1558-59-4Relevant academic research and scientific papers
Asymmetric reductive amination by a wild-type amine dehydrogenase from the thermophilic bacteria: Petrotoga mobilis
Mayol, Ombeline,David, Sylvain,Darii, Ekaterina,Debard, Adrien,Mariage, Aline,Pellouin, Virginie,Petit, Jean-Louis,Salanoubat, Marcel,De Berardinis, Véronique,Zaparucha, Anne,Vergne-Vaxelaire, Carine
, p. 7421 - 7428 (2016)
The biocatalytic reductive amination of ketone to chiral amine is one of the most challenging reactions. Using a genome-mining approach, we found proteins catalyzing the reductive amination of ketones without a carboxylic function in the α or β position. The synthesis of (4S)-4-aminopentanoic acid (ee ≥99.5%) was achieved with the thermoactive amine dehydrogenase (AmDH) AmDH4 from Petrotoga mobilis in 88% yield. The high stability and substrate tolerance make AmDH4 a very good starting point for further discovery of reductive amination biocatalysts with an enlarged substrate range. This is the first report of wild-type enzymes with related genes having proper NAD(P)H-AmDH activity.
APOPTOSIS SIGNAL-REGULATING KINASE INHIBITORS AND USES THEREOF
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Paragraph 00485, (2019/04/09)
Described herein are ASK1 inhibitors and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for the treatment of blood disease, autoimmune disorders, pulmonary disorders, hypertension, inflammatory diseases, fibrotic diseases, diabetes, diabetic nephropathy, renal diseases, respiratory diseases, cardiovascular diseases, acute lung injuries, acute or chronic liver diseases, and neurodegenerative diseases.
Potent Antimicrobial Activity of Lipidated Short α,γ-Hybrid Peptides
Benke, Sushil N.,Thulasiram, Hirekodathakallu V.,Gopi, Hosahudya N.
, p. 1610 - 1615 (2017/10/16)
Herein we report the potent antimicrobial activity of α,γ-hybrid lipopeptides composed of 1:1 alternating α- and γ-amino acids. Along with their potent antimicrobial activity against various Gram-positive and Gram-negative bacteria, these hybrid lipopepti
Substrate profile of an ω-transaminase from Burkholderia vietnamiensis and its potential for the production of optically pure amines and unnatural amino acids
Jiang, Jinju,Chen, Xi,Feng, Jinhui,Wu, Qiaqing,Zhu, Dunming
, p. 32 - 39 (2014/01/06)
A new (S)-enantioselective ω-transaminase (ω-TA) gene from Burkholderia vietnamiensis G4 was functionally expressed in Escherichia coli BL21 (DE3), and the purified recombinant N-terminal His-tagged ω-TA (HBV-ω-TA) had a dimeric structure with optimum pH and temperature of 8.4 and 40 C, respectively. The enzyme showed higher activities toward aromatic amines than aliphatic amines and (S)-1-methylbenzylamine ((S)-α-MBA) was the most active amino donor. For amino acceptor, keto acids, keto esters and aldehydes were more reactive than ketones with pyruvate ethyl ester being most active. Several chiral amines and unnatural amino acids or esters were synthesized using HBV-ω-TA as the catalyst and isopropylamine or (S)-α-MBA as amino donor. Notably, HBV-ω-TA catalyzed the amino transfer to β-keto esters to give optically pure β-amino acid esters. In addition, glyoxylate was used as amino acceptor for the first time in the kinetic resolution of racemic amines and optically pure amines, such as (R)-1-methylbenzylamine, (R)-1-phenylpropylamine, (R)-2-amino-4-phenylbutane and (R)-1-aminotetraline, were obtained.
A convenient synthesis of racemic and optically active 1-aza-1,3-dienes derived from γ-amino esters: Reduction to α,β-unsaturated and saturated γ-amino acid derivatives
Palacios, Francisco,Aparicio, Domitila,García, Jesús,Rodríguez, Encina,Fernández-Acebes, Alvaro
, p. 3131 - 3141 (2007/10/03)
A simple synthesis of racemic and optically active 1-azadienes derived from γ-amino esters by olefination reaction of alkyl glyoxylates and functionalized phosphonium salts or phosphine oxides is reported. Selective reduction of these 1-azadienes with hydrides yields (E)-γ-amino-α,β-unsaturated esters. A simple procedure for the preparation of saturated γ-amino acids and γ-amino esters from the previously synthesized vinylogous amino esters is also described.
