Mitsi A Blount

Summary

Affiliation: Vanderbilt University
Country: USA

Publications

  1. ncbi request reprint Binding of tritiated sildenafil, tadalafil, or vardenafil to the phosphodiesterase-5 catalytic site displays potency, specificity, heterogeneity, and cGMP stimulation
    Mitsi A Blount
    Department of Molecular Physiology and Biophysics, Vanderbilt University School of Medicine, Nashville, TN 37232 0615, USA
    Mol Pharmacol 66:144-52. 2004
  2. ncbi request reprint Conversion of phosphodiesterase-5 (PDE5) catalytic site to higher affinity by PDE5 inhibitors
    Mitsi A Blount
    Department of Molecular Physiology and Biophysics, Light Hall Room 702, Vanderbilt University School of Medicine, Nashville, TN 37232 0615, USA
    J Pharmacol Exp Ther 323:730-7. 2007
  3. ncbi request reprint Phosphorylation of phosphodiesterase-5 is promoted by a conformational change induced by sildenafil, vardenafil, or tadalafil
    Emmanuel P Bessay
    Department of Molecular Physiology and Biophysics, Vanderbilt University School of Medicine, Nashville, Tennessee 37232 0615, USA
    Front Biosci 12:1899-910. 2007
  4. ncbi request reprint A 46-amino acid segment in phosphodiesterase-5 GAF-B domain provides for high vardenafil potency over sildenafil and tadalafil and is involved in phosphodiesterase-5 dimerization
    Mitsi A Blount
    Department of Molecular Physiology and Biophysics, 702 Light Hall, Vanderbilt University School of Medicine, Nashville, TN 37232 0615, USA
    Mol Pharmacol 70:1822-31. 2006
  5. doi request reprint Phosphorylation increases affinity of the phosphodiesterase-5 catalytic site for tadalafil
    Emmanuel P Bessay
    Department of Molecular Physiology and Biophysics, 702 Light Hall, Vanderbilt University School of Medicine, Nashville, TN 37232 0615, USA
    J Pharmacol Exp Ther 325:62-8. 2008
  6. ncbi request reprint Radiolabeled ligand binding to the catalytic or allosteric sites of PDE5 and PDE11
    James L Weeks
    Department of Molecular Physiology and Biophysics, Vanderbilt University School of Medicine, Nashville, TN, USA
    Methods Mol Biol 307:239-62. 2005
  7. ncbi request reprint High lung PDE5: a strong basis for treating pulmonary hypertension with PDE5 inhibitors
    Jackie D Corbin
    Department of Molecular Physiology and Biophysics, Vanderbilt University School of Medicine, Nashville, TN 37232 0615, USA
    Biochem Biophys Res Commun 334:930-8. 2005
  8. ncbi request reprint Vardenafil: structural basis for higher potency over sildenafil in inhibiting cGMP-specific phosphodiesterase-5 (PDE5)
    Jackie D Corbin
    Department of Molecular Physiology and Biophysics, Vanderbilt University School of Medicine, 702 Light Hall, Nashville, TN 37232 0615, USA
    Neurochem Int 45:859-63. 2004
  9. ncbi request reprint Allosteric sites of phosphodiesterase-5 sequester cyclic GMP
    Jun Kotera
    Department of Molecular Physiology and Biophysics, Vanderbilt University School of Medicine, Nashville, TN 37232 0615, USA
    Front Biosci 9:378-86. 2004
  10. ncbi request reprint [3H]sildenafil binding to phosphodiesterase-5 is specific, kinetically heterogeneous, and stimulated by cGMP
    Jackie D Corbin
    Department of Molecular Physiology and Biophysics, Vanderbilt University School of Medicine, 702 Light Hall, Nashville, TN 37232 0615, USA
    Mol Pharmacol 63:1364-72. 2003

Collaborators

Detail Information

Publications14

  1. ncbi request reprint Binding of tritiated sildenafil, tadalafil, or vardenafil to the phosphodiesterase-5 catalytic site displays potency, specificity, heterogeneity, and cGMP stimulation
    Mitsi A Blount
    Department of Molecular Physiology and Biophysics, Vanderbilt University School of Medicine, Nashville, TN 37232 0615, USA
    Mol Pharmacol 66:144-52. 2004
    ..Without inhibitor present, cGMP accumulation would stimulate cGMP degradation, but with inhibitor present, this negative feedback process would be blocked...
  2. ncbi request reprint Conversion of phosphodiesterase-5 (PDE5) catalytic site to higher affinity by PDE5 inhibitors
    Mitsi A Blount
    Department of Molecular Physiology and Biophysics, Light Hall Room 702, Vanderbilt University School of Medicine, Nashville, TN 37232 0615, USA
    J Pharmacol Exp Ther 323:730-7. 2007
    ..This effect is predicted to improve the substrate affinity or inhibitory potencies of these compounds in intact cells...
  3. ncbi request reprint Phosphorylation of phosphodiesterase-5 is promoted by a conformational change induced by sildenafil, vardenafil, or tadalafil
    Emmanuel P Bessay
    Department of Molecular Physiology and Biophysics, Vanderbilt University School of Medicine, Nashville, Tennessee 37232 0615, USA
    Front Biosci 12:1899-910. 2007
    ....
  4. ncbi request reprint A 46-amino acid segment in phosphodiesterase-5 GAF-B domain provides for high vardenafil potency over sildenafil and tadalafil and is involved in phosphodiesterase-5 dimerization
    Mitsi A Blount
    Department of Molecular Physiology and Biophysics, 702 Light Hall, Vanderbilt University School of Medicine, Nashville, TN 37232 0615, USA
    Mol Pharmacol 70:1822-31. 2006
    ..This is the first evidence that PDE5 R domain, and GAF-B in particular, influences affinity and selectivity of the catalytic site for certain classes of inhibitors...
  5. doi request reprint Phosphorylation increases affinity of the phosphodiesterase-5 catalytic site for tadalafil
    Emmanuel P Bessay
    Department of Molecular Physiology and Biophysics, 702 Light Hall, Vanderbilt University School of Medicine, Nashville, TN 37232 0615, USA
    J Pharmacol Exp Ther 325:62-8. 2008
    ..By increasing the affinity of the catalytic site, phosphorylation should also consequently increase the potency and duration of PDE5 inhibitor action...
  6. ncbi request reprint Radiolabeled ligand binding to the catalytic or allosteric sites of PDE5 and PDE11
    James L Weeks
    Department of Molecular Physiology and Biophysics, Vanderbilt University School of Medicine, Nashville, TN, USA
    Methods Mol Biol 307:239-62. 2005
    ..These techniques have also been successfully applied to the study of binding of radiolabeled PDE5 inhibitors to PDE11, suggesting that these methods are applicable to the study of other PDEs, and perhaps other enzyme families...
  7. ncbi request reprint High lung PDE5: a strong basis for treating pulmonary hypertension with PDE5 inhibitors
    Jackie D Corbin
    Department of Molecular Physiology and Biophysics, Vanderbilt University School of Medicine, Nashville, TN 37232 0615, USA
    Biochem Biophys Res Commun 334:930-8. 2005
    ..The PDE5 level was one-half that of PKG in heart. Thus, abundance of PDE5 in lung vascular smooth muscle provides a strong molecular basis for PDE5 inhibitor treatment of pulmonary hypertension...
  8. ncbi request reprint Vardenafil: structural basis for higher potency over sildenafil in inhibiting cGMP-specific phosphodiesterase-5 (PDE5)
    Jackie D Corbin
    Department of Molecular Physiology and Biophysics, Vanderbilt University School of Medicine, 702 Light Hall, Nashville, TN 37232 0615, USA
    Neurochem Int 45:859-63. 2004
    ....
  9. ncbi request reprint Allosteric sites of phosphodiesterase-5 sequester cyclic GMP
    Jun Kotera
    Department of Molecular Physiology and Biophysics, Vanderbilt University School of Medicine, Nashville, TN 37232 0615, USA
    Front Biosci 9:378-86. 2004
    ..This could provide for negative feedback control of cGMP-signaling...
  10. ncbi request reprint [3H]sildenafil binding to phosphodiesterase-5 is specific, kinetically heterogeneous, and stimulated by cGMP
    Jackie D Corbin
    Department of Molecular Physiology and Biophysics, Vanderbilt University School of Medicine, 702 Light Hall, Nashville, TN 37232 0615, USA
    Mol Pharmacol 63:1364-72. 2003
    ..The data also indicate that after physiological elevation, cGMP may directly stimulate the catalytic site by binding to the allosteric cGMP-binding sites of PDE5, thus causing negative feedback on this pathway...
  11. ncbi request reprint Molecular properties of mammalian proteins that interact with cGMP: protein kinases, cation channels, phosphodiesterases, and multi-drug anion transporters
    Sharron H Francis
    Department of Molecular Physiology and Biophysics, Vanderbilt University School of Medicine, Nashville, TN 37232 0615, USA
    Front Biosci 10:2097-117. 2005
    ....
  12. doi request reprint Mammalian cyclic nucleotide phosphodiesterases: molecular mechanisms and physiological functions
    Sharron H Francis
    Department of Molecular Physiology and Biophysics, Vanderbilt University School of Medicine, Nashville, Tennessee 37232 0615, USA
    Physiol Rev 91:651-90. 2011
    ..The many recent advances in understanding PDE structures, functions, and physiological actions are discussed in this review...
  13. ncbi request reprint Forskolin stimulates phosphorylation and membrane accumulation of UT-A3
    Mitsi A Blount
    Renal Division, Emory University School of Medicine, Atlanta, GA 30322, USA
    Am J Physiol Renal Physiol 293:F1308-13. 2007
    ....
  14. pmc Phosphorylation of UT-A1 urea transporter at serines 486 and 499 is important for vasopressin-regulated activity and membrane accumulation
    Mitsi A Blount
    Renal Division, Department of Medicine, Emory University School of Medicine, Atlanta, GA 30322, USA
    Am J Physiol Renal Physiol 295:F295-9. 2008
    ..We conclude that the phosphorylation of UT-A1 on both serines 486 and 499 is important for activity and that this phosphorylation may be involved in UT-A1 membrane accumulation...