Zobrazeno 1 - 10
of 86
pro vyhledávání: '"A M, Nadzan"'
Autor:
Mi Chen, Hediki Sato, Sovouthy Tith, Yoshiyuki Ono, Hirotaka Kashiwagi, Toshiro Kozono, Akira Ishikawa, David Wallace, Thomas Arrhenius, Alex M. Nadzan, Jie-Fei Cheng, Haruhiko Sato
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:2411-2415
The discovery and structure–activity relationship of a novel series of coumarin-based TNF-α inhibitors is described. Starting from the initial lead 1a , various derivatives were prepared surrounding the coumarin core structure to optimize the in v
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2f018e2e24825365a6413e0972fc8956
https://doi.org/10.1016/j.bmcl.2004.03.022
https://doi.org/10.1016/j.bmcl.2004.03.022
Autor:
Donald Chu, Alex M. Nadzan, Anna Russell, Demin Zhou, Jie-Fei Cheng, Phoebe Yuen, Jason R.B. Dyck, Guang Yang, Steve McConnell, Gary D. Lopaschuk, Steven Brown, Miguel Barbosa, Andria Tsang, Vicki Thon, Michael Pena
Publikováno v:
Protein Expression and Purification. 34:261-269
The recombinant human malonyl-CoA decarboxylase (hMCD) was overexpressed in Escherichia coli with and without the first 39 N-terminal amino acids via a cleavable MBP-fusion construct. Proteolytic digestion using genenase I to remove the MBP-fusion ta
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::05372c67d8be846d53e40f1f192b1f5f
https://doi.org/10.1016/j.pep.2003.11.023
https://doi.org/10.1016/j.pep.2003.11.023
Autor:
Alex M. Nadzan, Marcus F. Boehm, Cesario Rm, Dardashti Laura J, Canan Koch Ss, Richard A. Heyman, Glenn Croston
Publikováno v:
Journal of Medicinal Chemistry. 42:742-750
A novel series of oxime ligands has been synthesized that displays potent, specific activation of the retinoid X receptors (RXRs). The oximes of 3-substituted (tetramethyltetrahydronaphthyl)carbonylbenzoic acids are readily available by condensation
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f77609d841b265ce2ef5e6cf1c70a802
https://doi.org/10.1021/jm980621r
https://doi.org/10.1021/jm980621r
Autor:
Karen S. Flatten, Lin Zhi, Rich A. Heyman, Susan Jeong, E. Adam Kallel, Glenn Croston, Luc J. Farmer, Alex M. Nadzan
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 7:2747-2752
A series of potent retinoid X receptor (RXR) selective ligands were designed and prepared. The lead compound 6a, showed good binding (Kd; 3–7 nM) and transactivation (EC50; 19–24 nM) to the RXR subfamily of retinoid receptors. More importantly, a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::ae9f5e21f3e243b50d0c726d327d716a
https://doi.org/10.1016/s0960-894x(97)10079-8
https://doi.org/10.1016/s0960-894x(97)10079-8
Autor:
Glenn Croston, Susan Jeong, Luc J. Farmer, Rich A. Heyman, Karen S. Flatten, E. Adam Kallel, Alex M. Nadzan, Stacie S. Canan Koch
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 7:2393-2398
A series of potent retinoid X receptor (RXR) selective ligands was designed and prepared. The lead compound 7a showed good binding (K i ; 20–50 nM) and transactivation (EC 50 ; 40–50 nM) to the RXR subfamily of retinoid receptors. More importantl
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::075808c7d07ab7aa1987ca53d8063e54
https://doi.org/10.1016/s0960-894x(97)00437-x
https://doi.org/10.1016/s0960-894x(97)00437-x
Autor:
Beth-Ann Badea, Chan Kou Hwang, Youssef L. Bennani, Laura J. Dar-ti, Stacie S. Canan Koch, Kristin S. Marron, Alex M. Nadzan
Publikováno v:
Tetrahedron Letters. 37:8109-8112
The treatment of bicyclic and tricyclic ketones with lithium ethynyl acetylide, followed by the addition of a catalytic amount of CSA or p-TSA, affords the corresponding exocyclic olefinic ester in good yields, and geometric ratios up to 13:1 favorin
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::f9731ceee4df41d56b9a8bc9817d23ac
https://doi.org/10.1016/0040-4039(96)01885-0
https://doi.org/10.1016/0040-4039(96)01885-0
Autor:
Ira G. Schulman, Ronald M. Evans, Glenn E. Croston, Stacie S. Canan Koch, Dardashti Laura J, Deepak S. Lala, Richard A. Heyman, Ranjan Mukherjee, A. M. Nadzan
Publikováno v:
Nature. 383:450-453
Retinoid X receptor (RXR) plays a central role in the regulation of many intracellular receptor signalling pathways and can mediate ligand-dependent transcription, acting as a homodimer or as a heterodimer. Here we identify an antagonist towards RXR
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fede7d15f73fe801ff99730ed4cd0c30
https://doi.org/10.1038/383450a0
https://doi.org/10.1038/383450a0
Autor:
William W. Lamph, Alex M. Nadzan, Richard A. Heyman, Deborah L. Love, Dale E. Mais, Lin Zhang, Glenn Croston, Marcus F. Boehm
Publikováno v:
Journal of Medicinal Chemistry. 39:2659-2663
Retinoic acid receptor (RAR) active retinoids have proven therapeutically useful for treating certain cancers and dermatological diseases. Herein, we describe the discovery of two new RAR active trienoic acid retinoids, (2E,4E,6E)-7-(3,5-di-tert-buty
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::782410ef29c0a91991c378e30d3faf53
https://doi.org/10.1021/jm960285j
https://doi.org/10.1021/jm960285j
Autor:
Chun Wel Lin, Thomas R. Miller, Alex M. Nadzan, Mark W. Holladay, James F. Kerwin, Alyssa B. O'Neill, Michael J. Bennett, Hao Bai, Michael Stashko, Jorge D. Brioni, Jeffrey W. Ralston
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 5:3057-3062
The development of a novel series of carbamoylamino acid benzoylpiperidides as CCK B ligands is described. Selected members of the series antagonized CCK 8 -induced calcium mobilization and showed efficacy in the mouse elevated-plus maze, a measure o
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::3a9417dff910f69b0bb3355c5436362d
https://doi.org/10.1016/0960-894x(95)00537-3
https://doi.org/10.1016/0960-894x(95)00537-3
Autor:
Marcus F. Boehm, Lin Zhang, Lin Zhi, Michael R. McClurg, Elain Berger, Murriel Wagoner, Dale E. Mais, Carla M. Suto, Peter J. A. Davies, Richard A. Heyman, Alex M. Nadzan
Publikováno v:
Journal of Medicinal Chemistry. 38:3146-3155
Structural modifications of the retinoid X receptor (RXR) selective compound 4-[1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-2- naphthyl)ethenyl]benzoic acid (LGD1069), which is currently in phase I/IIA clinical trials for cancer and dermatological in
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::eba60da857f429df0a05318959747210
https://doi.org/10.1021/jm00016a018
https://doi.org/10.1021/jm00016a018