SamuelLyleGrahamIIIMD

PubMed

• Discovery of pyrrolidine-based ?-secretase inhibitors: Lead advancement through conformational design for maintenance of ligand binding efficiency.
  Stachel, S.J., Steele, T.G., Petrocchi, A., Haugabook, S.J., McGaughey, G., Katharine Holloway, M., Allison, T., Munshi, S., Zuck, P., Colussi, D., Tugasheva, K., Wolf...> ;Bioorg Med Chem Lett. 2012 Jan 1
• Identification of a novel RAMP-independent CGRP receptor antagonist.
  Zartman, C.B., Bell, I.M., Gallicchio, S.N., Graham, S.L., Kane, S.A., Mallee, J.J., Rutledge, R.Z., Salvatore, C.A., Vacca, J.P., Williams, T.M.> ;Bioorg Med Chem Lett. 2011 Nov 15
• Pharmacological properties of MK-3207, a potent and orally active calcitonin gene-related peptide receptor antagonist.
  Salvatore, C.A., Moore, E.L., Calamari, A., Cook, J.J., Michener, M.S., O'Malley, S., Miller, P.J., Sur, C., Williams, D.L., Zeng, Z., Danziger, A., Lynch, J.J., Regan...> ;J Pharmacol Exp Ther. 2010 Apr
• First demonstration of cerebrospinal fluid and plasma A beta lowering with oral administration of a beta-site amyloid precursor protein-cleaving enzyme 1 inhibitor in ...
  Sankaranarayanan, S., Holahan, M.A., Colussi, D., Crouthamel, M., Devanarayan, V., Ellis, J., Espeseth, A., Gates, A.T., Graham, S.L., Gregro, A.R., Hazuda, D., Hochma...> ;J Pharmacol Exp Ther. 2009-01-01
• Discovery and X-ray crystallographic analysis of a spiropiperidine iminohydantoin inhibitor of beta-secretase.
  Barrow, J.C., Stauffer, S.R., Rittle, K.E., Ngo, P.L., Yang, Z., Selnick, H.G., Graham, S.L., Munshi, S., McGaughey, G.B., Holloway, M.K., Simon, A.J., Price, E.A., Sa...> ;J Med Chem. 2008-10-23
• Synthesis of the (3R,6S)-3-amino-6-(2,3-difluorophenyl)azepan-2-one of telcagepant (MK-0974), a calcitonin gene-related peptide receptor antagonist for the treatment o...
  Burgey, C.S., Paone, D.V., Shaw, A.W., Deng, J.Z., Nguyen, D.N., Potteiger, C.M., Graham, S.L., Vacca, J.P., Williams, T.M.> ;Org Lett. 2008 Aug 7
• Pharmacological characterization of MK-0974 [N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin...
  Salvatore, C.A., Hershey, J.C., Corcoran, H.A., Fay, J.F., Johnston, V.K., Moore, E.L., Mosser, S.D., Burgey, C.S., Paone, D.V., Shaw, A.W., Graham, S.L., Vacca, J.P.,...> ;J Pharmacol Exp Ther. 2008 Feb
• Potent, orally bioavailable calcitonin gene-related peptide receptor antagonists for the treatment of migraine: discovery of N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1-...
  Paone, D.V., Shaw, A.W., Nguyen, D.N., Burgey, C.S., Deng, J.Z., Kane, S.A., Koblan, K.S., Salvatore, C.A., Mosser, S.D., Johnston, V.K., Wong, B.K., Miller-Stein, C.M...> ;J Med Chem. 2007 Nov 15
• Discovery of isonicotinamide derived beta-secretase inhibitors: in vivo reduction of beta-amyloid.
  Stanton, M.G., Stauffer, S.R., Gregro, A.R., Steinbeiser, M., Nantermet, P., Sankaranarayanan, S., Price, E.A., Wu, G., Crouthamel, M., Ellis, J., Lai, M., Espeseth, A...> ;J Med Chem. 2007 Jul 26
• Discovery of oxadiazoyl tertiary carbinamine inhibitors of beta-secretase (BACE-1).
  Rajapakse HA, Nantermet PG, Selnick HG, Munshi S, McGaughey GB, Lindsley SR, Young MB, Lai M, Espeseth AS, Shi X, Colussi D, Pietrak B, Crouthamel M, Tugusheva K, Huan...> ;J. Med. Chem.. 2006-12-14
• Macrocyclic inhibitors of beta-secretase: functional activity in an animal model.
  Stachel, S.J., Coburn, C.A., Sankaranarayanan, S., Price, E.A., Wu, G., Crouthamel, M., Pietrak, B.L., Huang, Q., Lineberger, J., Espeseth, A.S., Jin, L., Ellis, J., H...> ;J Med Chem. 2006 Oct 19
• Biochemical and structural characterization of a novel class of inhibitors of the type 1 insulin-like growth factor and insulin receptor kinases.
  Mohr, J.D.> ;Biochemistry. 2005 Jul 12
• Biochemical and cell-based assays for characterization of BACE-1 inhibitors.
  Pietrak, B. L.,Crouthamel, M. C.,Tugusheva, K.,Lineberger, J. E.,Xu, M.,DiMuzio, J. M.,Steele, T.,Espeseth, A. S.,Stachel, S. J.,Coburn, C. A.,Graham, S. L.,Vacca, J. ...> ;Anal Biochem. 2005 Jul 1
• Dual protein farnesyltransferase-geranylgeranyltransferase-I inhibitors as potential cancer chemotherapeutic agents.
  deSolms, S.J., Ciccarone, T.M., MacTough, S.C., Shaw, A.W., Buser, C.A., Ellis-Hutchings, M., Fernandes, C., Hamilton, K.A., Huber, H.E., Kohl, N.E., Lobell, R.B., Rob...> ;J Med Chem. 2003 Jul 3
• 3-Aminopyrrolidinone farnesyltransferase inhibitors: design of macrocyclic compounds with improved pharmacokinetics and excellent cell potency.
  Bell, I.M., Gallicchio, S.N., Abrams, M., Beese, L.S., Beshore, D.C., Bhimnathwala, H., Bogusky, M.J., Buser, C.A., Culberson, J.C., Davide, J., Ellis-Hutchings, M., F...> ;J Med Chem. 2002 Jun 6
• 10 citations
  3,8-Diazabicyclo[3.2.1]octan-2-one Peptide Mimetics: Synthesis of a Conformationally Restricted Inhibitor of Farnesyltransferase†
  Christopher J. Dinsmore, Jeffrey M. Bergman, Michael J. Bogusky, J. Christopher Culberson, and Kelly A. Hamilton, Samuel L. Graham> ;Organic Letters. 2001 Feb 17
• 29 citations
  Design and in vivo analysis of potent non-thiol inhibitors of farnesyl protein transferase.
  Neville J. Anthony, Robert P. Gomez, Micheal D. Schaber, Scott D. Mosser, Kelly Hamilton, Timothy J. O'Neil, Kenneth S. Koblan, Samuel L. Graham, George D. Hartman, Da...> ;Journal of Medicinal Chemistry. 1999 Jul 27
• 27 citations
  2-Substituted Piperazines as Constrained Amino Acids. Application to the Synthesis of Potent, Non Carboxylic Acid Inhibitors of Farnesyltransferase
  Theresa M. Williams, Ciccarone Terrence M, Suzanne C. Mactough, Rhonda L. Bock, Michael W. Conner, Joseph P. Davide, Kelly Hamilton, Kenneth S. Koblan, Nancy E. Kohl, ...> ;Journal of Medicinal Chemistry. 1996 Mar 29
• 19 citations
  Pseudodipeptide Inhibitors of Protein Farnesyltransferase
  S J deSolms, Deana Aa, E A Giuliani, Samuel L. Graham, Nancy E. Kohl, Scott D. Mosser, Oliff Allen I, David L. Pompliano, Rands E, Scholz Th> ;Journal of Medicinal Chemistry. 1995 Sep 29
• 76 citations
  Pseudopeptide inhibitors of Ras farnesyl-protein transferase.
  Samuel L. Graham, S J deSolms, E A Giuliani, Nancy E. Kohl, Scott D. Mosser, Oliff Allen I, David L. Pompliano, Rands E, Michael J. Breslin, Deana Aa> ;Journal of Medicinal Chemistry. 1994 Mar 18
• A study of the dose dependency of a glycine receptor antagonist in focal ischemia.
  Chen J, Graham S, Moroni F, Simon R> ;J. Pharmacol. Exp. Ther.. 1993-11-01
• 10 citations
  Sulfonylmethanesulfonamide inhibitors of carbonic anhydrase
  Scholz Th, John M. Sondey, W. C. Randall, Harvey Schwam, Wayne J. Thompson, Pierre Mallorga, Michael F. Sugrue, Samuel Graham> ;Journal of Medicinal Chemistry. 1993 Jul 23
• 26 citations
  HIV-1 protease inhibitors based on hydroxyethylene dipeptide isosteres: an investigation into the role of the P1' side chain on structure-activity.
  Steven D. Young, Payne Linda S, Wayne J. Thompson, N. Gaffin, Terry A. Lyle, S. F. Britcher, Samuel L. Graham, T H Schultz, A A Deana, Paul L. Darke> ;Journal of Medicinal Chemistry. 1992 May 15
• 14 citations
  Topically active carbonic anhydrase inhibitors. 4. [(Hydroxyalkyl)sulfonyl]benzene and [(hydroxyalkyl)sulfonyl]thiophenesulfonamides.
  Kenneth L. Shepard, Samuel L. Graham, Hudcosky Rj, Michelson, Scholz Th, Harvey Schwam, Anthony M. Smith, John M. Sondey, K. M. Strohmaier, Robert L. Smith> ;Journal of Medicinal Chemistry. 1991 Oct 1
• 21 citations
  Design and synthesis of HIV protease inhibitors. Variations of the carboxy terminus of the HIV protease inhibitor L-682,679.
  S J deSolms, E A Giuliani, J. P. Guare, J. P. Vacca, William M. Sanders, Samuel L. Graham, J. M. Wiggins, Paul L. Darke, I S Sigal, Zugay Ja> ;Journal of Medicinal Chemistry. 1991 Sep 1
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