Zobrazeno 1 - 10
of 16
pro vyhledávání: '"Dennis Heyer"'
Autor:
Dennis Heyer, Jean Baptiste E Blanc, Jean Shearin, Lisa A. Miller, Sue H. Kadwell, Timothy M. Willson, William J. Hoekstra, Xi Liang, Hari S. Patel, Marie A. Iannone, Kenneth H. Pearce, Catherine A. Simmons
Publikováno v:
Journal of Medicinal Chemistry. 48:2243-2247
Traditional approaches to discovery of selective estrogen receptor modulators (SERMs) have relied on ER binding and cell-based estrogen response element-driven assays to identify compounds that are osteoprotective but nonproliferative in breast and u
Publikováno v:
Tetrahedron Letters. 40:2227-2230
The solid phase synthesis of 1,3,5-trisubsituted pyridin-2-ones is reported via selective 1 NH- alkylation of 3-amino-5-carbomethoxy-1 H -pyridin-2-one with a solid-supported halo-acid. Coupling of an acid to solid-supported 3-aminopyridinone was fol
Autor:
Dennis Heyer, Lisa A. Orband-Miller, Frank Navas, David W. Gray, Shawn P. Williams, Adwoa Akwabi-Ameyaw, Jean Shearin, Jing Fang, Subba Reddy Katamreddy, Aaron B. Miller, Jonathan E. Britton
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:5075-5077
A series of estrogen receptor ligands based on a 3-alkyl naphthalene scaffold was synthesized using an intramolecular enolate-alkyne cycloaromatization as the key step. Several of these compounds bearing a C6-OH group were shown to be high affinity l
Autor:
Paul R. Johnson, Dallas K. Croom, Sarah R. Bullard, Sean Ross, Ronald L. Brashear, James M. Way, Christopher R. Conlee, Shane M. Hart, Carina Ammala, Vicente Samano, James B. Thompson, Doug Minick, Yun Xu, Dennis Heyer, Shane Roller, Eric E. Boros, Sarva M. Tadepalli, Peckham Gregory, Andrew J. Carpenter, Jennifer A. Kashatus, Subba Reddy Katamreddy, Howard Ray Sauls, Richard Dana Caldwell, Celia P. Briscoe
Publikováno v:
Journal of medicinal chemistry. 55(24)
GPR119 is a 7-transmembrane receptor that is expressed in the enteroendocrine cells in the intestine and in the islets of Langerhans in the pancreas. Indolines and 6,7-dihydro-5H-pyrrolo[2,3-a]pyrimidines were discovered as G protein-coupled receptor
Autor:
Brad R, Henke, Dennis, Heyer
Publikováno v:
Current opinion in drug discoverydevelopment. 8(4)
Modulation of estrogen action is an effective treatment for alleviating the symptoms associated with menopause, and also provides an alternative to ablative surgery for the treatment of breast cancer. The side effects associated with the currently us
Autor:
Eric C. Bigham, David H. Drewry, Frank Navas, Michael J. Bishop, Stephen J. Hodson, Brian Edward Marron, Suganthini S. Nanthakumar, Judd Berman, Deanna T. Garrison, Lee Allen Barger, Mark H. Norman, Jennifer A. Kakel, Dennis Heyer, James A. Linn, Samuel W. Gerritz
Publikováno v:
Journal of combinatorial chemistry. 5(2)
The high-throughput manual solid-phase parallel synthesis of libraries comprising thousands of discrete samples using pellicular supports (i.e. SynPhase crowns and lanterns) and a suite of novel tools and techniques is described. Key aspects of this
Publikováno v:
Regulatory peptides. 106(1-3)
Numerous reports have implicated theY5 receptor as the 'feeding' receptor mediating the orexigenic action of neuropeptide Y (NPY). This notion is supported by the correlation between the in vitro functional and binding activities of different peptide
Publikováno v:
Neuropeptide Y and Drug Development
Publisher Summary This chapter discusses design, structure, and pharmacological characterization of peptide antagonists of neuropeptide. The structure-affinity pattern found for the pentapeptide series agrees well with reported structural requirement
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::a45cf4b6a17dbc018b01fb40779d17e8
https://doi.org/10.1016/b978-012304990-2/50008-1
https://doi.org/10.1016/b978-012304990-2/50008-1
Autor:
Johann Leban, Marilyn Jansen, A Tadepalli, Antonio Landavazo, Dennis Heyer, W Harrington, Andrew Spaltenstein, O H Viveros, R J Slepetis, Alejandro J. Daniels, J E Matthews
Neuropeptide Y (NPY) is one of the most abundant peptide transmitters in the mammalian brain. In the periphery it is costored and coreleased with norepinephrine from sympathetic nerve terminals. However, the physiological functions of this peptide re
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7f36b7f0ab342b3956cbf71c59a2e50c
https://europepmc.org/articles/PMC40925/
https://europepmc.org/articles/PMC40925/
Autor:
Jessica E. Matthews, Antonio Landavazo, Alejandro J. Daniels, Johann Leban, Dennis Heyer, Ann Aulabaugh
Publikováno v:
Journal of medicinal chemistry. 38(7)
Peptide analogs of neuropeptide Y (NPY) with a Tyr-32 and Leu-34 replacement resulted in the decapeptide TyrIleAsnLeuIleTyrArgLeuArgTyr-NH 2 (9; Table 1) and a 3700-fold improvement in affinity at Y 2 (rat brain; IC 50 =8.2±3 nM) receptors when comp