MRL Boston About Us :: Publications & Presentations

Publications & Presentations

This data is provided as a convenience for informational purposes and to provide information about MRL Boston.

PAMELA CARROLL, Ph.D.
Senior Research Fellow and Head of Target Validation

Carroll PM, Dougherty B, Ross-Macdonald P, Browman K, Fitzgerald K.
Model systems in drug discovery: chemical genetics meets genomics. Pharmacol Ther. 2003 Aug;99(2):183-220.

Lackner MR, Kindt RM, Carroll PM, Brown K, Cancilla MR, Chen C, de Silva H, Franke Y, Guan B, Heuer T, Hung T, Keegan K, Lee JM, Manne V, O’Brien C, Parry D, Perez-Vilar JJ, Reddy RK, Xiao H, Zhan H, Cockett M, Plowman G, Fitzgerald K, Costa M, Ross-Macdonald P.
Chemical genetics identifies Rab geranylgeranyl transferase as an apoptotic target of farnesyl transferase inhibitors. Cancer Cell. 2005 Apr;7(4):325-36.

Edgar KA, Belvin M, Parks AL, Whittaker K, Mahoney MB, Nicoll M, Park CC, Winter CG, Chen F, Lickteig K, Ahmad F, Esengil H, Lorenzi MV, Norton A, Rupnow BA, Shavesteh L, Tabios M, Young LM, Carroll PM, Kopczynski C, Plowman GD, Friedman LS, Francis-Lang HL.
Synthetic lethality of retinoblastoma mutant cells in the Drosophila eye by mutation of a novel peptidyl prolyl isomerase gene. Genetics. 2005 May;170(1):161-71.

MARK T. GOULET, Ph.D.
Executive Director, Medicinal Chemistry

Goulet, M.T.; Mosley, R.T. chapter: “Peptidomimetics”, in Encyclopedia of Hormones, Academic Press, 2003.

Janovick JA, Goulet M, Bush E, Greer J, Wettlaufer DG, Conn PM.
Structure-activity relations of successful pharmacologic chaperones for rescue of naturally occurring and manufactured mutants of the gonadotropin-releasing hormone receptor. J Pharmacol Exp Ther. 2003 May;305(2):608-14.

Ujjainwalla F, Warner D, Walsh TF, Wyvratt MJ, Zhou C, Yang L, Kalyani RN, MacNeil T, Van der Ploeg LH, Rosenblum CI, Tang R, Vongs A, Weinberg DH, Goulet MT.
Design and syntheses of melanocortin subtype-4 receptor agonists: evolution of the pyridazinone archetype. Bioorg Med Chem Lett. 2003 Dec 15;13(24):4431-5.

Jiang J, DeVita RJ, Goulet MT, Wyvratt MJ, Lo JL, Ren N, Yudkovitz JB, Cui J, Yang YT, Cheng K, Rohrer SP.
Syntheses and structure-activity relationship studies of piperidine-substituted quinolones as nonpeptide gonadotropin releasing hormone antagonists. Bioorg Med Chem Lett. 2004 Apr 5;14(7):1795-8.

DeVita RJ, Parikh M, Jiang J, Fair JA, Young JR, Walsh TF, Goulet MT, Lo JL, Ren N, Yudkovitz JB, Cui J, Yang YT, Cheng K, Rohrer SP, Wyvratt MJ.
Identification of neutral 4-O-alkyl quinolone nonpeptide GnRH receptor antagonists. Bioorg Med Chem Lett. 2004 Nov 15;14(22):5599-603.

Ujjainwalla F, Warner D, Snedden C, Grisson RD, Walsh TF, Wyvratt MJ, Kalyani RN, Macneil T, Tang R, Weinberg DH, Van der Ploeg L, Goulet MT.
Design and syntheses of melanocortin subtype-4 receptor agonists. Part 2: Discovery of the dihydropyridazinone motif. Bioorg Med Chem Lett. 2005 Jul 6.

ILONA KARIV, Ph.D.
Director,Automated Lead Optimization

Wang MM, Schnabel CA, Chachisvilis M, Yang R, Paliotti MJ, Simons LA, McMullin L, Hagen N, Lykstad K, Tu E, Pestana LM, Sur S, Zhang H, Butler WF, Kariv I, Marchand PJ.
Optical forces for noninvasive cellular analysis. Appl Opt. 2003 Oct 1;42(28):5765-73.

Forster AH, Wang MM, Butler WF, Chachisvilis M, Chung TD, Esener SC, Hall JM, Kibar O, Lykstad K, Marchand PJ, Mercer EM, Pestana LM, Sur S, Tu E, Yang R, Zhang H, Kariv I.
Use of moving optical gradient fields for analysis of apoptotic cellular responses in a chronic myeloid leukemia cell model. Anal Biochem. 2004 Apr 1;327(1):14-22.

Wang MM, Tu E, Raymond DE, Yang JM, Zhang H, Hagen N, Dees B, Mercer EM, Forster AH, Kariv I, Marchand PJ, Butler WF.
Microfluidic sorting of mammalian cells by optical force switching. Nat Biotechnol. 2005 Jan;23(1):83-7.

NANCY E. KOHL, Ph.D.
Senior Director, Cancer Biology and Therapeutics

deSolms SJ, Ciccarone TM, MacTough SC, Shaw AW, Buser CA, Ellis-Hutchings M, Fernandes C, Hamilton KA, Huber HE, Kohl NE, Lobell RB, Robinson RG, Tsou NN, Walsh ES, Graham SL, Beese LS, Taylor JS.
Dual protein farnesyltransferase-geranylgeranyltransferase-I inhibitors as potential cancer chemotherapeutic agents. J Med Chem. 2003 Jul 3;46(14):2973-84.

Lobell RB, Davide JP, Kohl NE, Burns HD, Eng WS, Gibson RE.
A cell-based radioligand binding assay for farnesyl: protein transferase inhibitors.
J Biomol Screen. 2003 Aug;8(4):430-8.

Sepp-Lorenzino L, Rands E, Mao X, Connolly B, Shipman J, Antanavage J, Hill S, Davis L, Beck S, Rickert K, Coll K, Ciecko P, Fraley M, Hoffman W, Hartman G, Heimbrook D, Gibbs J, Kohl N, Thomas K.
A novel orally bioavailable inhibitor of kinase insert domain-containing receptor induces antiangiogenic effects and prevents tumor growth in vivo. Cancer Res. 2004 Jan 15;64(2):751-6.

Bilodeau MT, Balitza AE, Koester TJ, Manley PJ, Rodman LD, Buser-Doepner C, Coll KE, Fernandes C, Gibbs JB, Heimbrook DC, Huckle WR, Kohl N, Lynch JJ, Mao X, McFall RC, McLoughlin D, Miller-Stein CM, Rickert KW, Sepp-Lorenzino L, Shipman JM, Subramanian R, Thomas KA, Wong BK, Yu S, Hartman GD.
Potent N-(1,3-thiazol-2-yl)pyridin-2-amine vascular endothelial growth factor receptor tyrosine kinase inhibitors with excellent pharmacokinetics and low affinity for the hERG ion channel. J Med Chem. 2004 Dec 2;47(25):6363-72.

Hardwick JS, Yang Y, Zhang C, Shi B, McFall R, Koury EJ, Hill SL, Dai H, Wasserman R, Phillips RL, Weinstein EJ, Kohl NE, Severino ME, Lamb JR, Sepp-Lorenzino L.
Identification of biomarkers for tumor endothelial cell proliferation through gene expression profiling. Mol Cancer Ther. 2005 Mar;4(3):413-25.

Cox CD, Breslin MJ, Mariano BJ, Coleman PJ, Buser CA, Walsh ES, Hamilton K, Huber HE, Kohl NE, Torrent M, Yan Y, Kuo LC, Hartman GD.
Kinesin spindle protein (KSP) inhibitors. Part 1: the discovery of 3,5-diaryl-4,5-dihydropyrazoles as potent and selective inhibitors of the mitotic kinesin KSP. Bioorg Med Chem Lett. 2005 Apr 15;15(8):2041-5.

Tao W, South VJ, Zhang Y, Davide JP, Farrell L, Kohl NE, Sepp-Lorenzino L, Lobell RB.
Induction of apoptosis by an inhibitor of the mitotic kinesin KSP requires both activation of the spindle assembly checkpoint and mitotic slippage. Cancer Cell. 2005 Jul;8(1):49-59.

LEX VAN DER PLOEG, Ph.D.
Vice President, Basic Research; Site Head RL Boston

Chung C, Varnerin JP, Morin NR, MacNeil DJ, Singh SB, Patel S, Scapin G, Van der Ploeg LH, Tota MR.
The role of tryptophan 1072 in human PDE3B inhibitor binding. Biochem Biophys Res Commun. 2003 Aug 8;307(4):1045-50.

Shearman LP, Camacho RE, Sloan Stribling D, Zhou D, Bednarek MA, Hreniuk DL, Feighner SD, Tan CP, Howard AD, Van der Ploeg LH, MacIntyre DE, Hickey GJ, Strack AM.
Chronic MCH-1 receptor modulation alters appetite, body weight and adiposity in rats. Eur J Pharmacol. 2003 Aug 15;475(1-3):37-47.

Grieco P, Balse-Srinivasan P, Han G, Weinberg D, MacNeil T, Van der Ploeg LH, Hruby VJ.
Extensive structure-activity studies of lactam derivatives of MT-II and SHU-9119: their activity and selectivity at human melanocortin receptors 3, 4, and 5. J Pept Res. 2003 Nov;62(5):199-206.

Edmondson SD, Mastracchio A, He J, Chung CC, Forrest MJ, Hofsess S, MacIntyre E, Metzger J, O'Connor N, Patel K, Tong X, Tota MR, Van der Ploeg LH, Varnerin JP, Fisher MH, Wyvratt MJ, Weber AE, Parmee ER.
Benzyl vinylogous amide substituted aryldihydropyridazinones and aryldimethylpyrazolones as potent and selective PDE3B inhibitors. Bioorg Med Chem Lett. 2003 Nov 17;13(22):3983-7.

Sabatier N, Caquineau C, Dayanithi G, Bull P, Douglas AJ, Guan XM, Jiang M, Van der Ploeg L, Leng G.
Alpha-melanocyte-stimulating hormone stimulates oxytocin release from the dendrites of hypothalamic neurons while inhibiting oxytocin release from their terminals in the neurohypophysis. J Neurosci. 2003 Nov 12;23(32):10351-8.

Chen HY, Trumbauer ME, Chen AS, Weingarth DT, Adams JR, Frazier EG, Shen Z, Marsh DJ, Feighner SD, Guan XM, Ye Z, Nargund RP, Smith RG, Van der Ploeg LH, Howard AD, MacNeil DJ, Qian S.
Orexigenic action of peripheral ghrelin is mediated by neuropeptide Y and agouti-related protein. Endocrinology. 2004 Jun;145(6):2607-12.

Varnerin JP, Chung CC, Patel SB, Scapin G, Parmee ER, Morin NR, MacNeil DJ, Cully DF, Van der Ploeg LH, Tota MR.
Expression, refolding, and purification of recombinant human phosphodiesterase 3B: definition of the N-terminus of the catalytic core. Protein Expr Purif. 2004 Jun;35(2):225-36.

Scapin G, Patel SB, Chung C, Varnerin JP, Edmondson SD, Mastracchio A, Parmee ER, Singh SB, Becker JW, Van der Ploeg LH, Tota M R.
Crystal structure of human phosphodiesterase 3B: atomic basis for substrate and inhibitor specificity. Biochemistry. 2004 May 25;43(20):6091-100.

Lewis HD, Beher D, Smith D, Hewson L, Cookson N, Reynolds DS, Dawson GR, Jiang M, Van der Ploeg LH, Qian S, Rosahl TW, Kalaria RN, Shearman MS.
Novel aspects of accumulation dynamics and A beta composition in transgenic models of AD. Neurobiol Aging. 2004 Oct;25(9):1175-85.

Palucki BL, Park MK, Nargund RP, Ye Z, Sebhat IK, Pollard PG, Kalyani RN, Tang R, Macneil T, Weinberg DH, Vongs A, Rosenblum CI, Doss GA, Miller RR, Stearns RA, Peng Q, Tamvakopoulos C, McGowan E, Martin WJ, Metzger JM, Shepherd CA, Strack AM, Macintyre DE, Van der Ploeg LH, Patchett AA.
Discovery of (2S)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-4-methyl-2-piperazinecarboxamide (MB243), a potent and selective melanocortin subtype-4 receptor agonist. Bioorg Med Chem Lett. 2005 Jan 3;15(1):171-5.

Meurer LC, Finke PE, Mills SG, Walsh TF, Toupence RB, Debenham JS, Goulet MT, Wang J, Tong X, Fong TM, Lao J, Schaeffer MT, Chen J, Shen CP, Sloan Stribling D, Shearman LP, Strack AM, Van der Ploeg LH.
Synthesis and SAR of 5,6-diarylpyridines as human CB1 inverse agonists. Bioorg Med Chem Lett. 2005 Feb 1;15(3):645-51.

Unmehopa UA, van Heerikhuize JJ, Spijkstra W, Woods JW, Howard AD, Zycband E, Feighner SD, Hreniuk DL, Palyha OC, Guan XM, Macneil DJ, Van der Ploeg LH, Swaab DF.
Increased melanin concentrating hormone receptor type I in the human hypothalamic infundibular nucleus in cachexia. J Clin Endocrinol Metab. 2005 Apr;90(4):2412-9.

Plummer CW, Finke PE, Mills SG, Wang J, Tong X, Doss GA, Fong TM, Lao JZ, Schaeffer MT, Chen J, Shen CP, Stribling DS, Shearman LP, Strack AM, Van der Ploeg LH.
Synthesis and activity of 4,5-diarylimidazoles as human CB1 receptor inverse agonists. Bioorg Med Chem Lett. 2005 Mar 1;15(5):1441-6.

Palucki BL, Park MK, Nargund RP, Tang R, MacNeil T, Weinberg DH, Vongs A, Rosenblum CI, Doss GA, Miller RR, Stearns RA, Peng Q, Tamvakopoulos C, Van der Ploeg LH, Patchett AA.
2-Piperazinecarboxamides as potent and selective melanocortin subtype-4 receptor agonists. Bioorg Med Chem Lett. 2005 Apr 15;15(8):1993-6.

Bakshi RK, Hong Q, Olson JT, Ye Z, Sebhat IK, Weinberg DH, MacNeil T, Kalyani RN, Tang R, Martin WJ, Strack A, McGowan E, Tamvakopoulos C, Miller RR, Stearns RA, Tang W, Maclntyre DE, van der Ploeg LH, Patchett AA, Nargund RP.
1-Amino-1,2,3,4-tetrahydronaphthalene-2-carboxylic acid as a Tic mimetic: application in the synthesis of potent human melanocortin-4 receptor selective agonists. Bioorg Med Chem Lett. 2005 Jul 15;15(14):3430-3.

Ye Z, Guo L, Barakat KJ, Pollard PG, Palucki BL, Sebhat IK, Bakshi RK, Tang R, Kalyani RN, Vongs A, Chen AS, Chen HY, Rosenblum CI, MacNeil T, Weinberg DH, Peng Q, Tamvakopoulos C, Miller RR, Stearns RA, Cashen DE, Martin WJ, Metzger JM, Strack AM, MacIntyre DE, Van der Ploeg LH, Patchett AA, Wyvratt MJ, Nargund RP.
Discovery and activity of (1R,4S,6R)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-2-methyl-2-azabicyclo[2.2.2]octane-6-carboxamide (3, RY764), a potent and selective melanocortin subtype-4 receptor agonist. Bioorg Med Chem Lett. 2005 Aug 1;15(15):3501-5.

Ye Z, Macneil T, Weinberg DH, Kalyani RN, Tang R, Strack AM, Murphy BA, Mosley RT, Euan Macintyre D, Van der Ploeg LH, Patchett AA, Wyvratt MJ, Nargund RP.
Structure-activity relationship of linear tetrapeptides Tic-DPhe-Arg-Trp-NH(2) at the human melanocortin-4 receptor and effects on feeding behaviors in rat. Peptides. 2005 Jun 29.

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