J. Audia

发表

Fragment-Based Discovery of a Selective and Cell-Active Benzodiazepinone CBP/EP300 Bromodomain Inhibitor (CPI-637).

Y. Leblanc, H. Jayaram, R. Sims, 2016, ACS medicinal chemistry letters.

Development of methyl isoxazoleazepines as inhibitors of BET.

R. Cummings, P. Sandy, Y. Leblanc, 2015, Bioorganic & medicinal chemistry letters.

Neurogenic Dural Protein Extravasation Induced by Meta-Chlorophenylpiperazine (Mcpp) Involves Nitric Oxide and 5-HT2B Receptor Activation

D. Nelson, J. Audia, L. Phebus, 2003, Cephalalgia : an international journal of headache.

GNE-371, a Potent and Selective Chemical Probe for the Second Bromodomains of Human Transcription-Initiation-Factor TFIID Subunit 1 and Transcription-Initiation-Factor TFIID Subunit 1-like.

H. Jayaram, F. A. Romero, R. Cummings, 2018, Journal of medicinal chemistry.

Diving into the Water: Inducible Binding Conformations for BRD4, TAF1(2), BRD9, and CECR2 Bromodomains.

Andrew C Good, Vickie Tsui, Jian Wang, 2016, Journal of medicinal chemistry.

US immigration order strikes against biotech

Christopher R. Westphal, Mara G. Aspinall, J. A. Scarlett, 2017, Nature Biotechnology.

N(1)-substituted ergolines and tryptamines show species differences for the agonist-labeled 5-HT2 receptor.

D. Nelson, J. Audia, M. P. Johnson, 1993, European journal of pharmacology.

Species differences in the pharmacology of the 5-hydroxytryptamine2 receptor: structurally specific differentiation by ergolines and tryptamines.

D. Nelson, J. Audia, D. Wainscott, 1993, The Journal of pharmacology and experimental therapeutics.

Identification of a Benzoisoxazoloazepine Inhibitor (CPI-0610) of the Bromodomain and Extra-Terminal (BET) Family as a Candidate for Human Clinical Trials.

P. Sandy, Y. Leblanc, H. Jayaram, 2016, Journal of medicinal chemistry.

A series of C-Terminal amino alcohol dipeptide Aβ inhibitors

E. Thorsett, L. Latimer, J. Audia, 2002 .

A practical synthesis of indoles via a Pd-catalyzed C-N ring formation.

Y. Leblanc, Alexander M. Taylor, A. Côté, 2014, Organic letters.

Discovery and Optimization of Tetramethylpiperidinyl Benzamides as Inhibitors of EZH2.

P. Trojer, R. Cummings, L. Bergeron, 2014, ACS medicinal chemistry letters.

Early Drug‐Discovery Efforts towards the Identification of EP300/CBP Histone Acetyltransferase (HAT) Inhibitors

R. Cummings, R. Sims, J. Audia, 2020, ChemMedChem.

Chapter 11. Serotonin Modulators and Cardiovascular/Gastrointestinal Diseases

J. Audia, Marlene L. Cohen, 1991 .

[3H]LY334370, a novel radioligand for the 5-HT1F receptor. I. In vitro characterization of binding properties

J. Zgombick, J. Krushinski, D. Nelson, 2005, Naunyn-Schmiedeberg's Archives of Pharmacology.

Kinetic analysis of LY320236: competitive inhibitor of type I and non-competitive inhibitor of type II human steroid 5α-reductase

K. Bemis, B. Neubauer, J. Audia, 2000, The Journal of Steroid Biochemistry and Molecular Biology.

Characterization of type I 5α-reductase activity in DU145 human prostatic adenocarcinoma cells

N. Bruchovsky, Chung Lee, J. Krushinski, 1996, The Journal of Steroid Biochemistry and Molecular Biology.

LY191704: a selective, nonsteroidal inhibitor of human steroid 5 alpha-reductase type 1.

C. D. Jones, D. Russell, N. Stamm, 1993, Proceedings of the National Academy of Sciences of the United States of America.

LY191704 inhibits type I steroid 5 alpha-reductase in human scalp.

C. D. Jones, D. Tindall, B. Neubauer, 1996, The Journal of clinical endocrinology and metabolism.

Preparation and biological evaluation of BACE1 inhibitors: Leveraging trans-cyclopropyl moieties as ligand efficient conformational constraints.

D. Timm, L. L. Winneroski, P. May, 2019, Bioorganic & medicinal chemistry.

Preparation and biological evaluation of conformationally constrained BACE1 inhibitors.

D. Timm, L. L. Winneroski, P. May, 2015, Bioorganic & medicinal chemistry.

Responses of LNCaP prostatic adenocarcinoma cell cultures to LY300502, a benzoquinolinone human type I 5α‐reductase inhibitor

B. Neubauer, J. Audia, D. Sutkowski, 1996, The Prostate. Supplement.

Synthesis of two useful, enantiomerically pure derivatives of (S)-4-hydroxy-2-cyclohexenone

S. Danishefsky, J. Audia, A. Villalobos, 1989 .

GNE-064: A Potent, Selective, and Orally Bioavailable Chemical Probe for the Bromodomains of SMARCA2 and SMARCA4 and the Fifth Bromodomain of PBRM1.

A. Good, P. Sandy, Y. Leblanc, 2022, Journal of medicinal chemistry.

GNE-886: A Potent and Selective Inhibitor of the Cat Eye Syndrome Chromosome Region Candidate 2 Bromodomain (CECR2).

P. Sandy, H. Jayaram, R. Sims, 2017, ACS medicinal chemistry letters.

Identification of (R)-N-((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide (CPI-1205), a Potent and Selective Inhibitor of Histone Methyltransferase EZH2, Suitable for Phase I Clinical Trials for B-Cell Lymp

Jon R. Wilson, A. Good, P. Trojer, 2016, Journal of medicinal chemistry.

[3H]LY334370, a novel radioligand for the 5-HT1F receptor. II. Autoradiographic localization in rat, guinea pig, monkey and human brain

J. Krushinski, D. Nelson, J. Audia, 2005, Naunyn-Schmiedeberg's Archives of Pharmacology.

In Vivo Assessment of Brain Interstitial Fluid with Microdialysis Reveals Plaque-Associated Changes in Amyloid-β Metabolism and Half-Life

D. Holtzman, S. Paul, J. Cirrito, 2003, The Journal of Neuroscience.

"Pictet-Spengler-like" Synthesis of Tetrahydro-beta-carbolines under Hydrolytic Conditions. Direct Use of Azalactones as Phenylacetaldehyde Equivalents.

J. Audia, J. Nissen, D. Evrard, 1996, The Journal of organic chemistry.

Discovery, Design, and Optimization of Isoxazole Azepine BET Inhibitors.

P. Sandy, Y. Leblanc, H. Jayaram, 2013, ACS medicinal chemistry letters.

Potent, selective tetrahydro-beta-carboline antagonists of the serotonin 2B (5HT2B) contractile receptor in the rat stomach fundus.

D. Nelson, J. Audia, M. Cohen, 1996, Journal of medicinal chemistry.

Acyclic stereocontrol in catalyzed intramolecular Diels−Alder cyclizations leading to octahydronaphthalenecarboxaldehydes

J. Audia, J. A. Marshall, J. Grote, 1987 .

Total synthesis of the Fusarium toxin Equisetin : Proof of the stereochemical relationship of the tetramate and terpenoid sectors

S. Danishefsky, J. Audia, E. Turos, 1989 .

Diels-alder cyclization of 2,8,10-undecatrienals as a route to 1,2,3,4,4a,5,6,8a-octahydronaphthalenes

B. Shearer, J. Audia, J. A. Marshall, 1986 .

N-[3-(2-Dimethylaminoethyl)-2-methyl-1H- indol-5-yl]-4-fluorobenzamide: a potent, selective, and orally active 5-HT(1F) receptor agonist potentially useful for migraine therapy.

J. Zgombick, D. Nelson, J. Audia, 2001, Journal of medicinal chemistry.

Intramolecular Diels-Alder cyclization of conjugated aldehydes: synthesis of a chlorothricolide intermediate

J. Audia, J. A. Marshall, J. Grote, 1984 .

Stereoselective epoxidations and electrophilic additions to partial ergot alkaloids and conformationally-fixed styrenes. Experimental and theoretical modeling evidence for the importance of torsional steering as a stereocontrol element

K. Houk, M. Martinelli, Yundong Wu, 1994 .

Acyclic stereocontrol in catalyzed intramolecular Diels―Alder cyclizations of 4-methyl-2,8,10-undecatrienals

J. Audia, J. A. Marshall, J. Grote, 1986 .

An application of the ireland reaction to the stereospecific synthesis of fused carbocyclic systems.

S. Danishefsky, J. Audia, 1988 .

Conjugate addition of organocuprates to trans-4a,5,6,7,8,8a-hexahydronaphthalene-1-carboxaldehydes. Synthesis of a chlorothricin degradation product

B. Shearer, J. Audia, J. A. Marshall, 1986 .

Improved Preparation of (E)-3-Trimethylsilyl-2-Buten-1-OL

J. Audia, J. A. Marshall, 1983 .

Discovery of Benzotriazolo[4,3-d][1,4]diazepines as Orally Active Inhibitors of BET Bromodomains.

P. Sandy, Y. Leblanc, H. Jayaram, 2016, ACS medicinal chemistry letters.

The promise and peril of chemical probes.

John P. Overington, Jian Jin, Matthieu Schapira, 2015, Nature chemical biology.

LY 191704 : A selective , nonsteroidal inhibitor of human steroid 5 a-reductase type 1 ( 5 a-reductase / dihydrotestosterone / benzoquinolinone / benign prostatic hyperplasia )

C. D. Jones, D. Russell, N. Stamm, 2005 .

Erratum: The promise and peril of chemical probes (Nature Chemical Biology (2015) 11 (536-541))

John P. Overington, Jayme L. Dahlin, Christopher M. Austin, 2015 .

Classical and dynamic resolution of 1 -amino-3-methyl-1 ,3,4,5-tetrahydrobenzo[d]azepin-2-one

T. Koenig, J. Audia, D. Mitchell, 2005 .

Robust Central Reduction of Amyloid-β in Humans with an Orally Available, Non-Peptidic β-Secretase Inhibitor

James E Audia, R. Dean, T. Lindstrom, 2011, The Journal of Neuroscience.

Histone Modifications and Cancer.

James E Audia, R. Campbell, J. Audia, 2016, Cold Spring Harbor perspectives in biology.

Synthesis of the individual enantiomers of the benzoquinolinone human type 1 steroid 5-α-reductase inhibitors LY191704 and LY266111

J. Deeter, J. Audia, D. Lawhorn, 1993 .

Identification of potent, selective KDM5 inhibitors.

P. Trojer, P. Sandy, Y. Leblanc, 2016, Bioorganic & medicinal chemistry letters.

Functional gamma‐secretase inhibitors reduce beta‐amyloid peptide levels in brain

F. D. Miller, R. Motter, D. Kholodenko, 2000, Journal of neurochemistry.

Design, Synthesis, and Pharmacological Evaluation of Second Generation EZH2 Inhibitors with Long Residence Time.

P. Trojer, R. Sims, Shilpi Arora, 2020, ACS medicinal chemistry letters.

EZH2 inhibitor efficacy in non-Hodgkin's lymphoma does not require suppression of H3K27 monomethylation.

P. Trojer, Shilpi Arora, R. Cummings, 2014, Chemistry & biology.

Chapter 1. Recent Advances in Migraine Therapy

T. Branchek, J. Audia, 1997 .

Identification of EZH2 and EZH1 small molecule inhibitors with selective impact on diffuse large B cell lymphoma cell growth.

E. Chan, P. Trojer, P. Sandy, 2013, Chemistry & biology.

Pharmacological characteristics of the newly cloned rat 5-hydroxytryptamine2F receptor.

D. Nelson, J. Audia, M. Cohen, 1993, Molecular pharmacology.

Ilaprazole and Other Novel Prazole-Based Compounds That Bind Tsg101 Inhibit Viral Budding of Herpes Simplex Virus 1 and 2 and Human Immunodeficiency Virus from Cells

C. Luan, J. Audia, J. Leis, 2021, Journal of Virology.

Ilaprazole and other novel prazole-based compounds that bind Tsg101 inhibit viral budding of HSV-1/2 and HIV from cells

C. Luan, J. Audia, J. Leis, 2020, bioRxiv.

Amyloid β‐Mediated Oxidative and Metabolic Stress in Rat Cortical Neurons: No Direct Evidence for a Role for H2O2 Generation

R. Rydel, M. Wogulis, P. May, 1996, Journal of neurochemistry.

Regulatory T Cell Modulation by CBP/EP300 Bromodomain Inhibition*

G. Hatzivassiliou, P. Sandy, H. Jayaram, 2016, The Journal of Biological Chemistry.

The Potent BACE1 Inhibitor LY2886721 Elicits Robust Central Aβ Pharmacodynamic Responses in Mice, Dogs, and Humans

R. Dean, T. Lindstrom, D. Timm, 2015, The Journal of Neuroscience.

Central and Peripheral Pharmacokinetic and Pharmacodynamic Effects of the β-site APP Cleavage Enzyme (BACE1) Inhibitor LY2811376 In Humans

R. Dean, M. Citron, L. Ereshefsky, 2010, Alzheimer's & Dementia.

Discovery, design, and synthesis of indole-based EZH2 inhibitors.

A. Good, P. Trojer, R. Cummings, 2015, Bioorganic & medicinal chemistry letters.

Identification and characterization of second-generation EZH2 inhibitors with extended residence times and improved biological activity

P. Trojer, R. Sims, Shilpi Arora, 2021, The Journal of biological chemistry.

Design and Synthesis of Styrenylcyclopropylamine LSD1 Inhibitors.

A. Good, P. Trojer, R. Cummings, 2020, ACS medicinal chemistry letters.

Preclinical characterization of LY2886721: A BACE1 inhibitor in clinical development for early Alzheimer's disease

T. Lindstrom, M. Citron, P. May, 2012, Alzheimer's & Dementia.

Comparison of the effects of serotonin selective, norepinephrine selective, and dual serotonin and norepinephrine reuptake inhibitors on lower urinary tract function in cats.

K. Thor, J. Audia, M. Katofiasc, 2002, Life sciences.

Collaboration and knowledge integration for successful brain therapeutics – lessons learned from the pandemic

M. Loza, Sohini Chowdhury, C. Bountra, 2022, Disease models & mechanisms.

5‐HT1F receptor agonists inhibit neurogenic dural inflammation in guinea pigs

Kirk W. Johnson, T. Branchek, J. Zgombick, 1997, Neuroreport.

Comparison of desmethylsertraline with sertraline as a monoamine uptake inhibitor in vivo

R. Fuller, S. Hemrick-Luecke, J. Audia, 1995, Progress in Neuro-Psychopharmacology and Biological Psychiatry.

Nonsteroidal inhibitors of human type I steroid 5-alpha-reductase.

A. Pike, N. Stamm, B. Neubauer, 1993, Journal of medicinal chemistry.

P4-339 Stereoselective inhibition of amyloid beta peptide secretion by LY450139, a novel functional gamma secretase inhibitor

P. May, D. Mcclure, J. Audia, 2004, Neurobiology of Aging.

Synthesis and 5α-reductase inhibitory activity of 8-substituted benzo[ƒ]quinolinones derived from palladium mediated coupling reactions

B. Neubauer, J. Audia, V. P. Rocco, 1998 .

Synthesis and 5α‐Reductase Inhibitory Activity of 8‐Substituted Benzo[f]quinolinones Derived from Palladium Mediated Coupling Reactions.

B. Neubauer, J. Audia, E. C. Smith, 2010 .

Mentoring Matters in Drug Discovery.

M. Blanco, J. Audia, 2020, ACS medicinal chemistry letters.

QSAR study of benzoquinolinones as inhibitors of human type 1 5-α-reductase.

Charles David Jones, James H. Wikel, Kerry G. Bemis, 1993 .

Responses of LNCaP prostatic adenocarcinoma cell cultures to LY300502, a benzoquinolinone human type I 5α‐reductase inhibitor

B. Neubauer, J. Audia, K. Hsiao, 1996 .

P1-180 Reduction in a-beta(1-40) and A-beta(1-42) in CSF and plasma in the beagle dog following acute oral dosing of the gamma secretase inhibitor, LY450139

P. May, J. Audia, P. Hyslop, 2004, Neurobiology of Aging.

Discovery, Design, and Optimization of Isoxazole Azepine BET Inhibitors.

P. Sandy, Y. Leblanc, H. Jayaram, 2013, ACS medicinal chemistry letters.

The promise and peril of chemical probes (vol 11, pg 536, 2015)

John P. Overington, Jayme L. Dahlin, Christopher M. Austin, 2015 .

Identification of EZH2 and EZH1 small molecule inhibitors with selective impact on diffuse large B cell lymphoma cell growth.

E. Chan, P. Trojer, P. Sandy, 2013, Chemistry & biology.