S
Samuel L. Graham
Researcher at Merck & Co.
Publications - 120
Citations - 5199
Samuel L. Graham is an academic researcher from Merck & Co.. The author has contributed to research in topics: Farnesyltransferase & Farnesyl Protein Transferase. The author has an hindex of 40, co-authored 120 publications receiving 5099 citations. Previous affiliations of Samuel L. Graham include University of Pennsylvania & Duke University.
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Journal ArticleDOI
Selective inhibition of ras-dependent transformation by a farnesyltransferase inhibitor.
Nancy E. Kohl,Scott D. Mosser,S J deSolms,E A Giuliani,David L. Pompliano,Samuel L. Graham,Robert L. Smith,Edward M. Scolnick,Oliff Allen I,Jackson B. Gibbs +9 more
TL;DR: Selective inhibition of ras-dependent cell transformation with a synthetic organic inhibitor of FPTase is demonstrated.
Journal ArticleDOI
Inhibition of farnesyltransferase induces regression of mammary and salivary carcinomas in ras transgenic mice
Nancy E. Kohl,Charles A. Omer,Michael W. Conner,Neville J. Anthony,Joseph P. Davide,S J deSolms,E A Giuliani,Robert P. Gomez,Samuel L. Graham,Kelly Hamilton +9 more
TL;DR: This first demonstration of anti-FPTase-mediated tumour regression suggests that FPTase inhibitors may be safe and effective anti-tumour agents in some cancers.
Journal Article
Evaluation of farnesyl:protein transferase and geranylgeranyl:protein transferase inhibitor combinations in preclinical models.
Robert B. Lobell,Charles A. Omer,Marc Abrams,Hema Bhimnathwala,Mary Jo Brucker,Carolyn A. Buser,Joseph P. Davide,S. Jane Desolms,Christopher J. Dinsmore,Michelle Ellis-Hutchings,Astrid M. Kral,Dongming Liu,William C. Lumma,Samuel V. Machotka,Elaine Rands,Theresa M. Williams,Samuel L. Graham,George D. Hartman,Oliff Allen I,David C. Heimbrook,Nancy E. Kohl +20 more
TL;DR: In human PSN-1 pancreatic tumor cells, and in other tumor lines having either wild-type or oncogenic Ki-ras, treatment with an FTI/GGTI combination or with a DPI blocks Ki-Ras prenylation and induces markedly higher levels of apoptosis relative to FTI or GGTI alone.
Journal ArticleDOI
Farnesyltransferase inhibition causes morphological reversion of ras-transformed cells by a complex mechanism that involves regulation of the actin cytoskeleton.
George C. Prendergast,Joseph P. Davide,S J deSolms,E A Giuliani,Samuel L. Graham,Jackson B. Gibbs,Oliff Allen I,Nancy E. Kohl +7 more
TL;DR: The results suggest that the mechanism of morphological reversion is complex and may involve farnesylated proteins that control the organization of cytoskeletal actin.
Journal ArticleDOI
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-1-yl)piperidine-1-carboxamide], a potent and orally active calcitonin gene-related peptide receptor antagonist for the treatment of migraine.
Christopher A. Salvatore,James C. Hershey,Halea A. Corcoran,John F. Fay,Victor K. Johnston,Eric L. Moore,Scott D. Mosser,Christopher S. Burgey,Daniel V. Paone,Anthony W. Shaw,Samuel L. Graham,Joseph P. Vacca,Theresa M. Williams,Kenneth S. Koblan,Stefanie A. Kane +14 more
TL;DR: MK-0974 produced a concentration-dependent inhibition of dermal vasodilation, generated by capsaicin-induced release of endogenous CGRP, with plasma concentrations of 127 and 900 nM required to block 50 and 90% of the blood flow increase, respectively.