modulators.

D. Powell, P. Verhoest, S. Nagpal, 2014, Journal of medicinal chemistry.

Quantitative Translational Analysis of Brain Kynurenic Acid Modulation via Irreversible Kynurenine Aminotransferase II Inhibition

K. A. Welch, T. Maurer, P. Verhoest, 2018, Molecular Pharmacology.

Chemoproteomics demonstrates target engagement and exquisite selectivity of the clinical phosphodiesterase 10A inhibitor MP-10 in its native environment.

N. Brandon, P. Verhoest, C. J. Schmidt, 2014, ACS chemical biology.

Designing small molecules for therapeutic success: a contemporary perspective.

T. Maurer, D. Hepworth, P. Verhoest, 2021, Drug discovery today.

Synthesis of ortho-substituted nitroaromatics via improved Negishi coupling conditions

Ji-Young Kim, P. Verhoest, Jaclyn L Henderson, 2011 .

Discovery of Brain-Penetrant, Irreversible Kynurenine Aminotransferase II Inhibitors for Schizophrenia.

J. Pandit, Ji-Young Kim, M. Hayward, 2012, ACS medicinal chemistry letters.

Acylhydrazones as M1/M3 selective muscarinic agonists

S. Semus, P. Verhoest, J. Blosser, 1996 .

Application of Structure-Based Design and Parallel Chemistry to Identify a Potent, Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor.

Laura McDowell, Scot Mente, Mihaly Hajos, 2017, Journal of medicinal chemistry.

Phosphodiesterase 9A Regulates Central cGMP and Modulates Responses to Cholinergic and Monoaminergic Perturbation In Vivo

Anne W. Schmidt, F. Menniti, M. Hajós, 2012, Journal of Pharmacology and Experimental Therapeutics.

PF-04447943, a novel PDE9A inhibitor, increases cGMP levels in cerebrospinal fluid: Translation from non-clinical species to healthy human volunteers

B. Corrigan, H. Soares, T. Nicholas, 2009, Alzheimer's & Dementia.

Photoaffinity Labeling and Quantitative Chemical Proteomics Identify LXRβ as the Functional Target of Enhancers of Astrocytic apoE.

P. Verhoest, C. Steppan, Travis T Wager, 2020, Cell chemical biology.

Synthesis and Use of 5-Vinyl-1,2,4-oxadiazoles as Michael Acceptors. A Rapid Synthesis of the Potent Muscarinic Agonist L-670,548

J. Macor, P. Verhoest, Robert L. Smith, 1996 .

Selective Brain Penetrant PDE 9 A Inhibitor for the Treatment of Cognitive Disorders

Ey, F. Menniti, F. Nelson, 2012 .

A chiral synthesis of (-)-spiro[1-azabicyclo[2.2.2]octane-3,5'- oxazolidin-2'-one]: a conformationally restricted analogue of acetylcholine that is a potent and selective alpha7 nicotinic receptor agonist.

J. Macor, P. Verhoest, G. Mullen, 2004, The Journal of organic chemistry.

(-)-Spiro[1-azabicyclo[2.2.2]octane-3,5'-oxazolidin-2'-one], a conformationally restricted analogue of acetylcholine, is a highly selective full agonist at the alpha 7 nicotinic acetylcholine receptor.

J. Macor, P. Verhoest, Yanyi Zhu, 2000, Journal of medicinal chemistry.

Identification of a Potent, Highly Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor Clinical Candidate.

J. Pandit, W. Hoffman, M. Hajós, 2018, Journal of medicinal chemistry.

Identification of a brain penetrant PDE9A inhibitor utilizing prospective design and chemical enablement as a rapid lead optimization strategy.

Anne W. Schmidt, F. Menniti, F. Nelson, 2009, Journal of medicinal chemistry.

Application of structure-based drug design and parallel chemistry to identify selective, brain penetrant, in vivo active phosphodiesterase 9A inhibitors.

Laura McDowell, Spiros Liras, Mihaly Hajos, 2012, Journal of medicinal chemistry.

The Discovery of a Novel Phosphodiesterase (PDE) 4B-Preferring Radioligand for Positron Emission Tomography (PET) Imaging.

R. J. Mather, L. Chen, K. Zasadny, 2017, Journal of medicinal chemistry.

Discovery and preclinical characterization of 1-methyl-3-(4-methylpyridin-3-yl)-6-(pyridin-2-ylmethoxy)-1H-pyrazolo-[3,4-b]pyrazine (PF470): a highly potent, selective, and efficacious metabotropic glutamate receptor 5 (mGluR5) negative allosteric modulator.

J. Cianfrogna, A. Stepan, Daniel P. Walker, 2014, Journal of medicinal chemistry.

Evaluating the differences in cycloalkyl ether metabolism using the design parameter "lipophilic metabolism efficiency" (LipMetE) and a matched molecular pairs analysis.

Gregory W. Kauffman, Christopher E. Keefer, A. Stepan, 2013, Journal of medicinal chemistry.

Design, synthesis, and pharmacological evaluation of a novel series of pyridopyrazine-1,6-dione γ-secretase modulators.

Gregory W. Kauffman, L. Pustilnik, S. Sakya, 2014, Journal of medicinal chemistry.

Pharmacological Characterization of 2-Methyl-N-((2′-(pyrrolidin-1-ylsulfonyl)biphenyl-4-yl)methyl)propan-1-amine (PF-04455242), a High-Affinity Antagonist Selective for κ-Opioid Receptors

Anne W. Schmidt, P. Verhoest, J. McLaughlin, 2011, Journal of Pharmacology and Experimental Therapeutics.

octane-3 , 5 ′-oxazolidin-2 ′-one ] , a Conformationally Restricted Analogue of Acetylcholine , Is a Highly Selective Full Agonist at the r 7 Nicotinic Acetylcholine Receptor

J. Macor, P. Verhoest, Yanyi Zhu, 2022 .

Discovery and Characterization of (R)-6-Neopentyl-2-(pyridin-2-ylmethoxy)-6,7-dihydropyrimido[2,1-c][1,4]oxazin-4(9H)-one (PF-06462894), an Alkyne-Lacking Metabotropic Glutamate Receptor 5 Negative Allosteric Modulator Profiled in both Rat and Nonhuman Primates.

J. Cianfrogna, A. Stepan, Daniel P. Walker, 2017, Journal of medicinal chemistry.

Preclinical Characterization of Selective Phosphodiesterase 10A Inhibitors: A New Therapeutic Approach to the Treatment of Schizophrenia

R. D. Williams, W. Hoffman, F. Menniti, 2008, Journal of Pharmacology and Experimental Therapeutics.

Azaindolines: derisking the indoline structural alert

P. Verhoest, A. Gilbert, Raghuram S. Tangirala, 2012 .

Late-Stage Microsomal Oxidation Reduces Drug–Drug Interaction and Identifies Phosphodiesterase 2A Inhibitor PF-06815189

G. S. Walker, A. Stepan, R. Obach, 2018, ACS Medicinal Chemistry Letters.

Design and discovery of a selective small molecule κ opioid antagonist (2-methyl-N-((2'-(pyrrolidin-1-ylsulfonyl)biphenyl-4-yl)methyl)propan-1-amine, PF-4455242).

Gregory W. Kauffman, Anne W. Schmidt, S. Liras, 2011, Journal of medicinal chemistry.

Challenges and Opportunities in the Discovery of New Therapeutics Targeting the Kynurenine Pathway.

P. Verhoest, A. Dounay, J. Tuttle, 2015, Journal of medicinal chemistry.

Quantitative Assessment of the Impact of Fluorine Substitution on P-Glycoprotein (P-gp) Mediated Efflux, Permeability, Lipophilicity, and Metabolic Stability.

Gregory W. Kauffman, P. Verhoest, Travis T Wager, 2016, Journal of medicinal chemistry.

The Discovery of a Novel Phosphodiesterase (PDE) 4B-Preferring Radioligand for Positron Emission Tomography (PET) Imaging.

R. J. Mather, L. Chen, K. Zasadny, 2017, Journal of medicinal chemistry.

Dendritic spine density deficits in the hippocampal CA1 region of young Tg2576 mice are ameliorated with the PDE9A inhibitor PF-04447943

P. Verhoest, Abigail Mariga, Thomas A. Lanz, 2010, Alzheimer's & Dementia.

Discovery of Clinical Candidate PF-06648671: A Potent γ-Secretase Modulator for the Treatment of Alzheimer's Disease.

Gregory W. Kauffman, L. Pustilnik, É. Hajós‐Korcsok, 2024, Journal of medicinal chemistry.

Discovery of cyclopropyl chromane-derived pyridopyrazine-1,6-dione γ-secretase modulators with robust central efficacy.

Gregory W. Kauffman, David S. Ramirez, L. Pustilnik, 2017, MedChemComm.

The Function, Enzyme Kinetics, Structural Biology, and Medicinal Chemistry of PDE10A

P. Verhoest, T. Chappie, 2014 .

Highly Potent , Selective , and E ffi cacious Metabotropic Glutamate Receptor 5 ( mGluR 5 ) Negative Allosteric Modulator

Ey, J. Cianfrogna, A. Stepan, 2014 .