CAS: 149-61-1; Malate

📜2-氧代丁二酸置于bovine Heart Lactate Dehydrogenase A,还原型辅酶ⅰ体系中,用 Aq. Phosphate Buffer 用作溶剂,化学反应生成苹果酸根
参考文献:L-2-Hydroxyglutarate Production Arises From Noncanonical Enzyme Function At Acidic Ph
标题:L-2-Hydroxyglutarate Production Arises From Noncanonical Enzyme Function At Acidic Ph
摘要:酸化作用增强乳酸脱氢酶和苹果酸脱氢酶介导的从α-酮戊二酸产生l-2-羟基戊二酸(l-2Hg)的非特异性反应,并稳定hif-1α水平.代谢物2-羟基戊二酸(2Hg)可以作为d-R-或l-S-手性异构体产生,每种都能抑制涉及多种生物过程的α-酮戊二酸(αkg)依赖性酶.异柠檬酸脱氢酶(idh)的致癌突变产生d-2Hg,导致细胞分化的病理阻断.另一方面,氧气限制导致l-2Hg积累,这可以促进正常细胞和恶性细胞对低氧应激的生理适应.在此,我们证明纯化的乳酸脱氢酶(ldh)和苹果酸脱氢酶(mdh)通过非特异性还原替代底物αkg,催化特异性产生l-2Hg.酸性ph通过促进αkg的质子化形式,该形式结合到ldha的底物结合口袋中的关键残基,从而增强l-2Hg的产生.酸增强的l-2Hg产生导致在常氧条件下稳定缺氧诱导因子1α(hif-1α).这些发现提供了关于微环境因素如何影响代谢物产生,从而改变细胞命运和功能的机制的见解.
Doi:10.1038/nchembio.2307

专利信息

专利号:US-11891375-B2
优先权日:2021-07-26
标 题 :Method for the synthesis of 2,4-dimethylpyrimidin-5-ol, intermediates, and method for the synthesis of Lemborexant using the intermediates
发明人：AKHATOU ABDESLAM; DOBARRO RODRÃ?GUEZ ALICIA
权利人:MOEHS IBERICA SL
摘要:A method is for the synthesis of 2,4-dimethylpyrimidin-5-ol, which can be used as an intermediate compound in the synthesis of Lemborexant. The method includes reacting a nitrophenyl compound with N,N-dimethylformamide diethyl acetal.

专利号:US-2009221568-A1
优先权日:2005-11-04
标题:Synthesis of Inhibitors of FtsZ
发明人：SHAW JARED; URGAONKAR SAMEER; RAYCHAUDHURI DEBABRATA; LA PIERRE HENRY
权利人:SHAW JARED; URGAONKAR SAMEER; RAYCHAUDHURI DEBABRATA; LA PIERRE HENRY
摘要:FtsZ, the bacterial analog of tubulin, is a promising new target for developing new antibiotics. It has been shown that polyphenols inhibit the GTPase activity of FtsZ, thereby inhibiting Z-ring formation during mitosis. The present invention provides novel polyphenols compounds, which can be accessed by the synthesis of dichamametin and 2′″-hydroxy-5″-benzylisouvarinol-B as described herein. These novel compounds are useful in treating infections, particularly infections caused by gram-positive organisms. Methods of preparing the inventive compounds are also provided. The compounds are prepared by the benzylation of pinocembrin or chrysin core structure. Pharmaceutical compositions and method of using the compounds to treat disease are also provided. These compounds may be screened for antimicrobial activity as well as other biological activities such as anti-neoplastic, anti-inflammatory, immunosuppressive, and cytotoxic activity.

专利号:US-10973847-B2
优先权日:2017-06-30
标题 :Core-to-surface polymerization for the synthesis of star polymers and uses thereof
发明人：JOHNSON JEREMIAH A; GOLDER MATTHEW R
权利人:MASSACHUSETTS INST TECHNOLOGY
摘要:Disclosed are methods, compositions, reagents, systems, and kits to prepare star polymers, as well as compositions and uses thereof. Various embodiments show that synthesis of these polymers contain low metal concentration to provide polymers for diverse biomedical applications including in vivo applications.

专利号:US-2025066288-A1
优先权日:2022-06-11
标 题 :Dihydrazide-dihydrazone compounds with adamantyl moiety and a process for synthesis of the same
发明人：PAWAR RUPA SACHIN
权利人:PAWAR RUPA SACHIN
摘要:The present disclosure relates generally to organic compounds. More specifically, the disclosure is directed to a dihydrazide-dihydrazone compound of Formula (I), a stereoisomer, a tautomer, a pharmaceutically acceptable salt or a pharmaceutically acceptable solvate thereof. The compounds of the present disclosure possess anti-microbial activity, specifically antifungal and antibacterial activity. The present disclosure also provides a process of synthesis of the compound of Formula (I).

专利号:US-7189849-B2
优先权日:1997-02-10
标 题:Synthesis of acyclic nucleoside derivatives
发明人：LEANNA M ROBERT; RASMUSSEN MICHAEL; HANNICK STEVEN M; TIEN JIEN-HEH J; LUKIN KIRILL A; TIAN ZHENPING; CHANG SOU-JEN; CURTY CYNTHIA B; NARAYANAN BIKSHANDARKOIL A; BELLETTINI JOHN; SHELAT BHADRA; SPITZ TIFFANY
权利人:MEDIVIR AB
摘要:Novel processes towards the synthesis of the antiviral valomaciclovir stearate in which an esterified guanine acetal is reduced to the corresponding alcohol, reacted with an activated amino acid and N-deprotected. The esterified guanine acetal is prepared from a 9-guanine derivative bearing an acyclic hydroxymethylbutylacetal. The processes are amendable to one-pot reactions.

专利号:US-2025002518-A1
优先权日:2023-06-16
标 题 :Synthesis of heteroarynes and use thereof
发明人：MATTMILLER ROBERTS COURTNEY COLLEEN; HUMKE JENNA NICOLE; QUINLIVAN ANSEL ANNABEL; BELLI ROMAN GIANCARLO; KARGBO SALLU SO; PLASEK ERIN ELIZABETH
权利人:UNIV MINNESOTA
摘要:Disclosed herein are heterocyclic arynes and methods for preparing the same. Heteroarynes such as 5-membered O- or N-heterocyclic arynes have been considered inaccessible due to ring strain associated with the triple bond. The methods described herein demonstrate that these arynes can be successfully prepared through the utility of pi-backbonding from a transition metal. Synthetic utility of this method has been demonstrated by the facile synthesis and functionalization of heterocycles using these heteroaryne building blocks.