Zobrazeno 1 - 10
of 15
pro vyhledávání: '"Thomas M. Graczyk"'
Publikováno v:
2017 Medicinal Chemistry Reviews ISBN: 9780996293242
2017 Medicinal Chemistry Reviews
2017 Medicinal Chemistry Reviews
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::50d9942c2287a02aefe8e4706e4af30d
https://doi.org/10.29200/acsmedchemrev-v52.ch20
https://doi.org/10.29200/acsmedchemrev-v52.ch20
Autor:
Guo-Hua Chu, William M. Barker, Rolf T. Windh, Patrick J. Little, Michael J. Derelanko, Bertrand Le Bourdonnec, Michael Koblish, Diane L. DeHaven-Hudkins, Minghua Gu, Thomas M. Graczyk, Daniel D. Wiant, Lara K. Leister, Bernice L. Brogdon, Robert N. DeHaven, Christopher W. Ajello, Steven A. Smith, Serge Belanger, David D. Christ, Paul A. Tuthill, Steve Kutz, Joel A. Cassel, Marina S. Feschenko, Roland E. Dolle
Publikováno v:
Journal of Medicinal Chemistry. 51:5893-5896
Selective delta opioid receptor agonists are promising potential therapeutic agents for the treatment of various types of pain conditions. A spirocyclic derivative was identified as a promising hit through screening. Subsequent lead optimization iden
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::619e8cbfdd85472b2463e048206eebc5
https://doi.org/10.1021/jm8008986
https://doi.org/10.1021/jm8008986
Autor:
Michael Koblish, Minghua Gu, Thomas M. Graczyk, Patrick J. Little, Nathalie Conway-James, Robert N. DeHaven, Serge Belanger, Diane L. DeHaven-Hudkins, Guo-Hua Chu, Joel A. Cassel, Roland E. Dolle
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:1951-1955
A novel series of malonamide derivatives was synthesized. These amides were shown to be potent and selective kappa opioid receptor agonists.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::32ad212de03125134561624676bd1165
https://doi.org/10.1016/j.bmcl.2007.01.053
https://doi.org/10.1016/j.bmcl.2007.01.053
Autor:
Mathieu Machaut, Joel A. Cassel, Gabriel J. Stabley, Robert N. DeHaven, Roland E. Dolle, Thomas M. Graczyk, Blanca Martinez-Teipel, Serge Belanger
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:3545-3548
( S )-4-(Carboxamido)phenylalanine (Cpa) is examined as a bioisosteric replacement for the terminal tyrosine (Tyr) residue in a variety of known peptide ligands for the μ , δ , and κ opioid receptors. The Cpa-containing peptides, assayed against c
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::63288140e896f649e1bebb0082a4e2f1
https://doi.org/10.1016/j.bmcl.2004.04.039
https://doi.org/10.1016/j.bmcl.2004.04.039
Publikováno v:
Journal of Virology. 76:9588-9599
Endoplasmic reticulum (ER) stress signaling is an adaptive cellular response to the loss of ER Ca 2+ homeostasis and/or the accumulation of misfolded, unassembled, or aggregated proteins in the ER lumen. ER stress-activated signaling pathways regulat
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::58933f66d11d9dbb7cb2b595b0ebc04d
https://doi.org/10.1128/jvi.76.19.9588-9599.2002
https://doi.org/10.1128/jvi.76.19.9588-9599.2002
Publikováno v:
Pain Management Nursing. 18:72
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::45556f5202e7ed3824fa4d2a701760e4
https://doi.org/10.1016/j.pmn.2017.02.193
https://doi.org/10.1016/j.pmn.2017.02.193
Autor:
Dimitar Gotchev, Dennis Yamashita, Thomas M. Graczyk, Yuan Catherine C K, Guodong Liu, Xiao-Tao Chen, Michael W. Lark, Michael Koblish, Conrad L. Cowan, Jonathan D. Violin, Scott M. DeWire, Philip Pitis, David H. Rominger
Publikováno v:
The Journal of pharmacology and experimental therapeutics. 344(3)
The concept of ligand bias at G protein-coupled receptors broadens the possibilities for agonist activities and provides the opportunity to develop safer, more selective therapeutics. Morphine pharmacology in β-arrestin-2 knockout mice suggested tha
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::59de0fb3f34235770d64772f7d1a26c8
https://pubmed.ncbi.nlm.nih.gov/23300227
https://pubmed.ncbi.nlm.nih.gov/23300227
Autor:
Thomas M. Graczyk, Patrick J. Little, Diane L. DeHaven-Hudkins, William M. Barker, Michael Koblish, Rolf T. Windh, Minghua Gu, Marina S. Feschenko, Joel A. Cassel, Guo-Hua Chu, Daniel D. Wiant, Steve Kutz, Lara Kathryn Leister, Robert N. DeHaven, Serge Belanger, Bertrand Le Bourdonnec, Roland E. Dolle, Bernice L. Brogdon, Steven A. Smith, Tuthill Paul Anson, Michael J. Derelanko, Q. Jean Zhou, Christopher W. Ajello
Publikováno v:
Journal of medicinal chemistry. 52(18)
Selective, nonpeptidic delta opioid receptor agonists have been the subject of great interest as potential novel analgesic agents. The discoveries of BW373U86 (1) and SNC80 (2) contributed to the rapid expansion of research in this field. However, po
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bfc53d00daff04ac1abedc34cfddc85c
https://pubmed.ncbi.nlm.nih.gov/19694468
https://pubmed.ncbi.nlm.nih.gov/19694468
Autor:
Allan J. Goodman, Serge Belanger, Robert N. DeHaven, Pamela R. Seida, Thomas M. Graczyk, Bertrand Le Bourdonnec, Roland E. Dolle
Publikováno v:
Journal of medicinal chemistry. 49(25)
To better understand structural requirements for a mu ligand of the trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine class to interact with the mu opioid receptor, we have described in the previous article (Le Bourdonnec, B. et al. J. Med. Chem. 2006
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e679225be6390e4cec8a40dc299743c5
https://pubmed.ncbi.nlm.nih.gov/17149859
https://pubmed.ncbi.nlm.nih.gov/17149859
Autor:
Thomas M. Graczyk, Mathieu Michaut, Robert N. DeHaven, Serge Belanger, Blanca Martinez-Teipel, Roland E. Dolle
Publikováno v:
Bioorganicmedicinal chemistry letters. 17(9)
A series of opioid peptide ligands containing modified N-terminal tyrosine (Tyr) residues was prepared and evaluated against cloned human mu, delta, and kappa opioid receptors. This work extends the recent discovery that (S)-4-carboxamidophenylalanin
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bfba88d5cdea83c4d6b89a9f12558ffd
https://pubmed.ncbi.nlm.nih.gov/17350835
https://pubmed.ncbi.nlm.nih.gov/17350835