R
Roger M. Freidinger
Researcher at Merck & Co.
Publications - 82
Citations - 2437
Roger M. Freidinger is an academic researcher from Merck & Co.. The author has contributed to research in topics: Gastrin & Cholecystokinin. The author has an hindex of 25, co-authored 82 publications receiving 2412 citations.
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Journal ArticleDOI
Bioactive conformation of luteinizing hormone-releasing hormone: evidence from a conformationally constrained analog.
TL;DR: An analog of luteinizing hormone-releasing hormone containing a gamma-lactam as a conformational constraint has been prepared with the use of a novel cyclization of a methionine sulfonium salt, and provides evidence for a bioactive conformation containing a beta-turn.
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HIV-1 protease specificity of peptide cleavage is sufficient for processing of gag and pol polyproteins.
Paul L. Darke,Ruth F. Nutt,Stephen F. Brady,Victor M. Garsky,Terrence M. Ciccarone,Chih-Tai Leu,Patricia K. Lumma,Roger M. Freidinger,Daniel F. Veber,Irving S. Sigal +9 more
TL;DR: A 99-amino acid HIV-1 protease, produced by chemical synthesis or by expression in bacteria, is shown here to hydrolyze peptides corresponding to all of the known cleavage sites in the HIV- 1 gag and pol polyproteins.
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Design of nonpeptidal ligands for a peptide receptor: cholecystokinin antagonists
B. E. Evans,Kenneth E. Rittle,Mark G. Bock,Robert M. DiPardo,Roger M. Freidinger,Willie L. Whitter,N. P. Gould,George F. Lundell,Carl F. Homnick +8 more
TL;DR: A series of 3-substituted 5-phenyl-1,4-benzodiazepines, nonpeptidal antagonists of the peptide hormone cholecystokinin, serve to illuminate the distinction between central and peripheral CCK receptors, as well as to provide orally effective CCK antagonists of potential pharmacological or therapeutic utility.
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The design of metabolically-stable peptide analogs
TL;DR: This work has shown that the application of conformational constraint to the design of peptide analogs which are resistant to metabolism while retaining high biological activity and the successful elimination of metabolism, transport and excretion are successful.
Journal ArticleDOI
A super active cyclic hexapeptide analog of somatostatin
Daniel F. Veber,Richard Saperstein,Ruth F. Nutt,Roger M. Freidinger,Stephen F. Brady,Paul E. Curley,Debra S. Perlow,William J. Paleveda,C. Dylion Colton,Anthony G. Zacchei,Dominick J. Tocco,Hoff Dale R,Richard L. Vandlen,John E. Gerich,L. D. Hall,Lawrence J. Mandarino,Eugene H. Cordes,Paul S. Anderson,Hirschmann Ralph F +18 more
TL;DR: The cyclic hexapeptide, cyclo (Pro-Phe-D-Trp-Lys-Thr-phe), I, has been shown to have the biological properties of somatostatin this paper.