Zobrazeno 1 - 10
of 165
pro vyhledávání: '"Peg Davis"'
Autor:
Frank Porreca, Aswini Kumar Giri, Brittany L. Forte, Yue Wang, Victor J. Hruby, David Rankin, Peg Davis, Todd W. Vanderah, Christopher R. Apostol, Gabriella Molnar, Keith M. Olson, Tally M. Largent-Milnes
Publikováno v:
Journal of Medicinal Chemistry. 58:8573-8583
Multifunctional ligands with agonist bioactivities at μ/δ opioid receptors (MOR/DOR) and antagonist bioactivity at the neurokinin-1 receptor (NK1R) have been designed and synthesized. These peptide-based ligands are anticipated to produce better bi
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:4148-4152
We report here the design and synthesis of novel multifunctional ligands that act as (μ/δ) opioid agonists and bradykinin 2 receptor antagonists. These multifunctional ligands were designed to interact with the multiple receptors to show an enhance
Autor:
Josephine Lai, Yue Wang, Lauren Wugalter, Neemah M. Bassirirad, Victor J. Hruby, David Rankin, Todd W. Vanderah, Peg Davis, Frank Porreca, Srinivas Deekonda, Vinod Kulkarni, Tally M. Largent-Milnes
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:4683-4688
We describe the design and synthesis of novel bivalent ligands based on the conjugation of 4-anilidopiperidine derivatives with enkephalin analogues. The design of non-peptide analogues is explored with 5-amino substituted tetrahydronaphthalen-2yl)me
Autor:
Peg Davis, Vinod Kulkarni, Scott Cowell, Shou Wu Ma, Frank Porreca, Victor J. Hruby, Edita Navratilova, Takashi Yamamoto, Todd W. Vanderah, Sharif Moye, Josephine Lai, Padma Nair
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:3716-3720
Several bifunctional peptides were synthesized and characterized based on the pentapeptide-derived ligand NP30 (1: Tyr-DAla-Gly-Phe-Gly-Trp-O-[3′,5′-Bzl(CF3)2]). Modification and truncation of amino acid residues were performed, and the tripeptid
Autor:
Antonio Limatola, Frank Porreca, Azzurra Stefanucci, Alfonso Carotenuto, Reza Samavati, Ferenc Zádor, Sándor Benyhe, Ettore Novellino, Adriano Mollica, Roberto Costante, Victor J. Hruby, Peg Davis, Francesco Pinnen, Stefano Pieretti, Anna Borsodi
Publikováno v:
ACS Medicinal Chemistry Letters. 5:1032-1036
Two novel opioid analogues have been designed by substituting the native d-Ala residues in position 2,2' of biphalin with two residues of d-penicillamine or l-penicillamine and by forming a disulfide bond between the thiol groups. The so-obtained com
Autor:
Cyf N, Ramos-Colon, Yeon Sun, Lee, Michael, Remesic, Sara M, Hall, Justin, LaVigne, Peg, Davis, Alexander J, Sandweiss, Mary I, McIntosh, Jessica, Hanson, Tally M, Largent-Milnes, Todd W, Vanderah, John, Streicher, Frank, Porreca, Victor J, Hruby
Publikováno v:
Journal of medicinal chemistry. 59(22)
Dynorphin A (Dyn A) is an endogenous ligand for the opioid receptors with preference for the κ opioid receptor (KOR), and its structure–activity relationship (SAR) has been extensively studied at the KOR to develop selective potent agonists and an
Autor:
Jennifer Y. Xie, Peg Davis, Ping Liu, Alec Okun, Michael H. Ossipov, Frank Porreca, Triza Brion, Bethany Remeniuk, Jiyang Ren, Tamara King, Gregory Dussor
Publikováno v:
Pain. 153:924-933
Osteoarthritis (OA) is a chronic condition characterized by pain during joint movement. Additionally, patients with advanced disease experience pain at rest (ie, ongoing pain) that is generally resistant to nonsteroidal antiinflammatory drugs. Inject
Autor:
Frank Porreca, Anatoly P. Sobolev, Azzurra Stefanucci, Cristina Campestre, Peg Davis, Victor J. Hruby, F. Pinnen, Adriano Mollica, Luisa Mannina, Federica Feliciani, Shou Wu Ma, Gino Lucente, Josephine Lai
Publikováno v:
Journal of medicinal chemistry (Online) 55 (2012): 3027–3035. doi:10.1021/jm201402v
info:cnr-pdr/source/autori:A. Mollica, F. Pinnen, A. Stefanucci, F. Feliciani, C. Campestre, L. Mannina, A. P. Sobolev, G. Lucente, P. Davis, J. Lai, S.-W. Ma, F. Porreca, V. J. Hruby/titolo:The cis-4-amino-L-proline residue as a scaffold for the synthesis of cyclic and linear endomorphin-2 analogues/doi:10.1021%2Fjm201402v/rivista:Journal of medicinal chemistry (Online)/anno:2012/pagina_da:3027/pagina_a:3035/intervallo_pagine:3027–3035/volume:55
info:cnr-pdr/source/autori:A. Mollica, F. Pinnen, A. Stefanucci, F. Feliciani, C. Campestre, L. Mannina, A. P. Sobolev, G. Lucente, P. Davis, J. Lai, S.-W. Ma, F. Porreca, V. J. Hruby/titolo:The cis-4-amino-L-proline residue as a scaffold for the synthesis of cyclic and linear endomorphin-2 analogues/doi:10.1021%2Fjm201402v/rivista:Journal of medicinal chemistry (Online)/anno:2012/pagina_da:3027/pagina_a:3035/intervallo_pagine:3027–3035/volume:55
Endomorphin-2 (EM-2: Tyr-Pro-Phe-Phe-NH(2)) is an endogenous tetrapeptide that combines potency and efficacy with high affinity and selectivity toward the μ opioid receptor, the most responsible for analgesic effects in the central nervous system. T
Autor:
Katherine E. Hanlon, Frank Porreca, Victor J. Hruby, Vinod Kulkarani, Ruben Vardanyan, Shou Wu Ma, Scott Cowell, Peg Davis, Todd W. Vanderah, Yeon Sun Lee, Josephine Lai
Publikováno v:
Journal of Medicinal Chemistry. 54:382-386
An SAR study on the Dmt-substituted enkephalin-like tetrapeptide with a N-phenyl-N-piperidin-4-ylpropionamide moiety at the C-terminal was performed and has resulted in highly potent ligands at μ and δ opioid receptors. In general, ligands with the
Autor:
F. Pinnen, Federica Feliciani, Victor J. Hruby, Frank Porreca, Peg Davis, Josephine Lai, Gino Lucente, Gustavo Portalone, Adriano Mollica, Giancarlo Fabrizi, Domenica Torino, Shou Wu Ma
Publikováno v:
Journal of Medicinal Chemistry. 53:4550-4554
New endomorphin-2 (EM-2) analogues incorporating (Z)-alpha,beta-didehydrophenylalanine (Delta(Z)Phe) in place of the native phenylalanine in EM-2 are reported. Tyr-Pro-Delta(Z)Phe-Phe-NH(2) {[Delta(Z)Phe(3)]EM-2} (1), Tyr-Pro-Phe-Delta(Z)Phe-NH(2) {[