Stephen M Soisson

Summary

Affiliation: Merck Research Laboratories
Country: USA

Publications

  1. pmc Identification of a potent synthetic FXR agonist with an unexpected mode of binding and activation
    Stephen M Soisson
    Merck Research Laboratories, POB 2000, Rahway, NJ 07065, USA
    Proc Natl Acad Sci U S A 105:5337-42. 2008
  2. pmc Structural definition and substrate specificity of the S28 protease family: the crystal structure of human prolylcarboxypeptidase
    Stephen M Soisson
    Global Structural Biology, Merck Research Laboratories, P, O, Box 4, West Point, PA 19486, USA
    BMC Struct Biol 10:16. 2010
  3. ncbi request reprint Synthesis and biological evaluation of platensimycin analogs
    Hong C Shen
    Departments of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065 0900, USA
    Bioorg Med Chem Lett 19:1623-7. 2009
  4. ncbi request reprint Isolation, enzyme-bound structure and antibacterial activity of platencin A1 from Streptomyces platensis
    Sheo B Singh
    Merck Research Laboratories, Rahway, NJ 07065, USA
    Bioorg Med Chem Lett 19:4756-9. 2009
  5. pmc Expression, purification and crystallization of human prolylcarboxypeptidase
    Pravien D Abeywickrema
    Global Structural Biology, Merck Research Laboratories, West Point, PA 19486, USA
    Acta Crystallogr Sect F Struct Biol Cryst Commun 66:702-5. 2010
  6. doi request reprint Mechanism of action of the cell-division inhibitor PC190723: modulation of FtsZ assembly cooperativity
    Nathaniel L Elsen
    Screening and Protein Sciences, Merck Research Laboratories, West Point, Pennsylvania 19486, United States
    J Am Chem Soc 134:12342-5. 2012
  7. pmc Structural basis for selective small molecule kinase inhibition of activated c-Met
    Keith W Rickert
    Global Structural Biology, Merck Research Laboratories, West Point, Pennsylvania 19486, USA
    J Biol Chem 286:11218-25. 2011
  8. doi request reprint Surface-entropy reduction approaches to manipulate crystal forms of beta-ketoacyl acyl carrier protein synthase II from Streptococcus pneumoniae
    Gopalakrishnan Parthasarathy
    Merck Research Laboratories, Rahway, NJ, USA
    Acta Crystallogr D Biol Crystallogr 64:141-8. 2008
  9. doi request reprint Discovery of a highly potent, selective, and bioavailable soluble epoxide hydrolase inhibitor with excellent ex vivo target engagement
    Hong C Shen
    Merck Research Laboratories, Merck and Co, Inc, Rahway, NJ 07065 0900, USA
    J Med Chem 52:5009-12. 2009
  10. ncbi request reprint Platensimycin is a selective FabF inhibitor with potent antibiotic properties
    Jun Wang
    Merck Research Laboratories, Rahway, New Jersey 07065, USA
    Nature 441:358-61. 2006

Collaborators

Detail Information

Publications12

  1. pmc Identification of a potent synthetic FXR agonist with an unexpected mode of binding and activation
    Stephen M Soisson
    Merck Research Laboratories, POB 2000, Rahway, NJ 07065, USA
    Proc Natl Acad Sci U S A 105:5337-42. 2008
    ..The structure of the FXR:MFA-1 complex differs significantly from that of the complex with a structurally distinct agonist, fexaramine, highlighting the inherent plasticity of the receptor...
  2. pmc Structural definition and substrate specificity of the S28 protease family: the crystal structure of human prolylcarboxypeptidase
    Stephen M Soisson
    Global Structural Biology, Merck Research Laboratories, P, O, Box 4, West Point, PA 19486, USA
    BMC Struct Biol 10:16. 2010
    ..The structural basis of the different substrate specificities of the two enzymes is not understood nor has the structure of the S28 fold been described...
  3. ncbi request reprint Synthesis and biological evaluation of platensimycin analogs
    Hong C Shen
    Departments of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065 0900, USA
    Bioorg Med Chem Lett 19:1623-7. 2009
    ..The medicinal chemistry efforts were focused on the modification of the enone moiety of platensimycin and several analogs showed significant activity against FabF and possess antibacterial activity...
  4. ncbi request reprint Isolation, enzyme-bound structure and antibacterial activity of platencin A1 from Streptomyces platensis
    Sheo B Singh
    Merck Research Laboratories, Rahway, NJ 07065, USA
    Bioorg Med Chem Lett 19:4756-9. 2009
    ..Isolation, structure, enzyme-bound structure and activity of platencin A(1) and two other congeners have been described...
  5. pmc Expression, purification and crystallization of human prolylcarboxypeptidase
    Pravien D Abeywickrema
    Global Structural Biology, Merck Research Laboratories, West Point, PA 19486, USA
    Acta Crystallogr Sect F Struct Biol Cryst Commun 66:702-5. 2010
    ..Purified PrCP yielded crystals belonging to space group R32, with unit-cell parameters a = b = 181.14, c = 240.13 A, that diffracted to better than 2.8 A resolution...
  6. doi request reprint Mechanism of action of the cell-division inhibitor PC190723: modulation of FtsZ assembly cooperativity
    Nathaniel L Elsen
    Screening and Protein Sciences, Merck Research Laboratories, West Point, Pennsylvania 19486, United States
    J Am Chem Soc 134:12342-5. 2012
    ..Together, the results reveal the molecular mechanism of FtsZ modulation by PC190723 and a conformational switch to the high-affinity state that enables polymer assembly...
  7. pmc Structural basis for selective small molecule kinase inhibition of activated c-Met
    Keith W Rickert
    Global Structural Biology, Merck Research Laboratories, West Point, Pennsylvania 19486, USA
    J Biol Chem 286:11218-25. 2011
    ..The results highlight the role of structural plasticity within the kinase domain in imparting the specificity of ligand binding and provide the framework for structure-guided design of activated c-Met inhibitors...
  8. doi request reprint Surface-entropy reduction approaches to manipulate crystal forms of beta-ketoacyl acyl carrier protein synthase II from Streptococcus pneumoniae
    Gopalakrishnan Parthasarathy
    Merck Research Laboratories, Rahway, NJ, USA
    Acta Crystallogr D Biol Crystallogr 64:141-8. 2008
    ..75 A resolution reveals that one of the mutations, E383A, appears to play a key role in disfavouring the less desirable triclinic crystal form and in generating a new surface for a packing interaction that stabilizes the new crystal form...
  9. doi request reprint Discovery of a highly potent, selective, and bioavailable soluble epoxide hydrolase inhibitor with excellent ex vivo target engagement
    Hong C Shen
    Merck Research Laboratories, Merck and Co, Inc, Rahway, NJ 07065 0900, USA
    J Med Chem 52:5009-12. 2009
    ..With minimal off-target activity and a good PK profile, the benchmark 2d exhibited remarkable in vitro and ex vivo target engagement. The eutomer entA-2d also elicited vasodilation effect in rat mesenteric artery...
  10. ncbi request reprint Platensimycin is a selective FabF inhibitor with potent antibiotic properties
    Jun Wang
    Merck Research Laboratories, Rahway, New Jersey 07065, USA
    Nature 441:358-61. 2006
    ..Platensimycin is the most potent inhibitor reported for the FabF/B condensing enzymes, and is the only inhibitor of these targets that shows broad-spectrum activity, in vivo efficacy and no observed toxicity...
  11. ncbi request reprint Reducing the peptidyl features of caspase-3 inhibitors: a structural analysis
    Joseph W Becker
    Departments of Medicinal Chemistry and Metabolic Disorders, Merck Research Laboratory, PO Box 2000, Rahway, New Jersey 07065, USA
    J Med Chem 47:2466-74. 2004
    ..These results advance the search for caspase-directed drugs by revealing how unacceptable molecular features can be removed without loss of potency...
  12. doi request reprint Restoring methicillin-resistant Staphylococcus aureus susceptibility to β-lactam antibiotics
    Christopher M Tan
    Infectious Diseases, Merck Research Laboratories, Kenilworth, NJ 07033, USA
    Sci Transl Med 4:126ra35. 2012
    ..Collectively, these data support a target-based approach to rationally develop synergistic combination agents that mitigate drug resistance and effectively treat MRSA infections...