CAS: 199110-64-0; Fmoc-Bip(4,4')-Oh

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205526-38-1 147923-08-8 155760-02-4

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Fm°C-4-bromo-L-phenylalanine phenylboronic acid N-(9H-fluoren-2-ylmethoxycarbonyloxy)succinimide H-p-BrPhe-OH(S)-N-((S)-1-amino-3-(biphenyl-4-yl)-1-oxopropan-2-yl)-5-guanidino-2-((2Z,5Z)-5-(4-hydroxy-3,5-dimethoxybenzylidene)-4-oxo-2-(phenylimino)thiazolidin-3-yl)pentanamide (S)-2-((S)-3-(biphenyl-4-yl)-2-((2Z,5Z)-5-(4-hydroxy-3,5-dimethoxybenzylidene)-4-oxo-2-(phenylimino)thiazolidin-3-yl)propanamido)-5-guanidinopentanamide 2O-W-F-I-Bip-H(1-Bzl)-NH2 2O-W-Bip-I-F-H(1-Bzl)-NH2

L-4-溴苯丙氨酸置于(1,1'-Bis(Diphenylphosphino)Ferrocene)Palladium(II) Dichloride,Sodium Carbonate,Potassium Carbonate体系中,用 水,异丙醇,丙酮 用作溶剂,化学反应 7.0H,反应生成3-(4-联苯基)-N-Fmoc-L-丙氨酸
参考文献:受自然启发的药物设计:自动剪裁的蛋白酶抑制剂模板的晶体学检测.
标题:受自然启发的药物设计:自动剪裁的蛋白酶抑制剂模板的晶体学检测.
摘要:从头开始发现药物仍然是寻找治疗相关靶蛋白的有效和选择性调节剂的挑战.在这里,我们揭示了x射线晶体学法意外发现的肽配体1,它是由治疗靶点mmp-13通过部分自降解和随后基于结构的优化自动构建为高效的选择性β-片层的拟肽抑制剂,衍生自金属蛋白酶的内源性组织抑制剂.事实证明,结合非蛋白原性氨基酸和环化策略是timp拟肽模拟设计的关键.优化的环肽4(zhawoc7726)具有21 N M Ic 50的膜渗透性mmp-13的选择性和相对于多药理学方法的诱人的选择性,包括抗癌靶标mmp-2(ic 50:170 N M)和mmp-9(ic 50:140 N M).
Doi:10.1002/anie.201812348

专利信息

专利号:US-8598089-B2
优先权日:2003-12-17
标题 :Methods for synthesis of encoded libraries
发明人：MORGAN BARRY; HALE STEPHEN; ARICO-MUENDEL CHRISTOPHER C; CLARK MATTHEW; WAGNER RICHARD; ISRAEL DAVID I; GEFTER MALCOLM L; BENJAMIN DENNIS; HANSEN NILS JAKOB VEST; KAVARANA MALCOLM J; CREASER STEFFAN PHILLIP; FRANKLIN GEORGE J; CENTRELLA PAOLO A; ACHARYA RAKSHA A
权利人:MORGAN BARRY; HALE STEPHEN; ARICO-MUENDEL CHRISTOPHER C; CLARK MATTHEW; WAGNER RICHARD; ISRAEL DAVID I; GEFTER MALCOLM L; BENJAMIN DENNIS; HANSEN NILS JAKOB VEST; KAVARANA MALCOLM J; CREASER STEFFAN PHILLIP; FRANKLIN GEORGE J; CENTRELLA PAOLO A; ACHARYA RAKSHA A; GLAXOSMITHKLINE LLC
摘要:The present invention provides a method of synthesizing libraries of molecules which include an encoding oligonucleotide tag.

专利号:US-8410028-B2
优先权日:2003-12-17
标 题:Methods for synthesis of encoded libraries
发明人：MORGAN BARRY; HALE STEPHEN; ARICO-MUENDEL CHRISTOPHER C; CLARK MATTHEW; WAGNER RICHARD; ISRAEL DAVID I; GEFTER MALCOLM L; BENJAMIN DENNIS; HANSEN NILS JAKOB VEST; KAVARANA MALCOLM J; CREASER STEFFAN PHILLIP; FRANKLIN GEORGE J; CENTRELLA PAOLO A; ACHARYA RAKSHA A
权利人:MORGAN BARRY; HALE STEPHEN; ARICO-MUENDEL CHRISTOPHER C; CLARK MATTHEW; WAGNER RICHARD; ISRAEL DAVID I; GEFTER MALCOLM L; BENJAMIN DENNIS; HANSEN NILS JAKOB VEST; KAVARANA MALCOLM J; CREASER STEFFAN PHILLIP; FRANKLIN GEORGE J; CENTRELLA PAOLO A; ACHARYA RAKSHA A; GLAXOSMITHKLINE LLC
摘要:The present invention provides a method of synthesizing libraries of molecules which include an encoding oligonucleotide tag.

专利号:US-2007042401-A1
优先权日:2003-12-17
标题 :Methods for synthesis of encoded libraries

专利号:US-2012245040-A1
优先权日:2003-12-17
标题 :Methods for synthesis of encoded libraries

专利号:US-2009062147-A1
优先权日:2003-12-17
标 题:Methods for synthesis of encoded libraries

专利号:US-7972994-B2
优先权日:2003-12-17
标 题 :Methods for synthesis of encoded libraries