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Alexander (Leggy) Arnold PhD

Professor

Institution: University of Wisconsin - Milwaukee
Department: Chemistry & Biochemistry

Publications (106)

Development and validation of an LC-MS/MS method for the determination of ARN14988, an acid ceramidase inhibitor, and its application to a pharmacokinetic study in a mouse model. (Rajaratnam V, Islam MM, Kub EF, Rajaratnam S, Kim KB, Rahman MT, Rashid F, Benko AM, Cook JM, Arnold LA, Mirza SP) Biomed Chromatogr 2023 Sep 26:e5754 PMID: 37750452 SCOPUS ID: 2-s2.0-85172152226 09/26/2023

Improved 2-pyridyl reductive homocoupling reaction using biorenewable solvent Cyrene™ (dihydrolevoglucosenone) (Webb DA, Alsudani Z, Xu G, Gao P, Arnold LA) RSC Sustainability 17 July 2023;1(6):1522-1529 SCOPUS ID: 2-s2.0-85172409681 07/17/2023

Design, Synthesis, and Biological Evaluation of Novel Spiro Imidazobenzodiazepines to Identify Improved Inhaled Bronchodilators. (Webb DA, Meyer MJ, Medubi KM, Tylek AS, Yocum GT, Roni MSR, Zahn NM, Swartwout SA, Masoud AK, Emala CW, Stafford DC, Arnold LA) J Med Chem 2023 Jul 27;66(14):9853-9865 PMID: 37418196 SCOPUS ID: 2-s2.0-85165680122 07/07/2023

Comparative anticonvulsant activity of the GABAkine KRM-II-81 and a deuterated analog. (Ping X, Meyer MJ, Zahn NM, Golani LK, Sharmin D, Pandey KP, Revanian S, Mondal P, Jin X, Arnold LA, Cerne R, Cook JM, Divović B, Savić MM, Lippa A, Smith JL, Witkin JM) Drug Dev Res 2023 May;84(3):527-531 PMID: 36748904 SCOPUS ID: 2-s2.0-85147501608 02/08/2023

Structural Analogs of the GABAkine KRM-II-81 Are Orally Bioavailable Anticonvulsants without Sedation. (Pandey KP, Divović B, Rashid F, Golani LK, Cerne R, Zahn NM, Meyer MJ, Arnold LA, Sharmin D, Mian MY, Smith JL, Ping X, Jin X, Lippa A, Tiruveedhula VVNPB, Cook JM, Savić MM, Witkin JM) J Pharmacol Exp Ther 2023 Apr;385(1):50-61 PMID: 36746611 PMCID: PMC10029819 SCOPUS ID: 2-s2.0-85150396986 02/07/2023 2 Citations

Imidazobenzodiazepine PI320 Relaxes Mouse Peripheral Airways by Inhibiting Calcium Mobilization. (Perez-Zoghbi JF, Sajorda DR, Webb DA, Arnold LA, Emala CW, Yocum GT) Am J Respir Cell Mol Biol 2022 Oct;67(4):482-490 PMID: 35776523 PMCID: PMC9564932 SCOPUS ID: 2-s2.0-85139536374 07/02/2022 1 Citation

Oral and Inhaled Fosamprenavir Reverses Pepsin-Induced Damage in a Laryngopharyngeal Reflux Mouse Model. (Johnston N, Samuels TL, Goetz CJ, Arnold LA, Smith BC, Seabloom D, Wuertz B, Ondrey F, Wiedmann TS, Vuksanovic N, Silvaggi NR, MacKinnon AC, Miller J, Bock J, Blumin JH) Laryngoscope 2023 Jan;133 Suppl 1(Suppl 1):S1-S11 PMID: 35678265 PMCID: PMC9732152 SCOPUS ID: 2-s2.0-85131512635 06/10/2022 3 Citations

Identification of a Vitamin-D Receptor Antagonist, MeTC7, which Inhibits the Growth of Xenograft and Transgenic Tumors In Vivo. (Khazan N, Kim KK, Hansen JN, Singh NA, Moore T, Snyder CWA, Pandita R, Strawderman M, Fujihara M, Takamura Y, Jian Y, Battaglia N, Yano N, Teramoto Y, Arnold LA, Hopson R, Kishor K, Nayak S, Ojha D, Sharon A, Ashton JM, Wang J, Milano MT, Miyamoto H, Linehan DC, Gerber SA, Kawar N, Singh AP, Tabdanov ED, Dokholyan NV, Kakuta H, Jurutka PW, Schor NF, Rowswell-Turner RB, Singh RK, Moore RG) J Med Chem 2022 Apr 28;65(8):6039-6055 PMID: 35404047 PMCID: PMC9059124 SCOPUS ID: 2-s2.0-85129087648 04/12/2022 2 Citations

Comparative pharmacodynamic and pharmacokinetic study of MIDD0301 and its (S) enantiomer. (Rashid Roni MS, Zahn NM, Yocum GT, Webb DA, Mian MY, Meyer MJ, Tylek AS, Cook JM, Emala CW, Stafford DC, Arnold LA) Drug Dev Res 2022 Jun;83(4):979-992 PMID: 35246861 PMCID: PMC9246881 SCOPUS ID: 2-s2.0-85125563573 03/06/2022 1 Citation

Metabolism, pharmacokinetics, and anticonvulsant activity of a deuterated analog of the α2/3-selective GABAkine KRM-II-81. (Golani LK, Divović B, Sharmin D, Pandey KP, Mian MY, Cerne R, Zahn NM, Meyer MJ, Tiruveedhula VVNPB, Smith JL, Ping X, Jin X, Lippa A, Schkeryantz JM, Arnold LA, Cook JM, Savić MM, Witkin JM) Biopharm Drug Dispos 2022 Apr;43(2):66-75 PMID: 35194800 SCOPUS ID: 2-s2.0-85126005718 02/24/2022 2 Citations

Development of Inhaled GABA_A Receptor Modulators to Improve Airway Function in Bronchoconstrictive Disorders. (Zahn NM, Roni MSR, Yocum GT, Meyer MJ, Webb DA, Mian MY, Cook JM, Stafford DC, Emala CW, Arnold LA) ACS Pharmacol Transl Sci 2022 Feb 11;5(2):80-88 PMID: 35187417 PMCID: PMC8844962 SCOPUS ID: 2-s2.0-85124662302 02/22/2022 3 Citations

Development of a Novel, Small-Molecule Brain-Penetrant Histone Deacetylase Inhibitor That Enhances Spatial Memory Formation in Mice. (Belayet JB, Beamish S, Rahaman M, Alanani S, Virdi RS, Frick DN, Rahman AFMT, Ulicki JS, Biswas S, Arnold LA, Roni MSR, Cheng EY, Steeber DA, Frick KM, Hossain MM) J Med Chem 2022 Feb 24;65(4):3388-3403 PMID: 35133171 PMCID: PMC9135144 SCOPUS ID: 2-s2.0-85124901172 02/09/2022 2 Citations

Identification and Quantification of MIDD0301 Metabolites. (Roni MSR, Zahn NM, Mikulsky BN, Webb DA, Mian MY, Knutson DE, Guthrie ML, Cook JM, Stafford DC, Arnold LA) Curr Drug Metab 2021;22(14):1114-1123 PMID: 34856893 PMCID: PMC8760168 SCOPUS ID: 2-s2.0-85123651139 12/04/2021 2 Citations

Strategies for the design of vitamin D receptor ligands (Mutchie TR, Webb DA, Milo ES, Arnold LA) Nuclear Receptors: The Art and Science of Modulator Design and Discovery 28 September 2021:199-217 SCOPUS ID: 2-s2.0-85164873600 09/28/2021

Biological evaluation and synthesis of calcitroic acid. (Yu OB, Webb DA, Di Milo ES, Mutchie TR, Teske KA, Chen T, Lin W, Peluso-Iltis C, Rochel N, Helmstädter M, Merk D, Arnold LA) Bioorg Chem 2021 Nov;116:105310 PMID: 34482171 PMCID: PMC8592288 SCOPUS ID: 2-s2.0-85114182880 09/06/2021 3 Citations

Assessment of Phenylboronic Acid Nitrogen Mustards as Potent and Selective Drug Candidates for Triple-Negative Breast Cancer. (Fan H, Zaman MAU, Chen W, Ali T, Campbell A, Zhang Q, Setu NI, Saxon E, Zahn NM, Benko AM, Arnold LA, Peng X) ACS Pharmacol Transl Sci 2021 Apr 09;4(2):687-702 PMID: 33860194 PMCID: PMC8033613 SCOPUS ID: 2-s2.0-85103481264 04/17/2021 6 Citations

Nebulized MIDD0301 Reduces Airway Hyperresponsiveness in Moderate and Severe Murine Asthma Models. (Zahn NM, Mikulsky BN, Roni MSR, Yocum GT, Mian MY, Knutson DE, Cook JM, Emala CW, Stafford DC, Arnold LA) ACS Pharmacol Transl Sci 2020 Dec 11;3(6):1381-1390 PMID: 33344908 PMCID: PMC7737320 SCOPUS ID: 2-s2.0-85097890423 12/22/2020 5 Citations

Design, synthesis and characterization of novel gamma‑aminobutyric acid type A receptor ligands (Pandey KP, Ahmed Khan MZ, Golani LK, Mondal P, Mian MY, Rashid F, Phani Babu Tiruveedhula VVN, Knutson DE, Zahn NM, Arnold LA, Witkin JM, Cook JM) Arkivoc 2 December 2020;2020(7):242-256 SCOPUS ID: 2-s2.0-85098770969 12/02/2020 4 Citations

Improved scale-up synthesis and purification of clinical asthma candidate MIDD0301. (Knutson DE, Roni R, Mian Y, Cook JM, Stafford DC, Arnold LA) Org Process Res Dev 2020 Aug 21;24(8):1467-1476 PMID: 32952391 PMCID: PMC7497793 SCOPUS ID: 2-s2.0-85096203696 09/22/2020 7 Citations

A Structure-Activity Relationship Comparison of Imidazodiazepines Binding at Kappa, Mu, and Delta Opioid Receptors and the GABA_A Receptor. (Li G, Nieman AN, Mian MY, Zahn NM, Mikulsky BN, Poe MM, Methuku KR, Liu Y, Cook JM, Stafford DC, Arnold LA) Molecules 2020 Aug 25;25(17) PMID: 32854311 PMCID: PMC7503500 SCOPUS ID: 2-s2.0-85090013186 08/29/2020 8 Citations

Targeting Nitric Oxide Production in Microglia with Novel Imidazodiazepines for Nonsedative Pain Treatment. (Nieman AN, Li G, Zahn NM, Mian MY, Mikulsky BN, Hoffman DA, Wilcox TM, Kehoe AS, Luecke IW, Poe MM, Alvarez-Carbonell D, Cook JM, Stafford DC, Arnold LA) ACS Chem Neurosci 2020 Jul 01;11(13):2019-2030 PMID: 32511908 PMCID: PMC7380323 SCOPUS ID: 2-s2.0-85087466986 06/09/2020 5 Citations

The Effects of pH on the Structure and Bioavailability of Imidazobenzodiazepine-3-Carboxylate MIDD0301. (Roni MSR, Li G, Mikulsky BN, Knutson DE, Mian MY, Zahn NM, Cook JM, Stafford DC, Arnold LA) Mol Pharm 2020 Apr 06;17(4):1182-1192 PMID: 32069056 PMCID: PMC7216793 SCOPUS ID: 2-s2.0-85083042068 02/19/2020 5 Citations

Design, synthesis and characterization of novel gamma‑aminobutyric acid type A receptor ligands. (Pandey KP, Khan ZA, Golani LK, Mondal P, Mian Y, Rashid F, Tiruveedhula VVNPB, Knutson DE, Sharmin D, Ahmed T, Rezvanian S, Zahn NM, Arnold LA, Witkin JM, Cook JM) ARKIVOC 2020;2020(Pt 7):242-256 PMID: 33642954 PMCID: PMC7909486 01/01/2020

Synthesis and biological evaluation of calcioic acid. (Yu OB, Mutchie TR, Di Milo ES, Arnold LA) Steroids 2020 Feb;154:108536 PMID: 31704333 PMCID: PMC6980330 SCOPUS ID: 2-s2.0-85075280378 11/11/2019 2 Citations

An anthrone-based Kv7.2/7.3 channel blocker with improved properties for the investigation of psychiatric and neurodegenerative disorders. (Porter JD, Vivas O, Weaver CD, Alsafran A, DiMilo E, Arnold LA, Dickson EJ, Dockendorff C) Bioorg Med Chem Lett 2019 Dec 01;29(23):126681 PMID: 31668424 PMCID: PMC6858848 SCOPUS ID: 2-s2.0-85074462524 11/02/2019 4 Citations

Correction to "A Novel Orally Available Asthma Drug Candidate That Reduces Smooth Muscle Constriction and Inflammation by Targeting GABA_A Receptors in the Lung". (Forkuo GS, Nieman AN, Kodali R, Zahn NM, Li G, Roni MSR, Stephen MR, Harris TW, Jahan R, Guthrie ML, Yu OB, Fisher JL, Yocum GT, Emala CW, Steeber DA, Stafford DC, Cook JM, Arnold LA) Mol Pharm 2019 Nov 04;16(11):4756 PMID: 31633359 SCOPUS ID: 2-s2.0-85074213063 10/22/2019

The parmodulin NRD-21 is an allosteric inhibitor of PAR1 Gq signaling with improved anti-inflammatory activity and stability. (Gandhi DM, Rosas R Jr, Greve E, Kentala K, D-R Diby N, Snyder VA, Stephans A, Yeung THW, Subramaniam S, DiMilo E, Kurtenbach KE, Arnold LA, Weiler H, Dockendorff C) Bioorg Med Chem 2019 Sep 01;27(17):3788-3796 PMID: 31320211 PMCID: PMC6706283 SCOPUS ID: 2-s2.0-85068855508 07/20/2019 5 Citations

Novel Benzodiazepine-Like Ligands with Various Anxiolytic, Antidepressant, or Pro-Cognitive Profiles. (Prevot TD, Li G, Vidojevic A, Misquitta KA, Fee C, Santrac A, Knutson DE, Stephen MR, Kodali R, Zahn NM, Arnold LA, Scholze P, Fisher JL, Marković BD, Banasr M, Cook JM, Savic M, Sibille E) Mol Neuropsychiatry 2019 Apr;5(2):84-97 PMID: 31192221 PMCID: PMC6528097 06/14/2019

MIDD0301 - A first-in-class anti-inflammatory asthma drug targets GABA_A receptors without causing systemic immune suppression. (Zahn NM, Huber AT, Mikulsky BN, Stepanski ME, Kehoe AS, Li G, Schussman M, Rashid Roni MS, Kodali R, Cook JM, Stafford DC, Steeber DA, Arnold LA) Basic Clin Pharmacol Toxicol 2019 Jul;125(1):75-84 PMID: 30694594 PMCID: PMC6565495 SCOPUS ID: 2-s2.0-85067227062 01/30/2019 10 Citations

Design and Evaluation of Heterobivalent PAR1-PAR2 Ligands as Antagonists of Calcium Mobilization. (Majewski MW, Gandhi DM, Rosas R Jr, Kodali R, Arnold LA, Dockendorff C) ACS Med Chem Lett 2019 Jan 10;10(1):121-126 PMID: 30655958 PMCID: PMC6331166 SCOPUS ID: 2-s2.0-85058668129 01/19/2019 9 Citations

Alternative binding sites at the vitamin D receptor and their ligands. (Mutchie TR, Yu OB, Di Milo ES, Arnold LA) Mol Cell Endocrinol 2019 Apr 05;485:1-8 PMID: 30654005 PMCID: PMC6444937 SCOPUS ID: 2-s2.0-85061138821 01/18/2019 12 Citations

A novel GABA_A receptor ligand MIDD0301 with limited blood-brain barrier penetration relaxes airway smooth muscle ex vivo and in vivo. (Yocum GT, Perez-Zoghbi JF, Danielsson J, Kuforiji AS, Zhang Y, Li G, Rashid Roni MS, Kodali R, Stafford DC, Arnold LA, Cook JM, Emala CW Sr) Am J Physiol Lung Cell Mol Physiol 2019 Feb 01;316(2):L385-L390 PMID: 30489155 PMCID: PMC6397346 SCOPUS ID: 2-s2.0-85060942334 11/30/2018 12 Citations

Discovery and Optimization of Novel Hydrogen Peroxide Activated Aromatic Nitrogen Mustard Derivatives as Highly Potent Anticancer Agents. (Chen W, Fan H, Balakrishnan K, Wang Y, Sun H, Fan Y, Gandhi V, Arnold LA, Peng X) J Med Chem 2018 Oct 25;61(20):9132-9145 PMID: 30247905 SCOPUS ID: 2-s2.0-85054882189 09/25/2018 39 Citations

A high-throughput screening assay for pyruvate carboxylase. (Wyatt BN, Arnold LA, St Maurice M) Anal Biochem 2018 Jun 01;550:90-98 PMID: 29655770 SCOPUS ID: 2-s2.0-85046152441 04/16/2018 4 Citations

A Novel Orally Available Asthma Drug Candidate That Reduces Smooth Muscle Constriction and Inflammation by Targeting GABA_A Receptors in the Lung. (Forkuo GS, Nieman AN, Kodali R, Zahn NM, Li G, Rashid Roni MS, Stephen MR, Harris TW, Jahan R, Guthrie ML, Yu OB, Fisher JL, Yocum GT, Emala CW, Steeber DA, Stafford DC, Cook JM, Arnold LA) Mol Pharm 2018 May 07;15(5):1766-1777 PMID: 29578347 PMCID: PMC5954213 SCOPUS ID: 2-s2.0-85046694256 03/27/2018 27 Citations

Design and Synthesis of Novel Deuterated Ligands Functionally Selective for the γ-Aminobutyric Acid Type A Receptor (GABA_AR) α6 Subtype with Improved Metabolic Stability and Enhanced Bioavailability. (Knutson DE, Kodali R, Divović B, Treven M, Stephen MR, Zahn NM, Dobričić V, Huber AT, Meirelles MA, Verma RS, Wimmer L, Witzigmann C, Arnold LA, Chiou LC, Ernst M, Mihovilovic MD, Savić MM, Sieghart W, Cook JM) J Med Chem 2018 Mar 22;61(6):2422-2446 PMID: 29481759 PMCID: PMC6941172 SCOPUS ID: 2-s2.0-85044203204 02/27/2018 27 Citations

Synthesis of chiral GABA_A receptor subtype selective ligands as potential agents to treat schizophrenia as well as depression. (Li G, Stephen MR, Kodali R, Zahn NM, Poe MM, Tiruveedhula VVNPB, Huber AT, Schussman MK, Qualmann K, Panhans CM, Raddatz NJ, Baker DA, Prevot TD, Banasr M, Sibille E, Arnold LA, Cook JM) ARKIVOC 2018;2018(4):158-182 PMID: 32774192 PMCID: PMC7413308 SCOPUS ID: 2-s2.0-85048931124 01/01/2018 11 Citations

Novel VDR antagonists based on the GW0742 scaffold. (Teske KA, Bogart JW, Arnold LA) Bioorg Med Chem Lett 2018 Feb 01;28(3):351-354 PMID: 29287957 PMCID: PMC6008168 SCOPUS ID: 2-s2.0-85039071345 12/31/2017 7 Citations

Modulating Vitamin D Receptor-Coregulator Binding With Small Molecules (Yu OB, Arnold LA) Vitamin D: Fourth Edition 14 December 2017;2:657-666 SCOPUS ID: 2-s2.0-85054944896 12/14/2017 1 Citation

Parallel Chemistry Approach to Identify Novel Nuclear Receptor Ligands Based on the GW0742 Scaffold. (Teske KA, Rai G, Nandhikonda P, Sidhu PS, Feleke B, Simeonov A, Yasgar A, Jadhav A, Maloney DJ, Arnold LA) ACS Comb Sci 2017 Oct 09;19(10):646-656 PMID: 28825467 PMCID: PMC5643073 SCOPUS ID: 2-s2.0-85030765458 08/22/2017 2 Citations

Further evaluation of the potential anxiolytic activity of imidazo[1,5-a][1,4]diazepin agents selective for α2/3-containing GABA_A receptors. (Witkin JM, Cerne R, Wakulchik M, S J, Gleason SD, Jones TM, Li G, Arnold LA, Li JX, Schkeryantz JM, Methuku KR, Cook JM, Poe MM) Pharmacol Biochem Behav 2017 Jun;157:35-40 PMID: 28442369 PMCID: PMC5519285 SCOPUS ID: 2-s2.0-85019841584 04/27/2017 20 Citations

Alleviation of Multiple Asthmatic Pathologic Features with Orally Available and Subtype Selective GABA_A Receptor Modulators. (Forkuo GS, Nieman AN, Yuan NY, Kodali R, Yu OB, Zahn NM, Jahan R, Li G, Stephen MR, Guthrie ML, Poe MM, Hartzler BD, Harris TW, Yocum GT, Emala CW, Steeber DA, Stafford DC, Cook JM, Arnold LA) Mol Pharm 2017 Jun 05;14(6):2088-2098 PMID: 28440659 PMCID: PMC5497587 SCOPUS ID: 2-s2.0-85020166818 04/26/2017 25 Citations

Hydrogen peroxide activated quinone methide precursors with enhanced DNA cross-linking capability and cytotoxicity towards cancer cells. (Wang Y, Fan H, Balakrishnan K, Lin Z, Cao S, Chen W, Fan Y, Guthrie QA, Sun H, Teske KA, Gandhi V, Arnold LA, Peng X) Eur J Med Chem 2017 Jun 16;133:197-207 PMID: 28388522 PMCID: PMC5652303 SCOPUS ID: 2-s2.0-85016812733 04/08/2017 26 Citations

Identification of a novel, fast-acting GABAergic antidepressant. (McMurray KMJ, Ramaker MJ, Barkley-Levenson AM, Sidhu PS, Elkin PK, Reddy MK, Guthrie ML, Cook JM, Rawal VH, Arnold LA, Dulawa SC, Palmer AA) Mol Psychiatry 2018 Feb;23(2):384-391 PMID: 28322281 PMCID: PMC5608625 SCOPUS ID: 2-s2.0-85015625674 03/23/2017 28 Citations

Pharmacological and antihyperalgesic properties of the novel α2/3 preferring GABA_A receptor ligand MP-III-024. (Fischer BD, Schlitt RJ, Hamade BZ, Rehman S, Ernst M, Poe MM, Li G, Kodali R, Arnold LA, Cook JM) Brain Res Bull 2017 May;131:62-69 PMID: 28267561 PMCID: PMC5501353 SCOPUS ID: 2-s2.0-85016137378 03/08/2017 21 Citations

Synthesis and Characterization of a Novel γ-Aminobutyric Acid Type A (GABA_A) Receptor Ligand That Combines Outstanding Metabolic Stability, Pharmacokinetics, and Anxiolytic Efficacy. (Poe MM, Methuku KR, Li G, Verma AR, Teske KA, Stafford DC, Arnold LA, Cramer JW, Jones TM, Cerne R, Krambis MJ, Witkin JM, Jambrina E, Rehman S, Ernst M, Cook JM, Schkeryantz JM) J Med Chem 2016 Dec 08;59(23):10800-10806 PMID: 27933953 PMCID: PMC5215686 SCOPUS ID: 2-s2.0-85003442743 12/10/2016 35 Citations

Optimization of substituted imidazobenzodiazepines as novel asthma treatments. (Jahan R, Stephen MR, Forkuo GS, Kodali R, Guthrie ML, Nieman AN, Yuan NY, Zahn NM, Poe MM, Li G, Yu OB, Yocum GT, Emala CW, Stafford DC, Cook JM, Arnold LA) Eur J Med Chem 2017 Jan 27;126:550-560 PMID: 27915170 PMCID: PMC5253108 SCOPUS ID: 2-s2.0-85000671290 12/05/2016 16 Citations

Calcitroic Acid-A Review. (Yu OB, Arnold LA) ACS Chem Biol 2016 Oct 21;11(10):2665-2672 PMID: 27574921 PMCID: PMC5074857 SCOPUS ID: 2-s2.0-84992184192 10/22/2016 28 Citations

Characterization of GABA_A receptor ligands with automated patch-clamp using human neurons derived from pluripotent stem cells. (Yuan NY, Poe MM, Witzigmann C, Cook JM, Stafford D, Arnold LA) J Pharmacol Toxicol Methods 2016;82:109-114 PMID: 27544543 PMCID: PMC5116268 SCOPUS ID: 2-s2.0-84989944608 10/18/2016 10 Citations

Development of GABAA Receptor Subtype-Selective Imidazobenzodiazepines as Novel Asthma Treatments. (Forkuo GS, Guthrie ML, Yuan NY, Nieman AN, Kodali R, Jahan R, Stephen MR, Yocum GT, Treven M, Poe MM, Li G, Yu OB, Hartzler BD, Zahn NM, Ernst M, Emala CW, Stafford DC, Cook JM, Arnold LA) Mol Pharm 2016 Jun 06;13(6):2026-38 PMID: 27120014 PMCID: PMC4899155 SCOPUS ID: 2-s2.0-84973661516 04/28/2016 24 Citations

Inhibitors for the Vitamin D Receptor-Coregulator Interaction. (Teske KA, Yu O, Arnold LA) Vitam Horm 2016;100:45-82 PMID: 26827948 PMCID: PMC4740976 SCOPUS ID: 2-s2.0-84964627234 02/02/2016 6 Citations

Synthesis and evaluation of vitamin D receptor-mediated activities of cholesterol and vitamin D metabolites. (Teske KA, Bogart JW, Sanchez LM, Yu OB, Preston JV, Cook JM, Silvaggi NR, Bikle DD, Arnold LA) Eur J Med Chem 2016 Feb 15;109:238-46 PMID: 26774929 PMCID: PMC4737989 SCOPUS ID: 2-s2.0-84954311265 01/18/2016 15 Citations

Genetic and pharmacological manipulation of glyoxalase 1 regulates voluntary ethanol consumption in mice. (McMurray KM, Sidhu PS, Cook JM, Arnold LA, Palmer AA) Addict Biol 2017 Mar;22(2):381-389 PMID: 26691867 PMCID: PMC4917470 SCOPUS ID: 2-s2.0-84952333628 12/23/2015 9 Citations

A Review of the Updated Pharmacophore for the Alpha 5 GABA(A) Benzodiazepine Receptor Model. (Clayton T, Poe MM, Rallapalli S, Biawat P, Savić MM, Rowlett JK, Gallos G, Emala CW, Kaczorowski CC, Stafford DC, Arnold LA, Cook JM) Int J Med Chem 2015;2015:430248 PMID: 26682068 PMCID: PMC4657098 12/19/2015

Antitumor Activity of 3-Indolylmethanamines 31B and PS121912. (Guthrie ML, Sidhu PS, Hill EK, Horan TC, Nandhikonda P, Teske KA, Yuan NY, Sidorko M, Rodali R, Cook JM, Han L, Silvaggi NR, Bikle DD, Moore RG, Singh RK, Arnold LA) Anticancer Res 2015 Nov;35(11):6001-7 PMID: 26504023 PMCID: PMC4633305 SCOPUS ID: 2-s2.0-84946067038 10/28/2015 6 Citations

Modulation of Transcription mediated by the Vitamin D Receptor and the Peroxisome Proliferator-Activated Receptor δ in the presence of GW0742 analogs. (Teske K, Nandhikonda P, Bogart JW, Feleke B, Sidhu P, Yuan N, Preston J, Goy R, Arnold LA) J Biomol Res Ther 2014;3(1) PMID: 25485183 PMCID: PMC4255951 12/09/2014

IDENTIFICATION OF VDR ANTAGONISTS AMONG NUCLEAR RECEPTOR LIGANDS USING VIRTUAL SCREENING. (Teske K, Nandhikonda P, Bogart JW, Feleke B, Sidhu P, Yuan N, Preston J, Goy R, Han L, Silvaggi NR, Singh RK, Bikle DD, Cook JM, Arnold LA) Nucl Receptor Res 2014;1 PMID: 25419525 PMCID: PMC4240308 11/25/2014

Anticancer activity of VDR-coregulator inhibitor PS121912. (Sidhu PS, Teske K, Feleke B, Yuan NY, Guthrie ML, Fernstrum GB, Vyas ND, Han L, Preston J, Bogart JW, Silvaggi NR, Cook JM, Singh RK, Bikle DD, Arnold LA) Cancer Chemother Pharmacol 2014 Oct;74(4):787-98 PMID: 25107568 PMCID: PMC4177010 SCOPUS ID: 2-s2.0-84939871260 08/12/2014 17 Citations

Development of novel Vitamin D Receptor-Coactivator Inhibitors. (Sidhu PS, Nassif N, McCallum MM, Teske K, Feleke B, Yuan NY, Nandhikonda P, Cook JM, Singh RK, Bikle DD, Arnold LA) ACS Med Chem Lett 2014 Feb 13;5(2):199-204 PMID: 24799995 PMCID: PMC4007349 SCOPUS ID: 2-s2.0-84894094945 05/07/2014 22 Citations

Glo1 inhibitors for neuropsychiatric and anti-epileptic drug development. (McMurray KM, Distler MG, Sidhu PS, Cook JM, Arnold LA, Palmer AA, Plant LD) Biochem Soc Trans 2014 Apr;42(2):461-7 PMID: 24646261 PMCID: PMC4036232 SCOPUS ID: 2-s2.0-84896922293 03/22/2014 19 Citations

A fluorescence-based high throughput assay for the determination of small molecule-human serum albumin protein binding. (McCallum MM, Pawlak AJ, Shadrick WR, Simeonov A, Jadhav A, Yasgar A, Maloney DJ, Arnold LA) Anal Bioanal Chem 2014 Mar;406(7):1867-75 PMID: 24390461 PMCID: PMC3959589 SCOPUS ID: 2-s2.0-84898039403 01/07/2014 26 Citations

PT19c, Another Nonhypercalcemic Vitamin D2 Derivative, Demonstrates Antitumor Efficacy in Epithelial Ovarian and Endometrial Cancer Models. (Kawar N, Maclaughlan S, Horan TC, Uzun A, Lange TS, Kim KK, Hopson R, Singh AP, Sidhu PS, Glass KA, Shaw S, Padbury JF, Vorsa N, Arnold LA, Moore RG, Brard L, Singh RK) Genes Cancer 2013 Nov;4(11-12):524-34 PMID: 24386512 PMCID: PMC3877664 SCOPUS ID: 2-s2.0-84891507095 01/05/2014 7 Citations

Peroxisome proliferation-activated receptor δ agonist GW0742 interacts weakly with multiple nuclear receptors, including the vitamin D receptor. (Nandhikonda P, Yasgar A, Baranowski AM, Sidhu PS, McCallum MM, Pawlak AJ, Teske K, Feleke B, Yuan NY, Kevin C, Bikle DD, Ayers SD, Webb P, Rai G, Simeonov A, Jadhav A, Maloney D, Arnold LA) Biochemistry 2013 Jun 18;52(24):4193-203 PMID: 23713684 PMCID: PMC3724348 SCOPUS ID: 2-s2.0-84879205984 05/30/2013 20 Citations

High-throughput identification of promiscuous inhibitors from screening libraries with the use of a thiol-containing fluorescent probe. (McCallum MM, Nandhikonda P, Temmer JJ, Eyermann C, Simeonov A, Jadhav A, Yasgar A, Maloney D, Arnold AL) J Biomol Screen 2013 Jul;18(6):705-13 PMID: 23446699 PMCID: PMC3692575 SCOPUS ID: 2-s2.0-84879484816 03/01/2013 21 Citations

Identification and analysis of hepatitis C virus NS3 helicase inhibitors using nucleic acid binding assays. (Mukherjee S, Hanson AM, Shadrick WR, Ndjomou J, Sweeney NL, Hernandez JJ, Bartczak D, Li K, Frankowski KJ, Heck JA, Arnold LA, Schoenen FJ, Frick DN) Nucleic Acids Res 2012 Sep 01;40(17):8607-21 PMID: 22740655 PMCID: PMC3458564 SCOPUS ID: 2-s2.0-84866952771 06/29/2012 48 Citations

Comparison of cell expression formats for the characterization of GABA(A) channels using a microfluidic patch clamp system. (Chen Q, Yim PD, Yuan N, Johnson J, Cook JM, Smith S, Ionescu-Zanetti C, Wang ZJ, Arnold LA, Emala CW) Assay Drug Dev Technol 2012 Aug;10(4):325-35 PMID: 22574655 PMCID: PMC3419985 SCOPUS ID: 2-s2.0-84865449180 05/12/2012 7 Citations

Discovery of the first irreversible small molecule inhibitors of the interaction between the vitamin D receptor and coactivators. (Nandhikonda P, Lynt WZ, McCallum MM, Ara T, Baranowski AM, Yuan NY, Pearson D, Bikle DD, Guy RK, Arnold LA) J Med Chem 2012 May 24;55(10):4640-51 PMID: 22563729 PMCID: PMC3364162 SCOPUS ID: 2-s2.0-84861489999 05/09/2012 39 Citations

Efficacy of a non-hypercalcemic vitamin-D2 derived anti-cancer agent (MT19c) and inhibition of fatty acid synthesis in an ovarian cancer xenograft model. (Moore RG, Lange TS, Robinson K, Kim KK, Uzun A, Horan TC, Kawar N, Yano N, Chu SR, Mao Q, Brard L, DePaepe ME, Padbury JF, Arnold LA, Brodsky A, Shen TL, Singh RK) PLoS One 2012;7(4):e34443 PMID: 22509304 PMCID: PMC3317945 SCOPUS ID: 2-s2.0-84859248610 04/18/2012 12 Citations

An integrated in vitro and in vivo high-throughput screen identifies treatment leads for ependymoma. (Atkinson JM, Shelat AA, Carcaboso AM, Kranenburg TA, Arnold LA, Boulos N, Wright K, Johnson RA, Poppleton H, Mohankumar KM, Féau C, Phoenix T, Gibson P, Zhu L, Tong Y, Eden C, Ellison DW, Priebe W, Koul D, Yung WK, Gajjar A, Stewart CF, Guy RK, Gilbertson RJ) Cancer Cell 2011 Sep 13;20(3):384-99 PMID: 21907928 PMCID: PMC3172881 SCOPUS ID: 2-s2.0-80052569769 09/13/2011 91 Citations

Similarities and differences between two modes of antagonism of the thyroid hormone receptor. (Sadana P, Hwang JY, Attia RR, Arnold LA, Neale G, Guy RK) ACS Chem Biol 2011 Oct 21;6(10):1096-106 PMID: 21815645 PMCID: PMC3199310 SCOPUS ID: 2-s2.0-80054988658 08/06/2011 12 Citations

Evaluation of the first Ergocalciferol-derived, non hypercalcemic anti-cancer agent MT19c in ovarian cancer SKOV-3 cell lines. (Brard L, Lange TS, Robison K, Kim KK, Ara T, McCallum MM, Arnold LA, Moore RG, Singh RK) Gynecol Oncol 2011 Nov;123(2):370-8 PMID: 21803404 SCOPUS ID: 2-s2.0-80054771437 08/02/2011 12 Citations

Ligand competition binding assay for the androgen receptor. (Féau C, Arnold LA, Kosinski A, Guy RK) Methods Mol Biol 2011;776:59-68 PMID: 21796520 SCOPUS ID: 2-s2.0-80052952709 07/29/2011 4 Citations

A quantitative high-throughput screen identifies novel inhibitors of the interaction of thyroid receptor beta with a peptide of steroid receptor coactivator 2. (Johnson RL, Hwang JY, Arnold LA, Huang R, Wichterman J, Augustinaite I, Austin CP, Inglese J, Guy RK, Huang W) J Biomol Screen 2011 Jul;16(6):618-27 PMID: 21482722 PMCID: PMC3162318 SCOPUS ID: 2-s2.0-79960549182 04/13/2011 14 Citations

Methylsulfonylnitrobenzoates, a new class of irreversible inhibitors of the interaction of the thyroid hormone receptor and its obligate coactivators that functionally antagonizes thyroid hormone. (Hwang JY, Huang W, Arnold LA, Huang R, Attia RR, Connelly M, Wichterman J, Zhu F, Augustinaite I, Austin CP, Inglese J, Johnson RL, Guy RK) J Biol Chem 2011 Apr 08;286(14):11895-908 PMID: 21321127 PMCID: PMC3069392 SCOPUS ID: 2-s2.0-79953303428 02/16/2011 30 Citations

Differential regulation of epidermal function by VDR coactivators. (Bikle DD, Teichert A, Arnold LA, Uchida Y, Elias PM, Oda Y) J Steroid Biochem Mol Biol 2010 Jul;121(1-2):308-13 PMID: 20298785 PMCID: PMC2906691 SCOPUS ID: 2-s2.0-77954759467 03/20/2010 22 Citations

Identification and characterization of the first small molecule inhibitor of MDMX. (Reed D, Shen Y, Shelat AA, Arnold LA, Ferreira AM, Zhu F, Mills N, Smithson DC, Regni CA, Bashford D, Cicero SA, Schulman BA, Jochemsen AG, Guy RK, Dyer MA) J Biol Chem 2010 Apr 02;285(14):10786-96 PMID: 20080970 PMCID: PMC2856285 SCOPUS ID: 2-s2.0-77951224332 01/19/2010 175 Citations

Novel flufenamic acid analogues as inhibitors of androgen receptor mediated transcription. (Féau C, Arnold LA, Kosinski A, Zhu F, Connelly M, Guy RK) ACS Chem Biol 2009 Oct 16;4(10):834-43 PMID: 19645433 PMCID: PMC2763043 SCOPUS ID: 2-s2.0-70350153884 08/04/2009 22 Citations

Inhibition of a viral enzyme by a small-molecule dimer disruptor. (Shahian T, Lee GM, Lazic A, Arnold LA, Velusamy P, Roels CM, Guy RK, Craik CS) Nat Chem Biol 2009 Sep;5(9):640-6 PMID: 19633659 PMCID: PMC2752665 SCOPUS ID: 2-s2.0-69249156893 07/28/2009 69 Citations

Improvement of pharmacological properties of irreversible thyroid receptor coactivator binding inhibitors. (Hwang JY, Arnold LA, Zhu F, Kosinski A, Mangano TJ, Setola V, Roth BL, Guy RK) J Med Chem 2009 Jul 09;52(13):3892-901 PMID: 19469546 PMCID: PMC2753520 SCOPUS ID: 2-s2.0-67649909039 05/28/2009 48 Citations

Quantification of the vitamin D receptor-coregulator interaction. (Teichert A, Arnold LA, Otieno S, Oda Y, Augustinaite I, Geistlinger TR, Kriwacki RW, Guy RK, Bikle DD) Biochemistry 2009 Feb 24;48(7):1454-61 PMID: 19183053 PMCID: PMC2654718 SCOPUS ID: 2-s2.0-61749101307 02/03/2009 59 Citations

A high-throughput ligand competition binding assay for the androgen receptor and other nuclear receptors. (Féau C, Arnold LA, Kosinski A, Guy RK) J Biomol Screen 2009 Jan;14(1):43-8 PMID: 19171919 PMCID: PMC2632761 SCOPUS ID: 2-s2.0-58849147947 01/28/2009 23 Citations

Synthesis and characterization of BODIPY-labeled colchicine. (Arnold LA, Ranaivo P, Guy RK) Bioorg Med Chem Lett 2008 Nov 15;18(22):5867-70 PMID: 18684625 PMCID: PMC2631555 SCOPUS ID: 2-s2.0-55249104717 08/08/2008 7 Citations

Erratum: A surface on the androgen receptor that allosterically regulates coactivator binding (Proceedings of the National Academy of Sciences of the United States of America (2007) 104, 41, (16074-16079) DOI: 10.1073/pnas. 0708036104) (Estébanez-Perpiñá E, Arnold LA, Nguyen P, Rodrigues ED, Mar E, Bateman R, Pallai P, Shokat KM, Baxter JD, Guy RK, Webb P, Fletterick RJ) Proceedings of the National Academy of Sciences of the United States of America 20 November 2007;104(47):18874 SCOPUS ID: 2-s2.0-36749090097 11/20/2007 4 Citations

Interaction between the androgen receptor and a segment of its corepressor SHP. (Jouravel N, Sablin E, Arnold LA, Guy RK, Fletterick RJ) Acta Crystallogr D Biol Crystallogr 2007 Nov;63(Pt 11):1198-200 PMID: 18007036 SCOPUS ID: 2-s2.0-36248949022 11/17/2007 19 Citations

Inhibitors of the interaction of a thyroid hormone receptor and coactivators: preliminary structure-activity relationships. (Arnold LA, Kosinski A, Estébanez-Perpiñá E, Fletterick RJ, Guy RK) J Med Chem 2007 Nov 01;50(22):5269-80 PMID: 17918822 PMCID: PMC2536611 SCOPUS ID: 2-s2.0-35848969820 10/09/2007 36 Citations

A surface on the androgen receptor that allosterically regulates coactivator binding. (Estébanez-Perpiñá E, Arnold LA, Nguyen P, Rodrigues ED, Mar E, Bateman R, Pallai P, Shokat KM, Baxter JD, Guy RK, Webb P, Fletterick RJ) Proc Natl Acad Sci U S A 2007 Oct 09;104(41):16074-9 PMID: 17911242 PMCID: PMC1999396 SCOPUS ID: 2-s2.0-35348812462 10/04/2007 249 Citations

Structural insight into the mode of action of a direct inhibitor of coregulator binding to the thyroid hormone receptor. (Estébanez-Perpiñá E, Arnold LA, Jouravel N, Togashi M, Blethrow J, Mar E, Nguyen P, Phillips KJ, Baxter JD, Webb P, Guy RK, Fletterick RJ) Mol Endocrinol 2007 Dec;21(12):2919-28 PMID: 17823305 SCOPUS ID: 2-s2.0-36849059727 09/08/2007 55 Citations

Synthesis of highly substituted dibenzo[b,f]azocines and their evaluation as protein kinase inhibitors. (Arnold LA, Kiplin Guy R) Bioorg Med Chem Lett 2006 Oct 15;16(20):5360-3 PMID: 16890431 SCOPUS ID: 2-s2.0-33748296097 08/08/2006 18 Citations

A high-throughput screening method to identify small molecule inhibitors of thyroid hormone receptor coactivator binding. (Arnold LA, Estébanez-Perpiñá E, Togashi M, Shelat A, Ocasio CA, McReynolds AC, Nguyen P, Baxter JD, Fletterick RJ, Webb P, Guy RK) Sci STKE 2006 Jun 27;2006(341):pl3 PMID: 16804159 SCOPUS ID: 2-s2.0-33745943980 06/29/2006 28 Citations

Discovery of small molecule inhibitors of the interaction of the thyroid hormone receptor with transcriptional coregulators. (Arnold LA, Estébanez-Perpiñá E, Togashi M, Jouravel N, Shelat A, McReynolds AC, Mar E, Nguyen P, Baxter JD, Fletterick RJ, Webb P, Guy RK) J Biol Chem 2005 Dec 30;280(52):43048-55 PMID: 16263725 SCOPUS ID: 2-s2.0-30044433051 11/03/2005 92 Citations

Synthesis of medium ring heterocycles using an intramolecular Heck reaction. (Arnold LA, Luo W, Guy RK) Org Lett 2004 Aug 19;6(17):3005-7 PMID: 15330669 SCOPUS ID: 2-s2.0-4444308033 08/28/2004 96 Citations

Highly enantioselective copper-catalyzed allylic alkylation with phosphoramidite ligands (Van Zijl AW, Arnold LA, Minnaard AJ, Feringa BL) Advanced Synthesis and Catalysis April 2004;346(4):413-420 SCOPUS ID: 2-s2.0-2342660181 04/01/2004 71 Citations

Catalytic enantioselective synthesis of (-)-prostaglandin E1 methyl ester based on a tandem 1,4-addition-aldol reaction. (Arnold LA, Naasz R, Minnaard AJ, Feringa BL) J Org Chem 2002 Oct 18;67(21):7244-54 PMID: 12375950 SCOPUS ID: 2-s2.0-0037131249 10/12/2002 103 Citations

Copper phosphoramidite catalyzed enantioselective ring-opening of oxabicyclic alkenes: remarkable reversal of stereocontrol. (Bertozzi F, Pineschi M, Macchia F, Arnold LA, Minnaard AJ, Feringa BL) Org Lett 2002 Aug 08;4(16):2703-5 PMID: 12153214 SCOPUS ID: 2-s2.0-0001701335 08/03/2002 133 Citations

New bidentate chiral phosphoramidites in copper-catalyzed asymmetric 1,4-addition of diethylzinc to cyclic α,β-enones: Enantioselective tandem 1,4-addition-aldol reactions with 2-cyclopentenone (Mandoli A, Arnold LA, De Vries AHM, Salvadori P, Feringa BL) Tetrahedron Asymmetry 30 July 2001;12(13):1929-1937 SCOPUS ID: 2-s2.0-0035973774 07/30/2001 52 Citations

Catalytic enantioselective synthesis of prostaglandin E(1) methyl ester using a tandem 1,4-addition-aldol reaction to a cyclopenten-3,5-dione monoacetal. (Arnold LA, Naasz R, Minnaard AJ, Feringa BL) J Am Chem Soc 2001 Jun 20;123(24):5841-2 PMID: 11403634 SCOPUS ID: 2-s2.0-0034801512 06/14/2001 131 Citations

Enantioselective copper-catalyzed allylic alkylation with dialkylzincs using phosphoramidite ligands. (Malda H, van Zijl AW, Arnold LA, Feringa BL) Org Lett 2001 Apr 19;3(8):1169-71 PMID: 11348186 SCOPUS ID: 2-s2.0-0035912307 05/12/2001 110 Citations

Enantioselective synthesis of bicyclic compounds via catalytic 1,4-addition-ring closing metathesis (Naasz R, Arnold LA, Minnaard AJ, Feringa BL) Chemical Communications 21 April 2001(8):735-736 SCOPUS ID: 2-s2.0-0035926076 04/21/2001 41 Citations

Highly Enantioselective Copper-Phosphoramidite Catalyzed Kinetic Resolution of Chiral 2-Cyclohexenones This work was supported by the Dutch Foundation for Scientific Research (NWO). (Naasz R, Arnold LA, Minnaard AJ, Feringa BL) Angew Chem Int Ed Engl 2001 Mar 02;40(5):927-930 PMID: 11241648 03/10/2001

Highly Enantioselective Copper-Phosphoramidite Catalyzed Kinetic Resolution of Chiral 2-Cyclohexenones. (Naasz R, Arnold LA, Minnaard AJ, Feringa BL) Angew Chem Int Ed Engl 2001 Mar 02;40(5):927-930 PMID: 29712175 03/02/2001

Enantioselective catalytic conjugate addition of dialkylzinc reagents using copper-phosphoramidite complexes; ligand variation and non-linear effects (Arnold LA, Imbos R, Mandoli A, De Vries AHM, Naasz R, Feringa BL) Tetrahedron 28 April 2000;56(18):2865-2878 SCOPUS ID: 2-s2.0-0034725134 04/28/2000 286 Citations

A new catalytic and enantioselective desymmetrization of symmetrical methylidene cycloalkene oxides (Bertozzi F, Crotti P, Macchia F, Pineschi M, Arnold A, Feringa BL) Organic Letters 6 April 2000;2(7):933-936 SCOPUS ID: 2-s2.0-0001423271 04/06/2000 38 Citations

A new diastereo- and enantioselective copper-catalyzed conversion of alkynyl epoxides into α-allenic alcohols (Bertozzi F, Crotti P, Macchia F, Pineschi M, Arnold A, Feringa BL) Tetrahedron Letters 25 June 1999;40(26):4893-4896 SCOPUS ID: 2-s2.0-0033603476 06/25/1999 45 Citations

Catalytic enantioselective annulations via 1,4-addition - Aldol cyclization of functionalized organozinc reagents [9] (Naasz R, Arnold LA, Pineschi M, Keller E, Feringa BL) Journal of the American Chemical Society 10 February 1999;121(5):1104-1105 SCOPUS ID: 2-s2.0-0033540709 02/10/1999 151 Citations

Catalytic enantioselective carbon-carbon bond formation by addition of dialkyizinc reagents to cyclic 1,3-diene monoepoxides (Badalassi F, Crotti P, Macchia F, Pineschi M, Arnold A, Feringa BL) Tetrahedron Letters 15 October 1998;39(42):7795-7798 SCOPUS ID: 2-s2.0-0032532776 10/15/1998 62 Citations

Highly enantioselective catalytic conjugate addition and tandem conjugate addition-aldol reactions of organozinc reagents (Feringa BL, Pineschi M, Arnold LA, Imbos R, De Vries AHM) Angewandte Chemie (International Edition in English) 1997;36(23):2620-2623 SCOPUS ID: 2-s2.0-0031573812 01/01/1997 464 Citations

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Profiles for MCW, MU, MSOE, UWM, BCW, CW, Froedtert, and VA Faculty

Alexander (Leggy) Arnold PhD

Professor

Publications (106)