CAS: 1097192-04-5; (S)-2-((((9H-Fluoren-9-yl)Methoxy)Carbonyl)Amino)-5-Azidopentanoic Acid

相似化合物

159610-89-6 1198791-53-5 942518-20-9

上下游产品

N-(9H-fluoren-2-ylmethoxycarbonyloxy)succinimide 2-amino-5-azidopentanoic acid (S)-5-Amino-2-(9H-fluoren-9-ylmethoxycarbonylamino)-pentanoic acid (fluorenylmethoxy)carbonyl chlorideNα-Ac-Lys-Gly-Nva(δ-N3)-Ser-Ile-Gln-Nle(δ-yl)-Leu-Arg-NH2 Nα-Ac-Lys-Gly-Nle(δ-yl)-Ser-Ile-Gln-Nva(δ-N3)-Leu-Arg-NH2 Nα-Ac-Lys-Gly-Pra-Ser-Ile-Gln-Nva(δ-N3)-Leu-Arg-NH2 Nα-Ac-Lys-Gly-Nva(δ-N3)-Ser-Ile-Gln-Pra-Leu-Arg-NH2

Tert-Butyl (S)-2-((Tert-Butoxycarbonyl)Amino)-5-Hydroxypentanoate置于盐酸,Sodium Azide,三乙胺体系中,用 乙酸乙酯,N,N-二甲基甲酰胺 用作溶剂,化学反应 17.0H,反应生成(S)-5-叠氮-2-(芴甲氧羰基-氨基)戊酸
参考文献:Identification Of A New P53/mdm2 Inhibitor Motif Inspired By Studies Of Chlorofusin
标题:Identification Of A New P53/mdm2 Inhibitor Motif Inspired By Studies Of Chlorofusin
摘要:Previous Studies On The Natural Product Chlorofusin Have Shown That The Full Peptide And Azaphilone Structure Are Required For Inhibition Of The Interaction Between Mdm2 And P53. In The Current Work,We Utilized The Cyclic Peptide As A Template And Introduced An Azidonorvaline Amino Acid In Place Of The Ornithine/azaphilone Of The Natural Product And Carried Out Click Chemistry With The Resulting Peptide. From This Small Library The First Ever Non-Azaphilone Containing Chlorofusin Analog With Mdm2/p53 Activity Was Identified. Further Studies Then Suggested That The Simple Structure Of The Fmoc-Norvaline Amino Acid That Had Undergone A Click Reaction Was Also Able To Inhibit Mdm2/p53 Interaction. This Is An Example Where Studies Of A Natural Product Have Led To The Serendipitous Identification Of A New Small Molecule Inhibitor Of A Protein-Protein Interaction. (C) 2015 Elsevier Ltd. All Rights Reserved.
Doi:10.1016/j.Bmcl.2015.06.014

专利信息

专利号:US-2013267680-A1
优先权日:2010-09-15
标题:Total chemical synthesis of ubiquitin, ubiquitin mutants and derivatives thereof
发明人：OVAA HUIB; EL OUALID FARID; MERKX REMCO NICOLAAS SEBASTIAAN MICHEL
权利人:OVAA HUIB; EL OUALID FARID; MERKX REMCO NICOLAAS SEBASTIAAN MICHEL; STICHTING HET NL KANKERINST
摘要:The present invention relates to the field of total chemical synthesis of ubiquitin and related peptides. More in particular, a method is provided of solid phase synthesis of ubiquitin, ubiquitin mutants and derivatives thereof. It was the object of the present invention to provide an approach for the total chemical synthesis of ubuiqitin, which allows for the chemical synthesis of virtually any Ub mutant and giving high overall efficiency and purity. The present inventors have surprisingly found that this object can be realized with a method relying on incorporation of special amino acid building blocks. This approach was found to allow for exceptionally high yields of up to 14% and to provide an synthetic entry into virtually any ubiquitin derivative.

专利号:WO-2012036551-A1
优先权日:2010-09-15
标题:Total chemical synthesis of ubiquitin, ubiquitin mutants and derivatives thereof