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Scientific Publications

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Selected Publications

Guerrero M, Urbano M, Kim EK, Gamo AM, Riley S, Abgaryan L, Leaf N, Van Orden LJ,Brown SJ, Xie JY, Porreca F, Cameron MD, Rosen H, Roberts E. Design and Synthesis of aNovel and Selective Kappa Opioid Receptor (KOR) Antagonist (BTRX-335140). J MedChem.2019 Feb 28;62(4):1761-1780.doi: 10.1021/acs.jmedchem.8b01679.Epub 2019Feb 13.PubMed PMID: 30707578; PubMed Central PMCID: PMC6395531.

Johnson JL, Ramadass M, He J,Brown SJ, Zhang J, Abgaryan L, Biris N, Gavathiotis E,Rosen H, Catz SD.  Identification of Neutrophil Exocytosis Inhibitors (Nexinhibs), SmallMolecule Inhibitors of Neutrophil Exocytosis and Inflammation: DRUGGABILITY OF THESMALL GTPase Rab27a.  J Biol Chem.2016 Dec 9;291(50):25965-25982.doi:10.1074/jbc.M116.741884.Epub 2016 Oct 4.PubMed PMID: 27702998; PubMedCentral PMCID: PMC5207069.

Sanna MG, Vincent KP, Repetto E, Nguyen N, Brown SJ, Abgaryan L, Riley SW, Leaf NB,Cahalan SM, Kiosses WB, Kohno Y, Brown JH, McCulloch AD, Rosen H, Gonzalez-CabreraPJ.  Bitopic Sphingosine 1-Phosphate Receptor 3 (S1P3) Antagonist Rescue fromComplete Heart Block: Pharmacological and Genetic Evidence for Direct S1P3 Regulation of Mouse Cardiac Conduction.  Mol Pharmacol.2016 Jan;89(1):176-86.doi:10.1124/mol.115.100222.Epub 2015 Oct 22.PubMed PMID: 26494861; PubMedCentral PMCID: PMC4702096.

Mittapalli G, Abgaryan L, Brown SJ, Saldanha SA, Volmar CH, Ferguson J, Roberts E,Hodder P, Rosen H.2014;.Review.Optimization and characterization of an antagonistfor vasopressin 1a (V1a) receptor. Epub2013.PubMed PMID: 25506967.

Karuppuchamy T, Behrens EH, González-Cabrera P, Sarkisyan G, Gima L, Boyer JD,Bamias G, Jedlicka P, Veny M, Clark D, Peach R, Scott F, Rosen H, Rivera-Nieves J.  Sphingosine-1-phosphate receptor-1 (S1P1) is expressed by lymphocytes, dendritic cells,and endothelium and modulated during inflammatory bowel disease.  Mucosal Immunol.2017Jan;10(1):162-171. doi: 10.1038/mi.2016.35. Epub 2016 Apr 6. PMID: 27049060

Becklund BR, Purton JF, Ramsey C, Favre S, Vogt TK, Martin CE, Spasova DS, Sarkisyan G,LeRoy E, Tan JT, Wahlus H, Bondi-Boyd B, Luther SA, Surh CD.  The aged lymphoid tissueenvironment fails to support naïve T cell homeostasis.  Sci Rep.2016 Aug 2;6:30842.doi:10.1038/srep30842.PubMed PMID: 27480406; PubMed Central PMCID: PMC4969611.

Sarkisyan G, Gay LJ, Nguyen N, Felding BH, Rosen H.  Host endothelial S1PR1 regulation of vascular permeability modulates tumor growth.  Am J Physiol Cell Physiol.2014 Jul1;307(1):C14-24.doi: 10.1152/ajpcell.00043.2014.Epub 2014 Apr 16.PubMed PMID:24740542; PubMed Central PMCID: PMC4080184.

Witherden DA, Watanabe M, Garijo O, Rieder SE, Sarkisyan G, Cronin SJ, Verdino P,Wilson IA, Kumanogoh A, Kikutani H, Teyton L, Fischer WH, Havran WL.  The CD100receptor interacts with its plexin B2 ligand to regulate epidermal γδ T cell function.  Immunity.2012 Aug 24;37(2):314-25.doi: 10.1016/j.immuni.2012.05.026.Epub 2012Aug 16.PubMed PMID: 22902232; PubMed CentralPMCID: PMC3430606.

Sarkisyan G, Cahalan SM, Gonzalez-Cabrera PJ, Leaf NB, Rosen H.  Real-time differentiallabeling of blood, interstitium, and lymphatic and single-field analysis of vasculaturedynamics in vivo.  Am J Physiol Cell Physiol.2012 May 15;302(10):C1460-8.doi:10.1152/ajpcell.00382.2011.Epub 2012 Feb 22.PubMed PMID: 22357735.

Gonzalez-Cabrera PJ, Cahalan SM, Nguyen N, Sarkisyan G, Leaf NB, Cameron MD, KagoT, Rosen H.  S1P(1) receptor modulation with cyclical recovery from lymphopeniaameliorates mouse model of multiple sclerosis.  Mol Pharmacol.2012 Feb;81(2):166-74.doi: 10.1124/mol.111.076109.Epub 2011 Oct 26.PubMedPMID: 22031473; PubMedCentral PMCID: PMC3263953.

Cahalan SM, Gonzalez-Cabrera PJ, Sarkisyan G, Nguyen N, Schaeffer MT, Huang L,Yeager A, Clemons B, Scott F, Rosen H.  Actions of a picomolar short-acting S1P₁ agonistin S1P₁-eGFP knock-in mice.  Nat Chem Biol.2011 May;7(5):254-6.doi:10.1038/nchembio.547.Epub 2011 Mar 27.PubMed PMID: 21445057; PubMed CentralPMCID: PMC3430385.

Sarkisyan G, Robert AJ, Hedlund PB.  The 5-HT(7) receptor as a mediator and modulator of antidepressant-like behavior.  Behav Brain Res. 2010 May 1;209(1):99-108. doi:10.1016/j.bbr.2010.01.022. Epub 2010 Jan 25.PMID:20097233

Hedlund PB, Leopoldo M, Caccia S, Sarkisyan G, Fracasso C, Martelli G, Lacivita E, BerardiF, Perrone R.  LP-211 is a brain penetrant selective agonist for the serotonin 5-HT(7) receptor.  Neurosci Lett.2010 Aug 30;481(1):12-6.doi: 10.1016/j.neulet.2010.06.036.Epub 2010 Jun 23.PubMed PMID: 20600619; PubMed Central PMCID: PMC2910240.
Sarkisyan G, Hedlund PB.  The 5-HT7 receptor is involved in allocentric spatial memory information processing.  Behav Brain Res. 2009 Aug 24;202(1):26-31. doi:10.1016/j.bbr.2009.03.011. Epub 2009 Mar 19. PMID: 19447277
Harutiunian-Kozak BA, Grigorian GG, Kozak JA, Sharanbekian AB,Sarkisyan GS,Khachvankian DK.  Orientation sensitive properties of visually driven neurons inextrastriate area 21a of cat cortex.  Arch Ital Biol. 2008 Jun;146(2):119-30.
Harutiunian-Kozak BA, Sharanbekian AB, Kazarian AL, Grigorian GG, Kozak JA, SarkisyanGS, Khachvankian DK.  Spatial summation processes in the receptive fields of visually driven neurons of the cat’s cortical area 21a.  ArchItal Biol. 2006 Aug;144(3-4):127-44.PMID:16977829

Selected PubChem Assays

TLR9 Primary data in Pubchem (AID 504734).

NOTCH Maybridge primary screen (AID 434982)

Primary cell-based high throughput assay for inhibitors of the Janus kinase 2 mutant JAK2V617F (AID 1446)

Counterscreen for inhibitors of Janus kinase 2 mutant JAK2V617F: Cell-based high throughput assay to identify inhibitors of parental Ba/F3 cell viability (AID 1486)

Counterscreen for inhibitors of mutant JAK2V617F: Cell-based high throughput assay to identify inhibitors of parental Ba/F3 cell viability (AID 1520)

Confirmation cell-based high throughput screening assay for inhibitors of the Janus kinase 2 mutant JAK2V617F (AID 1521)

Luminescent dose response cell-based high throughput screening assay for inhibitors of the Janus kinase 2 mutant JAK2V617F (1691)

Luminescent counterscreen for inhibitors of the Janus kinase 2 mutant JAK2V617F: dose response cell-based high throughput screening assay for inhibitors of parental Ba/F3 cell viability (AID 1699)

Summary of probe development efforts to identify inhibitors of the Janus kinase 2 mutant JAK2V617F (AID 1797)

Late stage results from the probe development effort to identify inhibitors of the Janus kinase 2 mutant JAK2V617F (AID 2165)

Summary of the probe development efforts to identify antagonists of the vasopressin 1a receptor (V1a-R) (AID 743018)