CAS: 646066-73-1; (S)-2-Amino-3-(3,4,5-Trifluorophenyl)Propionic Acid

上下游产品

acetyl-DL-3,4,5-trifluorophenylalanine 3,4,5-trifluorobenzyl bromide 2-acetylamino-2-(3,4,5-trifluoro-benzyl)-malonic acid diethyl 2-acetamido-2-(3,4,5-trifluorobenzyl)malonate

📜3,4,5-三氟溴苄置于盐酸,Sodium Hydroxide,乙醇,Aspergillus Genus Acylase,Sodium Acetate,Sodium体系中,用 甲醇,水,Xylene 作为反应溶剂,化学反应 57.0H,反应生成 L-3,4,5-三氟苯丙氨酸
参考文献:Exploration Of The Role Of Phenylalanine In The Thrombin Receptor Tethered-Ligand Peptide By Substitution With A Series Of Trifluorophenylalanines
标题:Exploration Of The Role Of Phenylalanine In The Thrombin Receptor Tethered-Ligand Peptide By Substitution With A Series Of Trifluorophenylalanines
摘要:凝血酶受体束缚配体 Sfllrnp(由表达 Ser-Phe-Leu-Leu-Arg-Asn-Pro 的单字母氨基酸代码组成的缩写)由受体激活所必需的 Phe-2 残基组成.为了探索该 Phe-2-苯基的分子特征,将一系列三氟苯丙氨酸 [(F3)Phe] 掺入该 S/phe/llrnp 中,以评估其诱导人血小板聚集的能力. L构型的完整(F3)Phe组,即(2,3,4-F3)Phe,(2,3,5-F3)Phe,(2,3,6-F3)Phe,(2,4,5-F3)Phe,(2,4,6-F3)Phe 和 (3,4,5-F3)Phe 由三氟苄基溴和乙酰胺丙二酸二乙酯制备. S/(2,3,4-F3)Phe/llrnp 与 S/phe/llrnp 等效,而含有 (2,4,5-F3)Phe 的类似物几乎是其两倍. (2,4,6-F3)Phe 类似物表现出大约 S/phe/llrnp 一半的活性. (3,4,5-F3)Phe-,(2,3,5-F3)Phe-和(2,3,6-F3)Phe-类似物非常弱.对这些测定结果的分析表明,Sfllrnp 的 Phe-2-苯基与受体芳香基团以边对面的 Ch/π 相互作用,利用 Phe-2-苯基边缘以及 2-3 位的苯氢.或5-6. Mopac 的计算机辅助半经验分子轨道计算表明,氟原子降低了其邻氢,间氢和对氢的电子密度,从而按顺序更强烈地增加了它们的酸性.所有这些表明h-> F 替换增强了边对面的ch/π 相互作用,从而增强了生物活性.发现 Phe-苯基上的 H-> F 取代可以进行有效的结构检查;即识别ch/π相互作用中的氢,并加强ch/π相互作用.
DOI:10.1246/bcsj.73.2531

专利信息

专利号:US-2022243244-A1
优先权日:2019-10-10
标 题 :Compositions and methods for in vivo synthesis of unnatural polypeptides
发明人：ROMESBERG FLOYD E; FISCHER EMIL C; HASHIMOTO KOJI; FELDMAN AARON W; DIEN VIVIAN T; ZHANG YORKE
权利人:SCRIPPS RESEARCH INST
摘要:Disclosed herein are compositions, methods, and kits for a cell incorporating unnatural amino acids into an unnatural polypeptide. Also disclosed herein are compositions, methods, and kits for increasing activity and yield of the unnatural polypeptide synthesized by the cell.

专利号:US-2023037284-A9
优先权日:2018-11-30
标题:Combination therapy of peptidomimetic macrocycles
发明人：GUERLAVAIS VINCENT; ANNIS DAVID ALLEN
权利人:AILERON THERAPEUTICS INC
摘要:The present disclosure describes the synthesis of peptidomimetic macrocycles and methods of using peptidomimetic macrocycles to treat a condition. The present disclosure also describes methods of using peptidomimetic macrocycles in combination with at least one additional pharmaceutically-active agent for the treatment of a condition, for example, cancer.

专利号:US-2025084410-A1
优先权日:2015-01-12
标 题:Incorporation of unnatural nucleotides and methods thereof
发明人：PTACIN JEROD; MALYSHEV DENIS A; CAFFARO CAROLINA E
权利人:SYNTHORX INC
摘要:Disclosed herein are methods, compositions and kits for the synthesis of proteins which comprises unnatural amino acids that utilize a mutant tRNA.

专利号:US-2018371021-A1
优先权日:2017-05-11
标 题 :Peptidomimetic macrocycles and uses thereof
发明人：AIVADO MANUEL; GUERLAVAIS VINCENT; OLSON KAREN
权利人:AILERON THERAPEUTICS INC
摘要:The present disclosure describes the synthesis of peptidomimetic macrocycles and methods of using peptidomimetic macrocycles to treat a condition. The present disclosure also describes methods of using peptidomimetic macrocycles in combination with at least one additional pharmaceutically-active agent for the treatment of a condition, for example, cancer.

专利号:WO-2021072167-A1
优先权日:2019-10-10
标 题:Compositions and methods for in vivo synthesis of unnatural polypeptides

专利号:US-11091522-B2
优先权日:2018-07-23
标题 :Peptidomimetic macrocycles and uses thereof
发明人：AIVADO MANUEL; GUERLAVAIS VINCENT; OLSON KAREN; ANNIS DAVID ALLEN
权利人:AILERON THERAPEUTICS INC
摘要:The present disclosure describes the synthesis of peptidomimetic macrocycles and methods of using peptidomimetic macrocycles to treat a condition. The present disclosure also describes methods of using peptidomimetic macrocycles in combination with at least one additional pharmaceutically-active agent for the treatment of a condition, for example, cancer.