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参考文献:有针对性的酶工程揭示了卤化酶稳定化的意外模式
标题:有针对性的酶工程揭示了卤化酶稳定化的意外模式
摘要:卤化酶是用于选择性ch活化的有价值的生物催化剂,但是尽管最近通过蛋白质工程努力扩大了其应用范围,但仍需要提高热稳定性和催化效率.一种定向进化运动,旨在产生具有热稳定性的黄素依赖性色氨酸6-卤化酶,并具有适合化学酶学目的的合理活性.通过将连续几轮eppcr与半理性诱变相结合来解决这些特征,从而导致三重突变体(thal-Glv)的热稳定性大大提高(mt M= 23.5 K),并且在25oc下的活性比野生型酶高.此外,活性位点突变对热稳定性和对映选择性都有显着影响.我们的数据有助于对生物卤化作用的详细理解,并为将来的工程策略提供了深厚的基础,以促进这些有吸引力的生物催化剂的化学酶法应用.
DOI:10.1002/cctc.201901827

专利信息

专利号:US-12351573-B2
优先权日:2019-05-09
标 题:Compounds for use in synthesis of peptidomimetics
发明人：AL-ABED YOUSEF; CHENG KAI FAN
权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
摘要:Synthesis of O-benzotriazole and O-imidazole synthons are described. Uses of synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the synthons and uses of azapeptides and other peptidomimetics are also described.

专利号:US-2023159450-A1
优先权日:2020-05-08
标 题 :Dimers for use in synthesis of peptidomimetics
发明人：AL-ABED YOUSEF; ALTITI AHMAD
权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
摘要:Dimers for use in synthesis of peptidomimetics are described. Uses of dimers as synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the dimers and uses of azapeptides and other peptidomimetics are also described.

专利号:US-2020354404-A1
优先权日:2019-05-09
标 题 :Peptidomimetic agents, synthesis and uses thereof
发明人：AL-ABED YOUSEF
权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
摘要:Compounds for use in synthesis of peptidomimetic agents; synthesis of peptidomimetic agents; peptidomimetic diagnostic and therapeutic agents; and uses of the compounds and peptidomimetic agents in drug discovery, diagnosis, prevention and treatment of diseases are described.

专利号:WO-2025128985-A1
优先权日:2023-12-14
标题 :Sulfoxide and sulfone derivatives of thiocarbazates as synthons for azapeptides synthesis and process of using same
发明人：AL-ABED YOUSEF
权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
摘要:Provided for herein are sulfoxide and sulfone derivatives of thiocarbazates that have the formula (I): wherein A, R, R 1 , R 2 , and n are defined herein. The compounds may be used as synthons in the synthesis of azaeptides and other aza- amino acid conjugates.

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.