Search Results - "Haertlein, B J"

Species differences in platelet responses to thrombin and SFLLRN. Receptor-mediated calcium mobilization and aggregation, and regulation by protein kinases by Derian, Claudia K., Santulli, Rosemary J., Tomko, Karen A., Haertlein, Barbara J., Andrade-Gordon, Patricia

“…The thrombin receptor on human platelets is activated by thrombin to stimulate platelet aggregation through the tethered ligand SFLLRN. This study examined the…”
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Administration of a potent antagonist of protease-activated receptor-1 (PAR-1) attenuates vascular restenosis following balloon angioplasty in rats by Andrade-Gordon, P, Derian, C K, Maryanoff, B E, Zhang, H C, Addo, M F, Cheung Wm, Damiano, B P, D'Andrea, M R, Darrow, A L, de Garavilla, L, Eckardt, A J, Giardino, E C, Haertlein, B J, McComsey, D F

“…Human platelets possess two distinct thrombin-activated receptors, PAR-1 (protease-activated receptor-1) and PAR-4, whereas human vascular smooth muscle cells…”
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Positive inotropic and hemodynamic properties of flosequinan, a new vasodilator, and a sulfone metabolite by Falotico, R, Haertlein, B J, Lakas-Weiss, C S, Salata, J J, Tobia, A J

“…Flosequinan, a new orally active vasodilator, and its sulfone metabolite were evaluated for inotropic activity in isolated ferret papillary muscles and…”
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Cardiovascular profile of RWJ 29009, a new potassium channel activator, in anesthetized and conscious dogs by Damiano, B P, Giardino, E C, Haertlein, B J, Stump, G L, Mitchell, J A, Falotico, R

“…RWJ-29009, (6S)-trans(-)-1-(6,7-dihydro-6-hydroxy-5,5-dimethyl-2-nitro-5 H-thieno[3,2-b]pyran-7-yl)-2-piperidinone, is a structurally novel and extremely…”
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Antiplatelet and Antithrombotic Activity of RWJ-53308, A Novel Orally Active Glycoprotein IIb/IIIa Antagonist by Damiano, Bruce P, Mitchell, John A, Giardino, Edward, Corcoran, Thomas, Haertlein, Barbara J, de Garavilla, Lawrence, Kauffman, Jack A, Hoekstra, William J, Maryanoff, Bruce E, Andrade-Gordon, Patricia

“…RWJ-53308 is a novel nonpeptide glycoprotein IIb/IIIa (GPIIb/IIIa) antagonist that inhibits fibrinogen binding to GPIIb/IIIa with an IC 50 of 0.4±0.3 nM…”
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Potent, Orally Active GPIIb/IIIa Antagonists Containing a Nipecotic Acid Subunit. Structure−Activity Studies Leading to the Discovery of RWJ-53308 by Hoekstra, William J, Maryanoff, Bruce E, Damiano, Bruce P, Andrade-Gordon, Patricia, Cohen, Judith H, Costanzo, Michael J, Haertlein, Barbara J, Hecker, Leonard R, Hulshizer, Becky L, Kauffman, Jack A, Keane, Patricia, McComsey, David F, Mitchell, John A, Scott, Lorraine, Shah, Rekha D, Yabut, Stephen C

“…Although intravenously administered antiplatelet fibrinogen receptor (GPIIb/IIIa) antagonists have become established in the acute-care clinical setting for…”
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A novel, potent dual inhibitor of the leukocyte proteases cathepsin G and chymase: molecular mechanisms and anti-inflammatory activity in vivo by de Garavilla, Lawrence, Greco, Michael N, Sukumar, Narayanasami, Chen, Zhi-Wei, Pineda, Agustin O, Mathews, F Scott, Di Cera, Enrico, Giardino, Edward C, Wells, Grace I, Haertlein, Barbara J, Kauffman, Jack A, Corcoran, Thomas W, Derian, Claudia K, Eckardt, Annette J, Damiano, Bruce P, Andrade-Gordon, Patricia, Maryanoff, Bruce E

“…Certain leukocytes release serine proteases that sustain inflammatory processes and cause disease conditions, such as asthma and chronic obstructive pulmonary…”
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In-Depth Study of Tripeptide-Based alpha -Ketoheterocycles as Inhibitors of Thrombin. Effective Utilization of the S sub(1)' Subsite and Its Implications to Structure-Based Drug Design by Costanzo, MJ, Almond, HR Jr, Hecker, L R, Schott, M R, Yabut, S C, Zhang, H-C, Andrade-Gordon, P, Corcoran, T W, Giardino, E C, Kauffman, JA, Lewis, J M, de Garavilla, L, Haertlein, B J, Maryanoff, B E

“…Thrombin inhibitors are potentially useful in medicine for their anticoagulant and antithrombotic effects. We synthesized and evaluated diverse…”
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In-Depth Study of Tripeptide-Based α-Ketoheterocycles as Inhibitors of Thrombin. Effective Utilization of the S 1 ‘ Subsite and Its Implications to Structure-Based Drug Design by Costanzo, Michael J., Almond, Harold R., Hecker, Leonard R., Schott, Mary R., Yabut, Stephen C., Zhang, Han-Cheng, Andrade-Gordon, Patricia, Corcoran, Thomas W., Giardino, Edward C., Kauffman, Jack A., Lewis, Joan M., de Garavilla, Lawrence, Haertlein, Barbara J., Maryanoff, Bruce E.

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Novel thieno[2,3-b]- and [3,4-b]pyrans as potassium channel openers. Thiophene systems--XVII by Press, J B, McNally, J J, Sanfilippo, P J, Addo, M F, Loughney, D, Giardino, E, Katz, L B, Falotico, R, Haertlein, B J

“…The syntheses and antihypertensive activity of the thieno[3,4-b]pyran and thieno[2,3-b]pyran isosteres of the potassium channel opener (PCO) RWJ 26629 (+/- 2a)…”
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Solid-phase parallel synthesis applied to lead optimization: Discovery of potent analogues of the GPIIb/IIIa antagonist RWJ-50042 by Hoekstra, William J., Maryanoff, Bruce E., Andrade-Gordon, Patricia, Cohen, Judith H., Costanzo, Michael J., Damiano, Bruce P., Haertlein, Barbara J., Harris, Bruce D., Kauffman, Jack A., Keane, Patricia M., McComsey, David F., Villani, Frank J., Yabut, Stephen C.

“…A study of β-turn peptide mimetics, related to the C-terminal γ-chain of fibrinogen and containing a nipecotic acid scaffold, led to RWJ-50042 ( 1), an…”
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