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Items: 1 to 50 of 68

1.

Characterization of an anesthetized dog model of transient cardiac ischemia and rapid pacing: a pilot study for preclinical assessment of the potential for proarrhythmic risk of novel drug candidates.

Damiano BP, van der Linde HJ, Van Deuren B, Somers Y, Lubomirski M, Teisman A, Gallacher DJ.

J Pharmacol Toxicol Methods. 2015 Mar-Apr;72:72-84. doi: 10.1016/j.vascn.2014.10.006. Epub 2014 Oct 23.

PMID:
25450838
2.

A thiocarbamate inhibitor of endothelial lipase raises HDL cholesterol levels in mice.

Greco MN, Connelly MA, Leo GC, Olson MW, Powell E, Huang Z, Hawkins M, Smith C, Schalk-Hihi C, Darrow AL, Xin H, Lang W, Damiano BP, Hlasta DJ.

Bioorg Med Chem Lett. 2013 May 1;23(9):2595-7. doi: 10.1016/j.bmcl.2013.02.113. Epub 2013 Mar 7.

PMID:
23528297
3.

Endothelial lipase is localized to follicular epithelial cells in the thyroid gland and is moderately expressed in adipocytes.

Connelly MA, D'Andrea MR, Qi J, Dzordzorme KC, Damiano BP.

J Histochem Cytochem. 2012 Sep;60(9):694-705. doi: 10.1369/0022155412454110. Epub 2012 Jun 26.

4.

Phase 0 study of the inhibition of cholesteryl ester transfer protein activity by JNJ-28545595 in plasma from normolipidemic and dyslipidemic humans.

Sarich TC, Connelly MA, Schranz DB, Ghosh A, Manitpisitkul P, Leary ET, Rothenberg P, Demarest KT, Damiano BP.

Int J Clin Pharmacol Ther. 2012 Aug;50(8):584-94. doi: 10.5414/CP201627.

PMID:
22578199
5.

Arterial antithrombotic activity of rivaroxaban, an orally active factor Xa inhibitor, in a rat electrolytic carotid artery injury model of thrombosis.

Parry TJ, Huang Z, Chen C, Connelly MA, Perzborn E, Andrade-Gordon P, Damiano BP.

Blood Coagul Fibrinolysis. 2011 Dec;22(8):720-6. doi: 10.1097/MBC.0b013e32834cb30e.

PMID:
21986468
6.

Design and optimization of benzimidazole-containing transient receptor potential melastatin 8 (TRPM8) antagonists.

Parks DJ, Parsons WH, Colburn RW, Meegalla SK, Ballentine SK, Illig CR, Qin N, Liu Y, Hutchinson TL, Lubin ML, Stone DJ Jr, Baker JF, Schneider CR, Ma J, Damiano BP, Flores CM, Player MR.

J Med Chem. 2011 Jan 13;54(1):233-47. doi: 10.1021/jm101075v. Epub 2010 Dec 3.

PMID:
21128593
7.

A novel fluorogenic substrate for the measurement of endothelial lipase activity.

Darrow AL, Olson MW, Xin H, Burke SL, Smith C, Schalk-Hihi C, Williams R, Bayoumy SS, Deckman IC, Todd MJ, Damiano BP, Connelly MA.

J Lipid Res. 2011 Feb;52(2):374-82. doi: 10.1194/jlr.D007971.

8.

Simultaneous PCNA and TUNEL labeling for testicular toxicity evaluation suggests that detection of apoptosis may be more sensitive than proliferation.

D'Andrea MR, Alicknavitch M, Nagele RG, Damiano BP.

Biotech Histochem. 2010 Apr 28;85(3):195-204. doi: 10.3109/10520290903547778.

PMID:
20109096
9.

Discovery and clinical evaluation of 1-{N-[2-(amidinoaminooxy)ethyl]amino}carbonylmethyl-6-methyl-3-[2,2-difluoro-2-phenylethylamino]pyrazinone (RWJ-671818), a thrombin inhibitor with an oxyguanidine P1 motif.

Lu T, Markotan T, Ballentine SK, Giardino EC, Spurlino J, Crysler CS, Brown K, Maryanoff BE, Tomczuk BE, Damiano BP, Shukla U, End D, Andrade-Gordon P, Bone RF, Player MR.

J Med Chem. 2010 Feb 25;53(4):1843-56. doi: 10.1021/jm901802n. Erratum in: J Med Chem. 2010 Apr 22;53(8):3422. Crysler, Carl S [added].

PMID:
20102150
10.

Torcetrapib produces endothelial dysfunction independent of cholesteryl ester transfer protein inhibition.

Connelly MA, Parry TJ, Giardino EC, Huang Z, Cheung WM, Chen C, Cools F, Van der Linde H, Gallacher DJ, Kuo GH, Sarich TC, Demarest KT, Damiano BP.

J Cardiovasc Pharmacol. 2010 May;55(5):459-68. doi: 10.1097/FJC.0b013e3181cf03cb.

PMID:
20051879
11.

Cooperative antithrombotic effect from the simultaneous inhibition of thrombin and factor Xa.

Giardino EC, Haertlein BJ, de Garavilla L, Costanzo MJ, Damiano BP, Andrade-Gordon P, Maryanoff BE.

Blood Coagul Fibrinolysis. 2010 Mar;21(2):128-34. doi: 10.1097/MBC.0b013e3283358100.

PMID:
20010091
12.

Nonpeptide urotensin-II receptor antagonists: a new ligand class based on piperazino-phthalimide and piperazino-isoindolinone subunits.

Lawson EC, Luci DK, Ghosh S, Kinney WA, Reynolds CH, Qi J, Smith CE, Wang Y, Minor LK, Haertlein BJ, Parry TJ, Damiano BP, Maryanoff BE.

J Med Chem. 2009 Dec 10;52(23):7432-45. doi: 10.1021/jm900683d.

PMID:
19731961
14.

PCNA indexing as a preclinical immunohistochemical biomarker for testicular toxicity.

D'Andrea MR, Lawrence D, Nagele RG, Wang CY, Damiano BP.

Biotech Histochem. 2008 Oct;83(5):211-20. doi: 10.1080/10520290802521804.

PMID:
19016366
15.

Pharmacological characterization of RWJ-676070, a dual vasopressin V(1A)/V(2) receptor antagonist.

Gunnet JW, Wines P, Xiang M, Rybczynski P, Andrade-Gordon P, de Garavilla L, Parry TJ, Cheung WM, Minor L, Demarest KT, Maryanoff BE, Damiano BP.

Eur J Pharmacol. 2008 Aug 20;590(1-3):333-42. doi: 10.1016/j.ejphar.2008.06.010. Epub 2008 Jun 7.

PMID:
18599033
16.

Orally efficacious thrombin inhibitors with cyanofluorophenylacetamide as the P2 motif.

Kreutter KD, Lu T, Lee L, Giardino EC, Patel S, Huang H, Xu G, Fitzgerald M, Haertlein BJ, Mohan V, Crysler C, Eisennagel S, Dasgupta M, McMillan M, Spurlino JC, Huebert ND, Maryanoff BE, Tomczuk BE, Damiano BP, Player MR.

Bioorg Med Chem Lett. 2008 May 1;18(9):2865-70. doi: 10.1016/j.bmcl.2008.03.087. Epub 2008 Apr 8.

PMID:
18420408
17.

Carba-nucleosides as potent antagonists of the adenosine 5'-diphosphate (ADP) purinergic receptor (P2Y12 on human platelets.

Ye H, Chen C, Zhang HC, Haertlein B, Parry TJ, Damiano BP, Maryanoff BE.

ChemMedChem. 2008 May;3(5):732-6. doi: 10.1002/cmdc.200700310. No abstract available.

PMID:
18224705
18.

7-fluoroindazoles as potent and selective inhibitors of factor Xa.

Lee YK, Parks DJ, Lu T, Thieu TV, Markotan T, Pan W, McComsey DF, Milkiewicz KL, Crysler CS, Ninan N, Abad MC, Giardino EC, Maryanoff BE, Damiano BP, Player MR.

J Med Chem. 2008 Jan 24;51(2):282-97. Epub 2007 Dec 27.

PMID:
18159923
19.

Studies with an orally bioavailable alpha V integrin antagonist in animal models of ocular vasculopathy: retinal neovascularization in mice and retinal vascular permeability in diabetic rats.

Santulli RJ, Kinney WA, Ghosh S, Decorte BL, Liu L, Tuman RW, Zhou Z, Huebert N, Bursell SE, Clermont AC, Grant MB, Shaw LC, Mousa SA, Galemmo RA Jr, Johnson DL, Maryanoff BE, Damiano BP.

J Pharmacol Exp Ther. 2008 Mar;324(3):894-901. Epub 2007 Dec 14.

PMID:
18083913
20.

Next-generation spirobenzazepines: identification of RWJ-676070 as a balanced vasopressin V1a/V2 receptor antagonist for human clinical studies.

Xiang MA, Rybczynski PJ, Patel M, Chen RH, McComsey DF, Zhang HC, Gunnet JW, Look R, Wang Y, Minor LK, Zhong HM, Villani FJ, Demarest KT, Damiano BP, Maryanoff BE.

Bioorg Med Chem Lett. 2007 Dec 1;17(23):6623-8. Epub 2007 Sep 19.

PMID:
17942308
21.

Phenylpiperidine-benzoxazinones as urotensin-II receptor antagonists: synthesis, SAR, and in vivo assessment.

Luci DK, Ghosh S, Smith CE, Qi J, Wang Y, Haertlein B, Parry TJ, Li J, Almond HR Jr, Minor LK, Damiano BP, Kinney WA, Maryanoff BE, Lawson EC.

Bioorg Med Chem Lett. 2007 Dec 1;17(23):6489-92. Epub 2007 Oct 1.

PMID:
17933531
22.

Discovery of potent, selective, orally active, nonpeptide inhibitors of human mast cell chymase.

Greco MN, Hawkins MJ, Powell ET, Almond HR Jr, de Garavilla L, Hall J, Minor LK, Wang Y, Corcoran TW, Di Cera E, Cantwell AM, Savvides SN, Damiano BP, Maryanoff BE.

J Med Chem. 2007 Apr 19;50(8):1727-30. Epub 2007 Mar 16.

PMID:
17361995
23.

Novel bis(indolyl)maleimide pyridinophanes that are potent, selective inhibitors of glycogen synthase kinase-3.

Zhang HC, BoƱaga LV, Ye H, Derian CK, Damiano BP, Maryanoff BE.

Bioorg Med Chem Lett. 2007 May 15;17(10):2863-8. Epub 2007 Feb 25.

PMID:
17350261
24.

Urotensin-II induces ear flushing in rats.

Qi JS, Schulingkamp R, Parry TJ, Colburn R, Stone D, Haertlein B, Minor LK, Andrade-Gordon P, Damiano BP.

Br J Pharmacol. 2007 Feb;150(4):415-23. Epub 2007 Jan 8.

25.

Exploration of potential prodrugs of RWJ-445167, an oxyguanidine-based dual inhibitor of thrombin and factor Xa.

Maryanoff BE, McComsey DF, Costanzo MJ, Yabut SC, Lu T, Player MR, Giardino EC, Damiano BP.

Chem Biol Drug Des. 2006 Jul;68(1):29-36.

PMID:
16923023
26.

Synthesis and biological evaluation of novel pyridazinone-based alpha4 integrin receptor antagonists.

Gong Y, Barbay JK, Dyatkin AB, Miskowski TA, Kimball ES, Prouty SM, Fisher MC, Santulli RJ, Schneider CR, Wallace NH, Ballentine SA, Hageman WE, Masucci JA, Maryanoff BE, Damiano BP, Andrade-Gordon P, Hlasta DJ, Hornby PJ, He W.

J Med Chem. 2006 Jun 1;49(11):3402-11.

PMID:
16722660
27.

Selection of a 2-azabicyclo[2.2.2]octane-based alpha4beta1 integrin antagonist as an inhaled anti-asthmatic agent.

Lawson EC, Santulli RJ, Dyatkin AB, Ballentine SA, Abraham WM, Rudman S, Page CP, de Garavilla L, Damiano BP, Kinney WA, Maryanoff BE.

Bioorg Med Chem. 2006 Jun 15;14(12):4208-16. Epub 2006 Feb 21.

PMID:
16495061
28.

Aza-bicyclic amino acid carboxamides as alpha4beta1/alpha4beta7 integrin receptor antagonists.

Dyatkin AB, Gong Y, Miskowski TA, Kimball ES, Prouty SM, Fisher MC, Santulli RJ, Schneider CR, Wallace NH, Hornby PJ, Diamond C, Kinney WA, Maryanoff BE, Damiano BP, He W.

Bioorg Med Chem. 2005 Dec 15;13(24):6693-702. Epub 2005 Aug 19.

PMID:
16112583
29.

Novel indolylindazolylmaleimides as inhibitors of protein kinase C-beta: synthesis, biological activity, and cardiovascular safety.

Zhang HC, Derian CK, McComsey DF, White KB, Ye H, Hecker LR, Li J, Addo MF, Croll D, Eckardt AJ, Smith CE, Li Q, Cheung WM, Conway BR, Emanuel S, Demarest KT, Andrade-Gordon P, Damiano BP, Maryanoff BE.

J Med Chem. 2005 Mar 24;48(6):1725-8.

PMID:
15771419
30.

A novel, potent dual inhibitor of the leukocyte proteases cathepsin G and chymase: molecular mechanisms and anti-inflammatory activity in vivo.

de Garavilla L, Greco MN, Sukumar N, Chen ZW, Pineda AO, Mathews FS, Di Cera E, Giardino EC, Wells GI, Haertlein BJ, Kauffman JA, Corcoran TW, Derian CK, Eckardt AJ, Damiano BP, Andrade-Gordon P, Maryanoff BE.

J Biol Chem. 2005 May 6;280(18):18001-7. Epub 2005 Feb 28.

31.

1,2,3,4-Tetrahydroquinoline-containing alphaVbeta3 integrin antagonists with enhanced oral bioavailability.

Ghosh S, Santulli RJ, Kinney WA, Decorte BL, Liu L, Lewis JM, Proost JC, Leo GC, Masucci J, Hageman WE, Thompson AS, Chen I, Kawahama R, Tuman RW, Galemmo RA Jr, Johnson DL, Damiano BP, Maryanoff BE.

Bioorg Med Chem Lett. 2004 Dec 6;14(23):5937-41.

PMID:
15501072
32.

Piperidine-containing beta-arylpropionic acids as potent antagonists of alphavbeta3/alphavbeta5 integrins.

De Corte BL, Kinney WA, Liu L, Ghosh S, Brunner L, Hoekstra WJ, Santulli RJ, Tuman RW, Baker J, Burns C, Proost JC, Tounge BA, Damiano BP, Maryanoff BE, Johnson DL, Galemmo RA Jr.

Bioorg Med Chem Lett. 2004 Oct 18;14(20):5227-32.

PMID:
15380233
33.

3-(7-Azaindolyl)-4-arylmaleimides as potent, selective inhibitors of glycogen synthase kinase-3.

Zhang HC, Ye H, Conway BR, Derian CK, Addo MF, Kuo GH, Hecker LR, Croll DR, Li J, Westover L, Xu JZ, Look R, Demarest KT, Andrade-Gordon P, Damiano BP, Maryanoff BE.

Bioorg Med Chem Lett. 2004 Jun 21;14(12):3245-50.

PMID:
15149684
34.

Mer receptor tyrosine kinase signaling participates in platelet function.

Chen C, Li Q, Darrow AL, Wang Y, Derian CK, Yang J, de Garavilla L, Andrade-Gordon P, Damiano BP.

Arterioscler Thromb Vasc Biol. 2004 Jun;24(6):1118-23. Epub 2004 May 6.

PMID:
15130911
35.

Aza-bicyclic amino acid sulfonamides as alpha(4)beta(1)/alpha(4)beta(7) integrin antagonists.

Dyatkin AB, Hoekstra WJ, Kinney WA, Kontoyianni M, Santulli RJ, Kimball ES, Fisher MC, Prouty SM, Abraham WM, de Garavilla L, Andrade-Gordon P, Hlasta DJ, He W, Hornby PJ, Damiano BP, Maryanoff BE.

Bioorg Med Chem Lett. 2004 Feb 9;14(3):591-6. Erratum in: Bioorg Med Chem Lett. 2004 May 3;14(9):2371.

PMID:
14741249
36.

RWJ-58259: a selective antagonist of protease activated receptor-1.

Damiano BP, Derian CK, Maryanoff BE, Zhang HC, Gordon PA.

Cardiovasc Drug Rev. 2003 Winter;21(4):313-26. Review.

PMID:
14647534
37.

Blockade of the thrombin receptor protease-activated receptor-1 with a small-molecule antagonist prevents thrombus formation and vascular occlusion in nonhuman primates.

Derian CK, Damiano BP, Addo MF, Darrow AL, D'Andrea MR, Nedelman M, Zhang HC, Maryanoff BE, Andrade-Gordon P.

J Pharmacol Exp Ther. 2003 Feb;304(2):855-61. Erratum in: J Pharmacol Exp Ther. 2003 Apr;305(1):402.

PMID:
12538843
38.

Thrombin regulation of cell function through protease-activated receptors: implications for therapeutic intervention.

Derian CK, Damiano BP, D'Andrea MR, Andrade-Gordon P.

Biochemistry (Mosc). 2002 Jan;67(1):56-64. Review.

39.

Increased expression of serine palmitoyltransferase (SPT) in balloon-injured rat carotid artery.

Uhlinger DJ, Carton JM, Argentieri DC, Damiano BP, Dandrea MR.

Thromb Haemost. 2001 Nov;86(5):1320-6.

PMID:
11816724
40.

Antiplatelet and antithrombotic activity of RWJ-53308, a novel orally active glycoprotein IIb/IIIa antagonist.

Damiano BP, Mitchell JA, Giardino E, Corcoran T, Haertlein BJ, de Garavilla L, Kauffman JA, Hoekstra WJ, Maryanoff BE, Andrade-Gordon P.

Thromb Res. 2001 Oct 15;104(2):113-26.

PMID:
11672755
41.

1,2,4-triazolo[3,4-a]pyridine as a novel, constrained template for fibrinogen receptor (GPIIb/IIIa) antagonists.

Lawson EC, Hoekstra WJ, Addo MF, Andrade-Gordon P, Damiano BP, Kauffman JA, Mitchell JA, Maryanoff BE.

Bioorg Med Chem Lett. 2001 Oct 8;11(19):2619-22.

PMID:
11551763
42.

Administration of a potent antagonist of protease-activated receptor-1 (PAR-1) attenuates vascular restenosis following balloon angioplasty in rats.

Andrade-Gordon P, Derian CK, Maryanoff BE, Zhang HC, Addo MF, Cheung Wm, Damiano BP, D'Andrea MR, Darrow AL, de Garavilla L, Eckardt AJ, Giardino EC, Haertlein BJ, McComsey DF.

J Pharmacol Exp Ther. 2001 Jul;298(1):34-42.

PMID:
11408522
43.

Discovery and optimization of a novel series of thrombin receptor (par-1) antagonists: potent, selective peptide mimetics based on indole and indazole templates.

Zhang HC, Derian CK, Andrade-Gordon P, Hoekstra WJ, McComsey DF, White KB, Poulter BL, Addo MF, Cheung WM, Damiano BP, Oksenberg D, Reynolds EE, Pandey A, Scarborough RM, Maryanoff BE.

J Med Chem. 2001 Mar 29;44(7):1021-4. No abstract available.

PMID:
11297447
44.

Potent, orally active GPIIb/IIIa antagonists containing a nipecotic acid subunit. Structure-activity studies leading to the discovery of RWJ-53308.

Hoekstra WJ, Maryanoff BE, Damiano BP, Andrade-Gordon P, Cohen JH, Costanzo MJ, Haertlein BJ, Hecker LR, Hulshizer BL, Kauffman JA, Keane P, McComsey DF, Mitchell JA, Scott L, Shah RD, Yabut SC.

J Med Chem. 1999 Dec 16;42(25):5254-65.

PMID:
10602710
45.

Altered vascular injury responses in mice deficient in protease-activated receptor-1.

Cheung WM, D'Andrea MR, Andrade-Gordon P, Damiano BP.

Arterioscler Thromb Vasc Biol. 1999 Dec;19(12):3014-24.

PMID:
10591683
46.
47.

Increased expression of protease activated receptor-2 (PAR-2) in balloon-injured rat carotid artery.

Damiano BP, D'Andrea MR, de Garavilla L, Cheung WM, Andrade-Gordon P.

Thromb Haemost. 1999 May;81(5):808-14.

PMID:
10365757
48.

Cardiovascular responses mediated by protease-activated receptor-2 (PAR-2) and thrombin receptor (PAR-1) are distinguished in mice deficient in PAR-2 or PAR-1.

Damiano BP, Cheung WM, Santulli RJ, Fung-Leung WP, Ngo K, Ye RD, Darrow AL, Derian CK, de Garavilla L, Andrade-Gordon P.

J Pharmacol Exp Ther. 1999 Feb;288(2):671-8.

PMID:
9918574
49.

Receptor-activating peptides distinguish thrombin receptor (PAR-1) and protease activated receptor 2 (PAR-2) mediated hemodynamic responses in vivo.

Cheung WM, Andrade-Gordon P, Derian CK, Damiano BP.

Can J Physiol Pharmacol. 1998 Jan;76(1):16-25.

PMID:
9564545
50.

Biological consequences of thrombin receptor deficiency in mice.

Darrow AL, Fung-Leung WP, Ye RD, Santulli RJ, Cheung WM, Derian CK, Burns CL, Damiano BP, Zhou L, Keenan CM, Peterson PA, Andrade-Gordon P.

Thromb Haemost. 1996 Dec;76(6):860-6.

PMID:
8972001

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