Enzymatic clickable functionalization of peptides via computationally engineered peptide amidase

Directed peptides C-terminal modification enabled by the engineered biomolecular catalyst-peptide amidase 12 B has been achieved via computational protein engineering. The engineered enzyme exhibits great promising potential in the C-terminal modification of opioid peptides using prop-2-yn-1-amine(PYA) or prop-2-en-l-amine(PEA) as the nucleophile. A variety of opioid peptides could be readily functionalized at the C-terminal chain in high yield in a mild and selective manner. Notably, modified opioid peptides bearing alkynyl moiety could be further functionalized through well-established click reaction.

Isoniazid metabolism and hepatotoxicity

Isoniazid(INH) is highly effective for the management of tuberculosis.However,it can cause liver injury and even liver failure.INH metabolism has been thought to be associated with INH-induced liver injury.This review summarized the metabolic pathways of INH and discussed their associations with INH-induced liver injury.

Nitrogen slow-release behavior of oxamide granules in two different types of paddy soils

Oxamide is a potential slow-release nitrogen(N)fertilizer,especially under waterlogged conditions,due to its low solubility in water and the slow-release of ammonium by soil amidases.To investigate the effects of oxamide granules(2.00-2.38 mm in diameter)as a single basal fertilizer(180 or 144 kg N ha^(-1))on rice growth,soil properties,and N use efficiency in terms of N recovery efficiency(NRE),we conducted field experiments on two different types of paddy soils over two rice-growing seasons.Results showed that the fertilization effects of oxamide granules varied between the two types of paddy soils.In the red clayey paddy soil,the grain yields for both rice-growing seasons were high with a significantly higher NRE in the oxamide treatment than in the urea treatment.However,in the alluvial sandy paddy soil,the grain yields in the oxamide treatment were slightly lower than those in the urea treatment.Furthermore,oxamide produced little improvement in NRE in the alluvial sandy paddy soil.Soil incubation experiments over 98 d were also carried out to evaluate the factors affecting the N release behavior of oxamide granules in the two types of paddy soils.We found that the amidase activity was higher and,therefore,the oxamide hydrolysis rate was faster in the alluvial sandy paddy soil,which had a higher soil pH value and organic matter content,compared to the red clayey paddy soil.The faster N release and the longer growth period resulted in a mismatch between N supply by oxamide and rice demand,which,in turn,led to little improvement in NRE and a decreased grain yield in the alluvial sandy paddy soil,especially in the reduced oxamide treatment.These results could help select the appropriate size of oxamide granules for use as a slow-release N fertilizer depending on the soil properties and growth period of rice.

Synthesis of Optically Active β-Alkyl-α-methylene-γ-butyro- lactones from Enantioselective Biotransformation of Nitriles, an Unusual Inversion of Enantioselectivity

A new approach to optically active β-alkyl-α-methylene-γ-butyrolactone derivatives was reported from the Rhodococcus sp. AJ270-catalyzed hydrolysis of appropriate nitriles. The inversion of enantioselectivity of the amidase has been observed when a methyl protection was introduced into the hydroxy group of the parent substrate.