Jovita Marcinkeviciene

Summary

Affiliation: Bristol-Myers Squibb
Country: USA

Publications

  1. ncbi Novel inhibition of porcine pepsin by a substituted piperidine. Preference for one of the enzyme conformers
    Jovita Marcinkeviciene
    Department of Chemical Enzymology, Bristol Myers Squibb Pharmaceutical Company, Wilmington, Delaware 19880 0400, USA
    J Biol Chem 277:28677-82. 2002
  2. ncbi Mechanism of Gly-Pro-pNA cleavage catalyzed by dipeptidyl peptidase-IV and its inhibition by saxagliptin (BMS-477118)
    Young B Kim
    Department of Chemical Enzymology, Bristol Myers Squibb Pharmaceutical Company, Pharmaceutical Research Institute, P O Box 5400, Princeton, NJ 08543 5400, USA
    Arch Biochem Biophys 445:9-18. 2006
  3. ncbi Probing prime substrate binding sites of human dipeptidyl peptidase-IV using competitive substrate approach
    Lisa M Kopcho
    Department of Chemical Enzymology, Pharmaceutical Research Institute, Bristol Myers Squibb Pharmaceutical Company, P O Box 5400, Princeton, NJ 08543 5400, USA
    Arch Biochem Biophys 436:367-76. 2005
  4. ncbi Comparative studies of active site-ligand interactions among various recombinant constructs of human beta-amyloid precursor protein cleaving enzyme
    Lisa M Kopcho
    Department of Chemical Enzymology, Hopewell, NJ, USA
    Arch Biochem Biophys 410:307-16. 2003
  5. doi Differential activation of recombinant human acetyl-CoA carboxylases 1 and 2 by citrate
    Gregory A Locke
    Department of Chemical Enzymology, Bristol Myers Squibb Pharmaceutical Company, R and D, P O Box 5400, Princeton, NJ 08543 5400, USA
    Arch Biochem Biophys 475:72-9. 2008
  6. ncbi A pre-steady state analysis of ligand binding to human glucokinase: evidence for a preexisting equilibrium
    Young B Kim
    Department of Chemical Enzymology, Bristol Myers Squibb Pharmaceutical Company, Pharmaceutical Research Institute, P O Box 5400, Princeton, New Jersey 08543 5400, USA
    Biochemistry 46:1423-31. 2007
  7. ncbi Kinetic studies on beta-site amyloid precursor protein-cleaving enzyme (BACE). Confirmation of an iso mechanism
    Larisa Toulokhonova
    Department of Chemical Enzymology, Bristol Myers Squibb Pharmaceutical Company, Wilmington, Delaware 19880 0400, USA
    J Biol Chem 278:4582-9. 2003
  8. doi P-glycoprotein efflux and other factors limit brain amyloid beta reduction by beta-site amyloid precursor protein-cleaving enzyme 1 inhibitors in mice
    Jere E Meredith
    Research and Development, Bristol Myers Squibb, 5 Research Parkway, Wallingford, CT, USA
    J Pharmacol Exp Ther 326:502-13. 2008
  9. pmc Involvement of DPP-IV catalytic residues in enzyme-saxagliptin complex formation
    William J Metzler
    Department of Molecular Biosciences, Bristol Myers Squibb Research and Development, Princeton, New Jersey 08543 4000, USA
    Protein Sci 17:240-50. 2008
  10. doi Discovery of 6-(aminomethyl)-5-(2,4-dichlorophenyl)-7-methylimidazo[1,2-a]pyrimidine-2-carboxamides as potent, selective dipeptidyl peptidase-4 (DPP4) inhibitors
    Wei Meng
    Departments of Discovery Chemistry, Bristol Myers Squibb, Research and Development, Princeton, New Jersey 08543 5400, USA
    J Med Chem 53:5620-8. 2010

Collaborators

Detail Information

Publications16

  1. ncbi Novel inhibition of porcine pepsin by a substituted piperidine. Preference for one of the enzyme conformers
    Jovita Marcinkeviciene
    Department of Chemical Enzymology, Bristol Myers Squibb Pharmaceutical Company, Wilmington, Delaware 19880 0400, USA
    J Biol Chem 277:28677-82. 2002
    ..Taken together, these data suggest that the enzyme can readily interconvert between two conformers, one capable of binding substrate and pepstatin A and the other capable of binding the substituted piperidine...
  2. ncbi Mechanism of Gly-Pro-pNA cleavage catalyzed by dipeptidyl peptidase-IV and its inhibition by saxagliptin (BMS-477118)
    Young B Kim
    Department of Chemical Enzymology, Bristol Myers Squibb Pharmaceutical Company, Pharmaceutical Research Institute, P O Box 5400, Princeton, NJ 08543 5400, USA
    Arch Biochem Biophys 445:9-18. 2006
    ..4 and 14.1 ppm were observed upon mixing the enzyme with saxagliptin. Fractionation factors (phi) of 0.6 and 0.5 for the 17.4 and 14.1 ppm peaks, respectively, are suggestive of short strong hydrogen bonds in the enzyme-inhibitor complex...
  3. ncbi Probing prime substrate binding sites of human dipeptidyl peptidase-IV using competitive substrate approach
    Lisa M Kopcho
    Department of Chemical Enzymology, Pharmaceutical Research Institute, Bristol Myers Squibb Pharmaceutical Company, P O Box 5400, Princeton, NJ 08543 5400, USA
    Arch Biochem Biophys 436:367-76. 2005
    ....
  4. ncbi Comparative studies of active site-ligand interactions among various recombinant constructs of human beta-amyloid precursor protein cleaving enzyme
    Lisa M Kopcho
    Department of Chemical Enzymology, Hopewell, NJ, USA
    Arch Biochem Biophys 410:307-16. 2003
    ..Thus, the use of the nonglycosylated, soluble catalytic domain of BACE is appropriate for studies aimed at understanding the determinants of ligand recognition by the enzyme active site...
  5. doi Differential activation of recombinant human acetyl-CoA carboxylases 1 and 2 by citrate
    Gregory A Locke
    Department of Chemical Enzymology, Bristol Myers Squibb Pharmaceutical Company, R and D, P O Box 5400, Princeton, NJ 08543 5400, USA
    Arch Biochem Biophys 475:72-9. 2008
    ..Taken together, these data suggest that recombinant human ACC1 and ACC2 are differentially activated by citrate, most likely through conformational changes leading to aggregation, with ACC2 being more sensitive to this activator...
  6. ncbi A pre-steady state analysis of ligand binding to human glucokinase: evidence for a preexisting equilibrium
    Young B Kim
    Department of Chemical Enzymology, Bristol Myers Squibb Pharmaceutical Company, Pharmaceutical Research Institute, P O Box 5400, Princeton, New Jersey 08543 5400, USA
    Biochemistry 46:1423-31. 2007
    ..In conclusion, our data support control of GK activity and Km through the ratio of distinct conformers (super-open, open, and closed) through either substrate or other ligand binding and/or dissociation...
  7. ncbi Kinetic studies on beta-site amyloid precursor protein-cleaving enzyme (BACE). Confirmation of an iso mechanism
    Larisa Toulokhonova
    Department of Chemical Enzymology, Bristol Myers Squibb Pharmaceutical Company, Wilmington, Delaware 19880 0400, USA
    J Biol Chem 278:4582-9. 2003
    ....
  8. doi P-glycoprotein efflux and other factors limit brain amyloid beta reduction by beta-site amyloid precursor protein-cleaving enzyme 1 inhibitors in mice
    Jere E Meredith
    Research and Development, Bristol Myers Squibb, 5 Research Parkway, Wallingford, CT, USA
    J Pharmacol Exp Ther 326:502-13. 2008
    ....
  9. pmc Involvement of DPP-IV catalytic residues in enzyme-saxagliptin complex formation
    William J Metzler
    Department of Molecular Biosciences, Bristol Myers Squibb Research and Development, Princeton, New Jersey 08543 4000, USA
    Protein Sci 17:240-50. 2008
    ..Together with the previously published enzymatic data, the structural and binding data presented here strongly support a histidine-assisted covalent bond formation between S630 hydroxyl oxygen and the nitrile group of saxagliptin...
  10. doi Discovery of 6-(aminomethyl)-5-(2,4-dichlorophenyl)-7-methylimidazo[1,2-a]pyrimidine-2-carboxamides as potent, selective dipeptidyl peptidase-4 (DPP4) inhibitors
    Wei Meng
    Departments of Discovery Chemistry, Bristol Myers Squibb, Research and Development, Princeton, New Jersey 08543 5400, USA
    J Med Chem 53:5620-8. 2010
    ....
  11. ncbi Diprolyl nitriles as potent dipeptidyl peptidase IV inhibitors
    Guohua Zhao
    Department of Discovery Chemistry, Bristol Myers Squibb, Pharmaceutical Research Institute, P O Box 5400, Princeton, NJ 08543 5400, USA
    Bioorg Med Chem Lett 15:3992-5. 2005
    ..Synthesis and structure-activity relationships of a series of substituted diprolyl nitriles are described, leading to the identification of compound 1 with a measured DPP4 K(i) of 3.6 nM...
  12. ncbi Discovery and preclinical profile of Saxagliptin (BMS-477118): a highly potent, long-acting, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes
    David J Augeri
    Department of Discovery Chemistry, Bristol Myers Squibb, Pharmaceutical Research Institute, P O Box 5400, Princeton, New Jersey 08543 5400, USA
    J Med Chem 48:5025-37. 2005
    ....
  13. ncbi Parallel synthesis of potent, pyrazole-based inhibitors of Helicobacter pylori dihydroorotate dehydrogenase
    Tasir S Haque
    Department of Medicinal Chemistry, Bristol Myers Squibb Company, Experimental Station, Route 141 and Henry Clay Road, Wilmington, Delaware 19880, USA
    J Med Chem 45:4669-78. 2002
    ..pylori DHODase, sub-microg/mL H. pylori minimum inhibitory concentration activity, low molecular weight, and >10 000-fold selectivity over human DHODase...
  14. ncbi Potent non-nitrile dipeptidic dipeptidyl peptidase IV inhibitors
    Ligaya M Simpkins
    Bristol Myers Squibb Research and Development, PO Box 5400, Princeton, NJ 08543 5400, USA
    Bioorg Med Chem Lett 17:6476-80. 2007
    ..A unique potency enhancement was achieved with beta-branched natural and unnatural amino acids, particularly adamantylglycines, linked to a (2S,3R)-2,3-methanopyrrolidine based scaffold...
  15. ncbi Seco-prolinenitrile inhibitors of dipeptidyl peptidase IV define minimal pharmacophore requirements at P1
    David R Magnin
    Department of Discovery Chemistry, Bristol Myers Squibb, Pharmaceutical Research Institute, PO Box 5400, Princeton, NJ 08543 5400, USA
    Bioorg Med Chem Lett 16:1731-4. 2006
    ..The inhibitors described herein assess the minimum structural requirements at P1 for this enzyme, resulting in the identification of inhibitors with low nM potency...
  16. doi [3H]BMS-599240--a novel tritiated ligand for the characterization of BACE1 inhibitors
    Lawrence G Iben
    Neuroscience Biology, Bristol Myers Squibb Research and Development, Wallingford, CT 06492, USA
    Eur J Pharmacol 593:10-5. 2008
    ..Thus, the radioligand [(3)H]BMS-599240 is a novel tool potentially useful for evaluation of BACE1 enzyme in biological samples, and for evaluation of inhibitor binding to BACE1...