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Items: 41

1.

A nonalcoholic fatty liver disease model in human induced pluripotent stem cell-derived hepatocytes, created by endoplasmic reticulum stress-induced steatosis.

Parafati M, Kirby RJ, Khorasanizadeh S, Rastinejad F, Malany S.

Dis Model Mech. 2018 Sep 25;11(9). pii: dmm033530. doi: 10.1242/dmm.033530.

2.

Discovery of Novel Small-Molecule Inducers of Heme Oxygenase-1 That Protect Human iPSC-Derived Cardiomyocytes from Oxidative Stress.

Kirby RJ, Divlianska DB, Whig K, Bryan N, Morfa CJ, Koo A, Nguyen KH, Maloney P, Peddibhotla S, Sessions EH, Hershberger PM, Smith LH, Malany S.

J Pharmacol Exp Ther. 2018 Jan;364(1):87-96. doi: 10.1124/jpet.117.243717. Epub 2017 Nov 3. Erratum in: J Pharmacol Exp Ther. 2018 Feb;364(2):179.

PMID:
29101218
3.

MondoA coordinately regulates skeletal myocyte lipid homeostasis and insulin signaling.

Ahn B, Soundarapandian MM, Sessions H, Peddibhotla S, Roth GP, Li JL, Sugarman E, Koo A, Malany S, Wang M, Yea K, Brooks J, Leone TC, Han X, Vega RB, Kelly DP.

J Clin Invest. 2016 Sep 1;126(9):3567-79. doi: 10.1172/JCI87382. Epub 2016 Aug 8.

4.

Assessment of drug-induced arrhythmic risk using limit cycle and autocorrelation analysis of human iPSC-cardiomyocyte contractility.

Kirby RJ, Qi F, Phatak S, Smith LH, Malany S.

Toxicol Appl Pharmacol. 2016 Aug 15;305:250-258. doi: 10.1016/j.taap.2016.06.025. Epub 2016 Jun 23.

PMID:
27343406
5.

Discovery of ML358, a Selective Small Molecule Inhibitor of the SKN-1 Pathway Involved in Drug Detoxification and Resistance in Nematodes.

Peddibhotla S, Fontaine P, Leung CK, Maloney P, Hershberger PM, Wang Y, Bousquet MS, Luesch H, Mangravita-Novo A, Pinkerton AB, Smith LH, Malany S, Choe K.

ACS Chem Biol. 2015 Aug 21;10(8):1871-9. doi: 10.1021/acschembio.5b00304. Epub 2015 May 22.

PMID:
25946346
6.

Inhibitors of Myocyte Triacylglyceride Accumulation.

Hershberger PM, Sugarman E, Maloney P, Peddibhotla S, Koo A, Suyama E, Ruidiaz ME, Heynen-Genel S, Nguyen KH, Vasile S, Mangravita-Novo A, Smith LH, Soundarapandian MM, Salaniwal S, Kung P, Vega RB, Chung TDY, Pinkerton AB, Malany S, Kelly DP.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2013 Dec 15 [updated 2015 Feb 11].

7.

Targeting α-synuclein oligomers by protein-fragment complementation for drug discovery in synucleinopathies.

Moussaud S, Malany S, Mehta A, Vasile S, Smith LH, McLean PJ.

Expert Opin Ther Targets. 2015 May;19(5):589-603. doi: 10.1517/14728222.2015.1009448. Epub 2015 Mar 18.

8.

Design of high-throughput screening assays and identification of a SUMO1-specific small molecule chemotype targeting the SUMO-interacting motif-binding surface.

Alontaga AY, Li Y, Chen CH, Ma CT, Malany S, Key DE, Sergienko E, Sun Q, Whipple DA, Matharu DS, Li B, Vega R, Li YJ, Schoenen FJ, Blagg BS, Chung TD, Chen Y.

ACS Comb Sci. 2015 Apr 13;17(4):239-46. doi: 10.1021/co500181b. Epub 2015 Mar 23.

9.

A high throughput screen for inhibitors of nematode detoxification genes.

Peddibhotla S, Leung CK, Maloney P, Hershberger PM, Nguyen K, Vasile S, Suyama E, Kane A, Bousquet MS, Leusch H, Stonich D, Mangravita-Novo A, Salaniwal S, Kung P, Diwan J, Smith LH, Chung TDY, Pinkerton AB, Malany S, Choe K.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2013 Apr 11 [updated 2014 Jan 13].

10.

Probing the CXCR6/CXCL16 Axis: Targeting Prevention of Prostate Cancer Metastasis.

Hershberger PM, Peddibhotla S, Sugarman E, Maloney P, Key D, Suyama E, Nguyen K, Vasile S, Kraft M, Stonich D, Mangravita-Novo A, Vicchiarelli M, Gosalia P, Milewski M, Li L, Hedrick M, Sun Q, Sergienko E, Cheltsov A, Salanawil S, Diwan J, Smith LH, Taichman RS, Chung TDY, Pinkerton AB, Malany S, Roth GP.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2012 Dec 15 [updated 2014 May 13].

11.

Potent inhibitors of lipid droplet formation.

Zou J, Ganji S, Pass I, Ardecky R, Peddibhotla M, Loribelle M, Heynen-Genel S, Sauer M, Pass I, Vasile S, Suyama E, Malany S, Mangravita-Novo A, Vicchiarelli M, McAnally D, Cheltsov A, Derek S, Shi S, Su Y, Zeng FY, Pinkerton AB, Smith LH, Kim S, Ngyuen H, Zeng FY, Diwan J, Heisel AJ, Coleman R, McDonough PM, Chung TDY.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2011 Oct 31 [updated 2014 May 13].

12.

Cardioprotective inhibitors of reperfusion injury.

Kane A, Peddibhotla S, Maloney P, Mehta A, Hood B, Suyama E, Nguyen K, Vasile S, Leavitt L, Cheltsov A, Salaiwal S, Stonich D, Mangravita-Novo A, Vicchiarelli M, Smith LH, Diwan J, Chung TDY, Pinkerton AB, Hershberger P, Malany S, Kitsis RN.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2012 Dec 10 [updated 2013 Mar 22].

13.

Identification of Inhibitors of triacylglyceride accumulation in muscle cells: comparing HTS results from 1536-well plate-based and high-content platforms.

Sugarman E, Koo A, Suyama E, Ruidiaz ME, Heynen-Genel S, Nguyen KH, Vasile S, Soundarapandian MM, Vega RB, Kelly DP, Smith LH, Malany S.

J Biomol Screen. 2014 Jan;19(1):77-87. doi: 10.1177/1087057113501198. Epub 2013 Aug 29.

14.

An ultra high-throughput, whole-animal screen for small molecule modulators of a specific genetic pathway in Caenorhabditis elegans.

Leung CK, Wang Y, Malany S, Deonarine A, Nguyen K, Vasile S, Choe KP.

PLoS One. 2013 Apr 29;8(4):e62166. doi: 10.1371/journal.pone.0062166. Print 2013.

15.

Lead optimization of 2-(piperidin-3-yl)-1H-benzimidazoles: identification of 2-morpholin- and 2-thiomorpholin-2-yl-1H-benzimidazoles as selective and CNS penetrating H₁-antihistamines for insomnia.

Ravula SB, Yu J, Tran JA, Arellano M, Tucci FC, Moree WJ, Li BF, Petroski RE, Wen J, Malany S, Hoare SR, Madan A, Crowe PD, Beaton G.

Bioorg Med Chem Lett. 2012 Jan 1;22(1):421-6. doi: 10.1016/j.bmcl.2011.10.115. Epub 2011 Nov 15.

PMID:
22153347
16.

Influence of pKa on the biotransformation of indene H1-antihistamines by CYP2D6.

Huang C, Moree WJ, Zamani-Kord S, Li BF, Tucci FC, Malany S, Wen J, Wang H, Hoare SR, Yang C, Madan A, Crowe PD, Beaton G.

Bioorg Med Chem Lett. 2011 Feb 1;21(3):947-51. doi: 10.1016/j.bmcl.2010.12.053. Epub 2010 Dec 16.

PMID:
21232954
17.

Identification of a novel selective H1-antihistamine with optimized pharmacokinetic properties for clinical evaluation in the treatment of insomnia.

Moree WJ, Li BF, Zamani-Kord S, Yu J, Coon T, Huang C, Marinkovic D, Tucci FC, Malany S, Bradbury MJ, Hernandez LM, Wen J, Wang H, Hoare SR, Petroski RE, Jalali K, Yang C, Sacaan A, Madan A, Crowe PD, Beaton G.

Bioorg Med Chem Lett. 2010 Oct 1;20(19):5874-8. doi: 10.1016/j.bmcl.2010.07.117. Epub 2010 Aug 3.

PMID:
20800486
18.

The discovery and structure-activity relationships of 2-(piperidin-3-yl)-1H-benzimidazoles as selective, CNS penetrating H1-antihistamines for insomnia.

Lavrador-Erb K, Ravula SB, Yu J, Zamani-Kord S, Moree WJ, Petroski RE, Wen J, Malany S, Hoare SR, Madan A, Crowe PD, Beaton G.

Bioorg Med Chem Lett. 2010 May 1;20(9):2916-9. doi: 10.1016/j.bmcl.2010.03.027. Epub 2010 Mar 10.

PMID:
20347297
19.

Selectivity profiling of novel indene H(1)-antihistamines for the treatment of insomnia.

Li BF, Moree WJ, Yu J, Coon T, Zamani-Kord S, Malany S, Jalali K, Wen J, Wang H, Yang C, Hoare SR, Petroski RE, Madan A, Crowe PD, Beaton G.

Bioorg Med Chem Lett. 2010 Apr 15;20(8):2629-33. doi: 10.1016/j.bmcl.2010.02.055. Epub 2010 Feb 18.

PMID:
20227880
20.

Novel benzothiophene H1-antihistamines for the treatment of insomnia.

Moree WJ, Jovic F, Coon T, Yu J, Li BF, Tucci FC, Marinkovic D, Gross RS, Malany S, Bradbury MJ, Hernandez LM, O'Brien Z, Wen J, Wang H, Hoare SR, Petroski RE, Sacaan A, Madan A, Crowe PD, Beaton G.

Bioorg Med Chem Lett. 2010 Apr 1;20(7):2316-20. doi: 10.1016/j.bmcl.2010.01.134. Epub 2010 Feb 2.

PMID:
20188547
21.

Characterization of novel selective H1-antihistamines for clinical evaluation in the treatment of insomnia.

Moree WJ, Li BF, Jovic F, Coon T, Yu J, Gross RS, Tucci F, Marinkovic D, Zamani-Kord S, Malany S, Bradbury MJ, Hernandez LM, O'Brien Z, Wen J, Wang H, Hoare SR, Petroski RE, Sacaan A, Madan A, Crowe PD, Beaton G.

J Med Chem. 2009 Sep 10;52(17):5307-10. doi: 10.1021/jm900933k.

PMID:
19663387
22.

Brain-penetrating 2-aminobenzimidazole H(1)-antihistamines for the treatment of insomnia.

Coon T, Moree WJ, Li B, Yu J, Zamani-Kord S, Malany S, Santos MA, Hernandez LM, Petroski RE, Sun A, Wen J, Sullivan S, Haelewyn J, Hedrick M, Hoare SJ, Bradbury MJ, Crowe PD, Beaton G.

Bioorg Med Chem Lett. 2009 Aug 1;19(15):4380-4. doi: 10.1016/j.bmcl.2009.05.086. Epub 2009 May 27.

PMID:
19553115
23.

Analytical method for simultaneously measuring ex vivo drug receptor occupancy and dissociation rate: application to (R)-dimethindene occupancy of central histamine H1 receptors.

Malany S, Hernandez LM, Smith WF, Crowe PD, Hoare SR.

J Recept Signal Transduct Res. 2009;29(2):84-93. doi: 10.1080/10799890902721339.

PMID:
19308787
24.

N-[6-amino-2-(heteroaryl)pyrimidin-4-yl]acetamides as A2A receptor antagonists with improved drug like properties and in vivo efficacy.

Lanier MC, Moorjani M, Luo Z, Chen Y, Lin E, Tellew JE, Zhang X, Williams JP, Gross RS, Lechner SM, Markison S, Joswig T, Kargo W, Piercey J, Santos M, Malany S, Zhao M, Petroski R, Crespo MI, Díaz JL, Saunders J, Wen J, O'Brien Z, Jalali K, Madan A, Slee DH.

J Med Chem. 2009 Feb 12;52(3):709-17. doi: 10.1021/jm800908d.

PMID:
19140664
25.

Lead optimization of 4-acetylamino-2-(3,5-dimethylpyrazol-1-yl)-6-pyridylpyrimidines as A2A adenosine receptor antagonists for the treatment of Parkinson's disease.

Zhang X, Tellew JE, Luo Z, Moorjani M, Lin E, Lanier MC, Chen Y, Williams JP, Saunders J, Lechner SM, Markison S, Joswig T, Petroski R, Piercey J, Kargo W, Malany S, Santos M, Gross RS, Wen J, Jalali K, O'Brien Z, Stotz CE, Crespo MI, Díaz JL, Slee DH.

J Med Chem. 2008 Nov 27;51(22):7099-110. doi: 10.1021/jm800851u.

PMID:
18947224
26.

2,6-Diaryl-4-acylaminopyrimidines as potent and selective adenosine A(2A) antagonists with improved solubility and metabolic stability.

Moorjani M, Luo Z, Lin E, Vong BG, Chen Y, Zhang X, Rueter JK, Gross RS, Lanier MC, Tellew JE, Williams JP, Lechner SM, Malany S, Santos M, Crespo MI, Díaz JL, Saunders J, Slee DH.

Bioorg Med Chem Lett. 2008 Oct 15;18(20):5402-5. doi: 10.1016/j.bmcl.2008.09.048. Epub 2008 Sep 14.

PMID:
18835161
27.

Synthesis of N-pyrimidinyl-2-phenoxyacetamides as adenosine A2A receptor antagonists.

Zhang X, Rueter JK, Chen Y, Moorjani M, Lanier MC, Lin E, Gross RS, Tellew JE, Williams JP, Lechner SM, Markison S, Joswig T, Malany S, Santos M, Castro-Palomino JC, Crespo MI, Prat M, Gual S, Díaz JL, Saunders J, Slee DH.

Bioorg Med Chem Lett. 2008 Mar 15;18(6):1778-83. doi: 10.1016/j.bmcl.2008.02.032. Epub 2008 Feb 16.

PMID:
18329269
28.

2-Amino-N-pyrimidin-4-ylacetamides as A2A receptor antagonists: 2. Reduction of hERG activity, observed species selectivity, and structure-activity relationships.

Slee DH, Moorjani M, Zhang X, Lin E, Lanier MC, Chen Y, Rueter JK, Lechner SM, Markison S, Malany S, Joswig T, Santos M, Gross RS, Williams JP, Castro-Palomino JC, Crespo MI, Prat M, Gual S, Díaz JL, Jalali K, Sai Y, Zuo Z, Yang C, Wen J, O'Brien Z, Petroski R, Saunders J.

J Med Chem. 2008 Mar 27;51(6):1730-9. doi: 10.1021/jm701187w. Epub 2008 Feb 29.

PMID:
18307293
29.

2-Amino-N-pyrimidin-4-ylacetamides as A2A receptor antagonists: 1. Structure-activity relationships and optimization of heterocyclic substituents.

Slee DH, Chen Y, Zhang X, Moorjani M, Lanier MC, Lin E, Rueter JK, Williams JP, Lechner SM, Markison S, Malany S, Santos M, Gross RS, Jalali K, Sai Y, Zuo Z, Yang C, Castro-Palomino JC, Crespo MI, Prat M, Gual S, Díaz JL, Saunders J.

J Med Chem. 2008 Mar 27;51(6):1719-29. doi: 10.1021/jm701185v. Epub 2008 Feb 29.

PMID:
18307292
30.

2,6-Diaryl-4-phenacylaminopyrimidines as potent and selective adenosine A(2A) antagonists with reduced hERG liability.

Moorjani M, Zhang X, Chen Y, Lin E, Rueter JK, Gross RS, Lanier MC, Tellew JE, Williams JP, Lechner SM, Malany S, Santos M, Ekhlassi P, Castro-Palomino JC, Crespo MI, Prat M, Gual S, Díaz JL, Saunders J, Slee DH.

Bioorg Med Chem Lett. 2008 Feb 15;18(4):1269-73. doi: 10.1016/j.bmcl.2008.01.036. Epub 2008 Jan 13.

PMID:
18249540
31.

Identification of novel, water-soluble, 2-amino-N-pyrimidin-4-yl acetamides as A2A receptor antagonists with in vivo efficacy.

Slee DH, Zhang X, Moorjani M, Lin E, Lanier MC, Chen Y, Rueter JK, Lechner SM, Markison S, Malany S, Joswig T, Santos M, Gross RS, Williams JP, Castro-Palomino JC, Crespo MI, Prat M, Gual S, Díaz JL, Wen J, O'Brien Z, Saunders J.

J Med Chem. 2008 Feb 14;51(3):400-6. doi: 10.1021/jm070623o. Epub 2008 Jan 12.

PMID:
18189346
32.

Histamine induces interleukin-6 expression in the human synovial sarcoma cell line (SW982) through the H1 receptor.

Wang SL, Malany S, Wang Q, Santos MA, Crowe PD, Maki RA.

Inflamm Res. 2006 Sep;55(9):393-8.

PMID:
17122961
33.

A novel cell-based assay for G-protein-coupled receptor-mediated cyclic adenosine monophosphate response element binding protein phosphorylation.

Selkirk JV, Nottebaum LM, Ford IC, Santos M, Malany S, Foster AC, Lechner SM.

J Biomol Screen. 2006 Jun;11(4):351-8. Epub 2006 Apr 28.

PMID:
16751331
34.

Single amino acid residue determinants of non-peptide antagonist binding to the corticotropin-releasing factor1 (CRF1) receptor.

Hoare SR, Brown BT, Santos MA, Malany S, Betz SF, Grigoriadis DE.

Biochem Pharmacol. 2006 Jul 14;72(2):244-55. Epub 2006 Apr 25.

PMID:
16750175
35.

Point mutations identify the glutamate binding pocket of the N-methyl-D-aspartate receptor as major site of conantokin-G inhibition.

Wittekindt B, Malany S, Schemm R, Otvos L, Maccecchini ML, Laube B, Betz H.

Neuropharmacology. 2001 Nov;41(6):753-61.

PMID:
11640930
36.

Orientation of alpha-neurotoxin at the subunit interfaces of the nicotinic acetylcholine receptor.

Malany S, Osaka H, Sine SM, Taylor P.

Biochemistry. 2000 Dec 19;39(50):15388-98.

PMID:
11112524
37.
38.

Subunit interface selective toxins as probes of nicotinic acetylcholine receptor structure.

Taylor P, Malany S, Molles BE, Osaka H, Tsigelny I.

Pflugers Arch. 2000 Jan;440(Suppl 1):R115-R117. doi: 10.1007/s004240000028.

PMID:
28008504
39.

Theoretical and experimental investigations of electrostatic effects on acetylcholinesterase catalysis and inhibition.

Malany S, Baker N, Verweyst M, Medhekar R, Quinn DM, Velan B, Kronman C, Shafferman A.

Chem Biol Interact. 1999 May 14;119-120:99-110.

PMID:
10421443
40.

Subunit interface selectivity of the alpha-neurotoxins for the nicotinic acetylcholine receptor.

Osaka H, Malany S, Kanter JR, Sine SM, Taylor P.

J Biol Chem. 1999 Apr 2;274(14):9581-6.

41.

Toxins selective for subunit interfaces as probes of nicotinic acetylcholine receptor structure.

Taylor P, Osaka H, Molles BE, Sugiyama N, Marchot P, Ackermann EJ, Malany S, McArdle JJ, Sine SM, Tsigelny I.

J Physiol Paris. 1998 Apr;92(2):79-83. Review.

PMID:
9782448

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