G. R. Sitko
United States Military Academy
29 Papers
513 Citations
G. R. Sitko is an academic researcher from United States Military Academy. The author has contributed to research in topics: Glycoprotein IIb/IIIa inhibitors & Fibrinogen receptor. The author has an hindex of 17, co-authored 29 publications.
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Papers
Metabolism-directed optimization of 3-aminopyrazinone acetamide thrombin inhibitors. Development of an orally bioavailable series containing P1 and P3 pyridines
Christopher S. Burgey,Robinson Kyle A,Terry A. Lyle,Sanderson Philip E,S. Dale Lewis,Bobby J. Lucas,Julie A. Krueger,Rominder Singh,Cynthia Miller-Stein,Rebecca B. White,Bradley K. Wong,Elizabeth A. Lyle,Peter D. Williams,Craig A. Coburn,Bruce D. Dorsey,James C. Barrow,Maria T. Stranieri,Marie A. Holahan,G. R. Sitko,Jacquelynn J. Cook,Daniel R. McMasters,Colleen M. McDonough,William M. Sanders,Audrey A. Wallace,Franklin C. Clayton,Dennis L. Bohn,Yvonne M. Leonard,Theodore J. Detwiler,Joseph J. Lynch,Youwei Yan,Zhongguo Chen,Lawrence Kuo,Stephen J. Gardell,Jules A. Shafer,Joseph P. Vacca +34 more
TL;DR: A metabolism-based approach to the optimization of the 3-(2-phenethylamino)-6-methylpyrazinone acetamide template resulted in the modification of each of the three principal components comprising this series.
125
An Antibody Against the Exosite of the Cloned Thrombin Receptor Inhibits Experimental Arterial Thrombosis in the African Green Monkey
Jacquelynn J. Cook,G. R. Sitko,Bohumil Bednar,Cindra L. Condra,M J Mellott,Dong-Mei Feng,Ruth F. Nutt,Jules A. Shafer,Robert J. Gould,Thomas M. Connolly +9 more
TL;DR: It is demonstrated that blockade of the platelet thrombin receptor can prevent arterial thrombosis in this animal model without significantly altering hemostatic parameters and suggest that the throm bin receptor is an attractive antithrombotic target.
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Non-peptide glycoprotein IIb/IIIa antagonists. 11. Design and in vivo evaluation of 3,4-dihydro-1 (1H)-isoquinolinone-based antagonists and ethyl ester prodrugs.
John H. Hutchinson,Jacquelynn J. Cook,Karen M. Brashear,Michael J. Breslin,Joan D. Glass,Robert J. Gould,Wasyl Halczenko,Marie A. Holahan,R. J. Lynch,G. R. Sitko,Maria T. Stranieri,George D. Hartman +11 more
TL;DR: The structure-activity relationship of a series of orally active glycoprotein IIb/IIIa antagonists containing a nitrogen heterocycle grafted onto a 3,4-dihydro-1 (1H)-isoquinolinone core is described and 6d, a potent fibrinogen receptor antagonist able to inhibit the ADP-induced aggregation of human gel-filtered platelets with an IC50 of 12 nM is described.
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Non-Peptide GPIIb/IIIa Inhibitors. 20. Centrally Constrained Thienothiophene α-Sulfonamides Are Potent, Long Acting in Vivo Inhibitors of Platelet Aggregation
Melissa S. Egbertson,Jacquelynn J. Cook,Bohumil Bednar,John D. Prugh,Rodney A. Bednar,Stanley L. Gaul,Robert J. Gould,George D. Hartman,Carl F. Homnick,Marie A. Holahan,Laura A. Libby,Joseph J. Lynch,R. J. Lynch,G. R. Sitko,Maria T. Stranieri,L.M. Vassallo +15 more
TL;DR: Flow cytometry studies revealed that the binding of 4 to resting platelets is a diffusion-controlled process and that 4 binds to dog and human platelets with comparable affinity, indicating a potentially useful and safe separation of efficacy and bleeding time.
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Investigation of (Oxodioxolenyl)methyl Carbamates as Nonchiral Bioreversible Prodrug Moieties for Chiral Amines
Jose Alexander,Bindra Dilbir,Joan D. Glass,Marie A. Holahan,Mara L. Renyer,Gerald S. Rork,G. R. Sitko,Maria T. Stranieri,Raymond F. Stupienski,Hemalata Veerapanane,Jacquelynn J. Cook +10 more
TL;DR: Application of this prodrug strategy to the chiral fibrinogen receptor antagonist L-734,217 resulted in a prodrug that gave quantitative reconversion in rat and dog plasma in vitro and oral bioavailability of 23 +/- 6% in dogs for the parent drug.
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