Lipases are endowed with a substrate specificity that surpasses that of any other known enzyme. This confers on these enzymes an application potential that is literally boundless. Lipases can be employed in the production of pharmaceuticals, cosmetics, leather, detergents, foods, perfumery, medical diagnostics, and other organic synthetic materials. This review attempts to present a comprehensive discussion on the present status of this unique group of enzymes in industry, as well as the actual potential. It represents an endeavor to provide a sincere answer to the question, “What can be done with this enzyme?” as well as, “Can lipase be utilized for this purpose?” It is intended that the manuscript will cover or at least mention all known applications, based on the exploitation of a particular type of reaction catalyzed by lipases. An attempt will be made to cover as large a number of references as possible, so as to further underline the importance and significance of lipase action for industry.

Applications of lipase

Comparison of lipases by different assays

http://digital.csic.es/bitstream/10261/17327/1/SUCROSE-ESTERS-digitalCSIC.pdf

Enzymatic acylation of di- and trisaccharides with fatty acids: choosing the appropriate enzyme, support and solvent

Biotransformations with Lipases

An amide of hyaluronic acid or a derivative thereof which comprises at least one repetitive unit of general formula (I): wherein R = NR6R7, or alcoholic group of the aliphatic, aromatic, arylaliphatic, cycloaliphatic, heterocyclic series, OH, O-, alcoholic group of hyaluronic acid, amino group of deacylated hyaluronic acid; R1, R2, R3, R4 = H, SO3-, acyl group derived from a carboxylic acid of the aliphatic, aromatic, arylaliphatic, cycloaliphatic, heterocyclic series, -CO- (CH2)2-COOY; Y = negative charge, or H; R5 = -CO-CH3, H, SO3-, acyl group derived from a carboxylic acid of the aliphatic, aromatic, arylaliphatic, cycloaliphatic, heterocyclic series, acylic group of hyaluronic acid; R6 = is H or a aliphatic, aromatic, arylaliphatic, cycloaliphatic, or heterocyclic group, substituted or unsubstituted; R7 = is H or an aliphatic, aromatic, arylaliphatic, cycloaliphatic, or heterocyclic group, substituted or unsubstituted; wherein at least one of R or R5 forms an amide group.

Amides of hyaluronic acid and the derivatives thereof and a process for their preparation

Regioselective deprotection of 3′,5′-O-acylated pyrimidine nucleosides by lipase and esterase

Lipase-catalyzed regioselective acylation of sugar moieties of nucleosides

With the aim of diminishing the toxicity of 5-fluorouracil (1) and obtaining biologically active derivatives of 1 suitable for oral administration, α-alkoxyalkyl groups were introduced at the 1-, 3-and 1, 3-positions of 1. Alkoxyalkylation can be effected by four methods : (i) reaction of 1-alkoxyalkyl chloride (2) with 1, (ii) reaction of acetal with 2, 4-bis (trimethylsiloxy)-5-fluoropy-rimidine, (iii) addition reaction of α-unsaturated ether with 1, (iv) aminolysis of 1-alkylthio-carbonyl-3-(1-alkoxyalkyl)-5-fluorouracil. The toxicity of the products was less than that of 1, and some of these compounds showed moderate antitumor activity against L-1210 leukemia.

5-Fluorouracil derivatives. X. Synthesis and antitumor activities of alpha-alkoxyalkyl-5-fluorouracils.

Selective protection of the three hydroxyl groups of sugar moiety of nucleosides have been studied by enzyme-catalyzed esterification in organic solvents. Selectively protected products were obtained. The reaction provides an efficient method for selective protection of nucleosides.

Enzyme Aided Regioselective Acylation of Nucleosides

The invention relates an epoxysuccinamide derivative represented by a formula (I): ##STR1## wherein R 1 represents a hydrogen atom, an alkyl or aminoalkyl group, R 2 represents an aminoalkyl group which May be substituted, an aryl group which may be substituted, a heterocyclic group which may be substituted, an aralkyl group which may be substituted, or an alkyl group substituted by a heterocyclic ring which may be substituted, or R 1 and R 2 may form a nitrogen-containing heterocyclic ring, which may be substituted, together with the adjacent nitrogen atoms, and R 3 and R 4 are the same or different from each other and independently represent a hydrogen atom, or an alkyl or aralkyl group, or a salt thereof, a preparation process thereof, and a medicine comprising such a derivative or salt as an active ingredient. This compound has a specific inhibitory activity for cathepsin L and family enzymes thereof, and is useful as an agent for preventing and treating metabolic osteopathy such as osteoporosis and hypercalcemia.

Atsuhiko Uemura

Papers

Regioselective deprotection of 3′,5′-O-acylated pyrimidine nucleosides by lipase and esterase

Lipase-catalyzed regioselective acylation of sugar moieties of nucleosides

5-Fluorouracil derivatives. X. Synthesis and antitumor activities of alpha-alkoxyalkyl-5-fluorouracils.

Enzyme Aided Regioselective Acylation of Nucleosides

Epoxysuccinamide derivative or salt thereof