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Fmoc-L-Tyr(CH2-Chx)-OH
Chemischer Name: N-alpha-(9-Fluorenylmethyloxycarbonyl)-O-cyclohexylmethyl-L-tyrosine // Synonyme: Fmoc-Tyr(CH2-Chx)-OH, Fmoc-Phe(4-OCH2-Chx)-OH, N-alpha-(9-Fluorenylmethyloxycarbonyl)-4-cyclohexylmethoxy-L-phenylalanine
- Art-Nr.:FAA3645
- CAS Nr.:960360-37-6
- Formel:C31H33NO5
- Molare Masse:499,61 g/mol
Startet von 900,00 €
description
This compound has been used to modify active peptides, in order to fill hydropohobic pockets and increase interactions. Peptides have been designed, which stabilize the CD4-bound conformation of gp120 leading to neutralized HIV entry in vitro and in vivo. It has been published that filling the subpocket at the JMJD2 active site, leads to inhibition of the JMJD2 subfamily of histone demethylases.
references
Interfacial Cavity Filling To Optimize CD4−Mimetic Miniprotein Interactions with HIV‑1 Surface Glycoprotein; Laurence Morellato-Castillo, Priyamvada Acharya, Olivier Combes, Johan Michiels, Anne Descours, Oscar H. P. Ramos, Yongping Yang, Guido Vanham, Kevin K. Ariën, Peter D. Kwong, Loïc Martin, and Pascal Kessler; J. Med. Chem. 2013; 56: 5033−5047. DOI: org/10.1021/jm4002988
Selective Inhibitors of the JMJD2 Histone Demethylases: Combined Nondenaturing Mass Spectrometric Screening and Crystallographic Approaches; Nathan R. Rose, Esther C. Y. Woon, Guy L. Kingham, Oliver N. F. King, Jasmin Mecinovic Ian J. Clifton, Stanley S. Ng, Jobina Talib-Hardy, Udo Oppermann, Michael A. McDonough, and Christopher J. Schofield; J. Med. Chem. 2010; 53: 1810–1818. DOI: 10.1021/jm901680b
Synthesis and biological evaluation of phosphonate derivatives as autotaxin (ATX) inhibitors; Peng Cui, Jose L. Tomsig, William F. McCalmont, Sangderk Lee, Christopher J. Becker, Kevin R. Lynch and Timothy L. Macdonald; Bioorg Med. Chem. Lett. 2007; 17: 1634–1640; DOI: 10.1016/j.bmcl.2006.12.114
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