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Search term: pharmacology

Results 1 - 100 of 585 > >>
EC Number
Application
Commentary
alcohol dehydrogenase
pharmacology
the alcohol dehydrogenase effectively catalyzes the reductions of various substituted alpha-chloroacetophenones to form the (R)-enantiomer of the corresponding chlorohydrins with excellent ennatiomeric purity. The co-factor NADH can be recycled by the D-glucose dehydrogenase and D-glucose regeneration system or via the simple hydrogen transfer mode using iso-propanol as the hydrogen donor. The applicability of the alcohol-dehydrogenase-catalyzed hydrogen transfer reduction in the synthesis of optically active chlorohydrins is demonstrated by carrying out several reductions on the preparative scale. Thus enzyme is a valuable biocatalyst for the preparation of chiral chlorohydrins of pharmaceutical interest
homoserine dehydrogenase
pharmacology
enzyme is a target for inhibitor design for construction of antimicrobial agents
L-xylulose reductase
pharmacology
enzyme is a target for design and development of potent and specific structure-based inhibitors binding in the active site
mannitol-1-phosphate 5-dehydrogenase
pharmacology
inhibition of AfM1PDH might be a useful target for therapy of Aspergillus fumigatus infections
UDP-glucose 6-dehydrogenase
pharmacology
target for inhibitor design
3-hydroxyacyl-CoA dehydrogenase
pharmacology
the short-chain 3-hydroxyacyl-CoA dehydrogenase is a target for intervention in case of Alzheimer's disease and Parkinson's disease
11beta-hydroxysteroid dehydrogenase (NAD+)
pharmacology
the enzyme is an important therapeutic target for diabetes in humans
phosphogluconate dehydrogenase (NADP+-dependent, decarboxylating)
pharmacology
the enzyme is a target for inhibitor development for usage as drugs against African Trypanosomiasis
3-quinuclidinone reductase (NADPH)
pharmacology
stereospecific production of (R)-3-quinuclidinol, an important chiral building block for the synthesis of various pharmaceuticals
3-quinuclidinone reductase (NADH)
pharmacology
stereospecific production of (R)-3-quinuclidinol, an important chiral building block for the synthesis of various pharmaceuticals
3-quinuclidinone reductase (NADH)
pharmacology
stereospecific production of (R)-3-quinuclidinol, an important chiral building block for the synthesis of various pharmaceuticals. The 3-quinuclidinone reductase and Leifsonia sp. alcohol dehydrogenase genes are efficiently expressed in Escherichia coli cells. A number of constructed Echerichia coli biocatalysts (intact or immobilized) are applied to the resting cell reaction and optimized. Under the optimized conditions, (R)-(-)-3-quinuclidinolis synthesized from 3-quinuclidinone (15% w/v, 939 mM) giving a conversion yield of 100% for the immobilized enzyme. The optical purity of the (R)-(-)-3-quinuclidinol produced by the enzymatic reactions is above 99.9%
3-quinuclidinone reductase (NADH)
pharmacology
stereospecific production of (R)-3-quinuclidinol, an important chiral building block for the synthesis of various pharmaceuticals, high yield of (R)-3-quinuclidinol up to 916 g/L * d using a bioreduction approach
3-quinuclidinone reductase (NADH)
pharmacology
stereospecific production of (R)-3-quinuclidinol, an important chiral building block for the synthesis of various pharmaceuticals; stereospecific production of (R)-3-quinuclidinol, an important chiral building block for the synthesis of various pharmaceuticals. The 3-quinuclidinone reductase and Leifsonia sp. alcohol dehydrogenase genes are efficiently expressed in Escherichia coli cells. A number of constructed Echerichia coli biocatalysts (intact or immobilized) are applied to the resting cell reaction and optimized. Under the optimized conditions, (R)-(-)-3-quinuclidinolis synthesized from 3-quinuclidinone (15% w/v, 939 mM) giving a conversion yield of 100% for the immobilized enzyme. The optical purity of the (R)-(-)-3-quinuclidinol produced by the enzymatic reactions is above 99.9%
11beta-hydroxysteroid dehydrogenase
pharmacology
the enzyme is an important therapeutic target for diabetes in humans
11beta-hydroxysteroid dehydrogenase
pharmacology
isozyme 11beta-HSD1 is a target in treatment of metabolic diseases such as diabetes mellitus type 2 or obesity
prostaglandin-F synthase
pharmacology
enzyme is a target for cyclooxygenase-independent antineoplastic actions of nonsteroidal anti-inflammatory drugs
IMP dehydrogenase
pharmacology
the enzyme is a potential target as modulators in MTX chemotherapy of resistant cells, overview
quinate/shikimate dehydrogenase
pharmacology
enzymes of the shikimate pathway has been promoted as a target for the development of antimicrobial agents
zerumbone synthase
pharmacology
zerumbone is a predominating potential multi-anticancer agent
aspartate-semialdehyde dehydrogenase
pharmacology
enzyme is a target for development of antibiotics
aspartate-semialdehyde dehydrogenase
pharmacology
inhibitor design from enzyme three-dimensional structure
glyceraldehyde-3-phosphate dehydrogenase (phosphorylating)
pharmacology
lung-stage schistosomula immunofluorescence reactivity is diminished following antiserum absorption with reconbinant glyceraldehyde 3-phosphate dehydrogenase. Discussion of glyceraldehyde 3-phosphate dehydrogenase as a candidate vaccine antigen
aldehyde oxidase
pharmacology
metabolic inactivation of neonicotinoid insecticide substrates by enzyme system coupled with Drosophila nicotinic acetylcholine receptor
enoyl-[acyl-carrier-protein] reductase (NADH)
pharmacology
the enzyme is a target for the antitubercular drug isoniazid. InhA inhibitors targeted at the enoyl substrate binding site may be effective against existing isoniazid-resistant strains of Mycobacterium tuberculosis
enoyl-[acyl-carrier-protein] reductase (NADH)
pharmacology
the enzyme is a target for developing novel anti-tubercular agents
enoyl-[acyl-carrier-protein] reductase (NADH)
pharmacology
the enzyme is a target for developing novel anti-tubercular agents; the enzyme is a target for the antitubercular drug isoniazid. InhA inhibitors targeted at the enoyl substrate binding site may be effective against existing isoniazid-resistant strains of Mycobacterium tuberculosis
dihydroorotate dehydrogenase (NAD+)
pharmacology
drug design based upon selective enzyme inhibition
3-oxo-5alpha-steroid 4-dehydrogenase (NADP+)
pharmacology
enzyme is a target for drug developement
DELTA14-sterol reductase
pharmacology
enzyme is a potential antifungal target site, development of antifungal compounds
DELTA24-sterol reductase
pharmacology
3beta-hydroxysterol DELTA24-reductase on the surface of hepatitis C virus-related hepatocellular carcinoma cells can be a target for molecular targeting therapy
meromycolic acid enoyl-[acyl-carrier-protein] reductase
pharmacology
structural investigations of reactive isoniazid species in order to promote the design of new inhibitors of InhA as potential antituberculous drugs
meromycolic acid enoyl-[acyl-carrier-protein] reductase
pharmacology
the enzyme is a target for the development of new anti-tubercular drugs
meromycolic acid enoyl-[acyl-carrier-protein] reductase
pharmacology
the enzyme is a target for developing novel anti-tubercular agents
meromycolic acid enoyl-[acyl-carrier-protein] reductase
pharmacology
the enzyme is a target for developing novel anti-tubercular agents; the enzyme is a target for the development of new anti-tubercular drugs
L-galactonolactone oxidase
pharmacology
because humans lack the capacity to synthesize ascorbate, the trypanosomal enzymes involved in ascorbate biosynthesis are interesting targets for drug therapy
dihydroorotate dehydrogenase (quinone)
pharmacology
A77 1726 inhibits cell growth in multiple myeloma cell lines at clinically achievable concentrations by induction of apoptosis. Inhibition of cell growth is partly due to inhibition of multiple myeloma cell proliferation. A77 1726 shows synergistic and additive activity together with genotoxic agents melphalan, treosulfan, and doxorubicin
glutaryl-CoA dehydrogenase (ETF)
pharmacology
targeted suppression of GCDH by lentivirus-mediated shRNA and excessive intake of lysine may be a useful cell model of glutaric aciduria type 1, overview
coproporphyrinogen dehydrogenase
pharmacology
the structure of HemN sets the stage for the development of inhibitors with antibacterial function due to the uniquely bacterial occurence of the enzyme
menaquinone-9 beta-reductase
pharmacology
menaquinone synthesis may be a drug target in Mycobacterium tuberculosis
menaquinone-9 beta-reductase
pharmacology
menaquinone synthesis may be a drug target in Mycobacteria
D-amino-acid oxidase
pharmacology
co-administration of the enzyme inhibitor 5-chloro-benzo[d]isoxazol-3-ol significantly enhances the efficacy of D-serine in attenuating prepulse inhibition deficits by administration of dizocilpine, an NMDA receptor antagonist. Therefore, co-administration of D-serine and a DAAO inhibitor has therapeutic potential for the treatment of schizophrenia
D-amino-acid oxidase
pharmacology
diminished DAO activity and elevations in D-serine may serve as an effective therapeutic intervention for the treatment of psychiatric symptoms
pteridine reductase
pharmacology
successful antifolate chemotherapy in Leishmania will have to target simultaneously both pterine reductase 1 and dihydrofolate reductase-thymidylate synthase
N1-acetylpolyamine oxidase
pharmacology
N,N'-butanedienyl butanediamine, i.e. MDL 72527 or CPC-200, a small molecule specific inhibitor of polyamine oxidase, effectively blocks androgen-induced reactive oxygen species production in human prostate cancer cells, as well as significantly delays prostate cancer progression and death in animals developing spontaneous prostate cancer
NAD(P)H dehydrogenase (quinone)
pharmacology
a series of lavendamycin analogues are tested in docking studies employing an X-ray derived NQO1 active site computational model, structure-based analogue design criteria are valid, resulting in the design of two analogues with high substrate specificity and selective toxicity toward NQO1-rich cells
aromatic nitroreductase [NAD(P)H]
pharmacology
Pseudomonas aeruginosa NfsB and nitro-CBI-DEI is a promising enzyme/prodrug combination for gene directed enzyme prodrug therapy
factor-independent urate hydroxylase
pharmacology
urate oxidase is a potential therapeutic protein in the prevention and treatment of tumor lysis syndrome and hyperuricemia. However, its severe immunogenicity limits its clinical application. Engineering site-specific modifications of keto groups in urate oxidase by using evolved Methanocaldococcus jannaschii aminoacyl-tRNA synthetase(s)/suppressor tRNA pairs reduces its antigenicity. The mutated uricase exhibits decreased antigenic properties, while its catalytic activities remain unchanged
glutathione-disulfide reductase
pharmacology
enzyme is a target for enzyme inhibitor and antimalarial drug development
CoA-glutathione reductase
pharmacology
anti-staphylococcal agent, possible target for the design of selective inhibitors that would interrupt the thiol metabolism of the human pathogen Staphylococcus aureus
trypanothione-disulfide reductase
pharmacology
enzyme is a drug target
trypanothione-disulfide reductase
pharmacology
enzyme is a target for selective drug design
trypanothione-disulfide reductase
pharmacology
trypanothione reductase plays a central role in the trypanosomatid parasite’s defense against oxidative stress, trypanothione reductase is a promising target for antitrypanosomal drugs, 2-iminobenzimidazole class are potent trypanothione reductase inhibitors against Trypanosoma brucei rhodesiense and low cytotoxicity against human cells
trypanothione-disulfide reductase
pharmacology
trypanothione reductase plays a central role in the trypanosomatid parasite’s defense against oxidative stress, trypanothione reductase is a promising target for antitrypanosomal drugs, novel inhibitors are identified
trypanothione-disulfide reductase
pharmacology
trypanothione reductase plays a central role in the trypanosomatid parasite’s defense against oxidative stress, trypanothione reductase is a promising target for antitrypanosomal drugs, synthesis of dethiotrypanothione and related trypanothione analogues featuring ring-closing olefin metathesis macrocyclizations is described
trypanothione-disulfide reductase
pharmacology
trypanothione reductase plays a central role in the trypanosomatid parasite’s defense against oxidative stress, trypanothione reductase is a promising target for antitrypanosomal drugs, binding affinity towards trypanothione reductase and glutathione reductase of nitrofuran derivatives is assessed by standard molecular docking procedures and both, energy and structural output analysis, nitrofuran ligands display a slight preference to bind the closely related human glutathione reductase, they should not be considered as drugs with selective inhibition of trypanothione reductase
3-hydroxyanthranilate 3,4-dioxygenase
pharmacology
the enzyme is a target for pharmacological downregulation because it is involved in formation of quinolinic acid, a highly potent excitotoxin implicated in a number of neurodegenerative conditions
arachidonate 5-lipoxygenase
pharmacology
human 5-lipoxygenase is a well-validated target for anti-inflammatory therapy. Development of 5-LOX inhibitors with higher activities is highly required
indoleamine 2,3-dioxygenase
pharmacology
first reaction in the tryptophan catabolic pathway in mammals
indoleamine 2,3-dioxygenase
pharmacology
IDO-1 is a target for pharmacological inhibition in the treatment of cancer
sulfur oxygenase/reductase
pharmacology
sulfur metabolism
Renilla-type luciferase
pharmacology
used as an assay for assessing potential liver toxicity by measuring GADD45-beta induction as an control for increased DNA damage
Renilla-type luciferase
pharmacology
investigations into regulation and functional roles of kinases
[histone-H3]-lysine-9-demethylase
pharmacology
KDM4A possesses the potential to act as an oxygen sensor in the context of chromatin modifications, with possible implications for epigenetic regulation in hypoxic disease states
hyoscyamine (6S)-dioxygenase
pharmacology
tropane alkaloids including hyoscyamine, anisodamine, scopolamine and anisodine, are used medicinally as anticholinergic agents with increasing market demand, improvement of production by metabolic engineering introduction of genes encoding the branch-controlling enzyme tropinone reductase I and the downstream rate-limiting enzyme hyoscyamine-6beta-hydroxylase
proline 3-hydroxylase
pharmacology
the prolyl 3-hydroxylase P3H2 is a novel targets for epigenetic silencing in breast cancer; the prolyl 3-hydroxylase P3H3 is a novel targets for epigenetic silencing in breast cancer
hypoxia-inducible factor-proline dioxygenase
pharmacology
modulation of PHD2 activity might be considered as a new way to inhibit glioblastoma progression
kynurenine 3-monooxygenase
pharmacology
the enzyme is a potential drug target for treatment of neurodegenerative disorders such as Huntington's and Alzheimer's diseases
kynurenine 3-monooxygenase
pharmacology
kynurenine represents a branch point of the kynurenine pathway, being converted into the neurotoxin 3-hydroxykynurenine via kynurenine monooxygenase, neuroprotectant kynurenic acid, and anthranilic acid. As a result of this branch point, kynurenine monooxygenase is an attractive drug target for several neurodegenerative and/or neuroinflammatory diseases, especially Huntington's, Alzheimer's, and Parkinson's diseases
anhydrotetracycline 6-monooxygenase
pharmacology
synthesis of chlortetracycline
nitric-oxide synthase (NADPH)
pharmacology
NO synthase can be used to gain insight into the biological role of endogenous agmatine
4-hydroxybenzoate 1-hydroxylase
pharmacology
construction of a novel artificial pathway for arbutin biosynthesis in Escherichia colid. De novo biosynthesis of arbutin from simple carbon sources is established and a generalizable strategy for the biosynthesis of shikimate pathway derived chemicals is provided. Arbutin is a hydroquinone glucoside compound existing in various plants. It is widely used in pharmaceuticaland cosmetic industries owing to its well-known skin-lightening property as well as anti-oxidant, anti-microbial, and anti-inflammatory activities. A 4-hydroxybenzoate 1-hydroxylase gene from Candida parapsilosis CBS604 and a glucosyltransferase (arbutin synthase) gene from Rauvolfia serpentina are introduced into Escherichia coli lead to the production of 54.71 mg/l of arbutin from glucose. Further redirection of carbon flux into arbutin biosynthesis pathway by enhancing shikimate pathway genes enables production of 3.29 g/l arbutin, which is a 60-fold increase compared with the initial strain. Final optimization of glucose concentration added in the culture medium is able to further improve the titer of arbutin to 4.19 g/l in shake flasks experiments, which is around 77-fold higher than that of initial strain
sterol 14alpha-demethylase
pharmacology
the chemotherapy of leishmaniasis is a serious problem in the field of neglected tropical diseases. Since the biosynthesis of specific sterols is vital for effective survival, normal proliferation and infectivity of Leishmania parasites, the sterol 14alpha-demethylase inhibitors obtained from azole antifungal drug discovery programs can be used in antileishmanial therapy
sterol 14alpha-demethylase
pharmacology
the enzyme constitutes an important biological target for the most popular class of antifungals
sterol 14alpha-demethylase
pharmacology
Chagas disease is caused by the protozoan parasite Trypanosoma cruzi, which depends on the production of endogenous sterols, and therefore can be blocked by sterol 14alpha-demethylase inhibitors
7-methylxanthine demethylase
pharmacology
methylxanthine intermediates of caffeine catabolism obtained by the action of N-demethylases have many applications. In medicine, theobromine and theophylline are used as diuretics, vasodilators, and myocardial stimulants. Monomethylxanthines can be converted to effective caffeine derivatives by chemical derivatization and hence can serve as interesting alternatives to caffeine. Xanthine also finds pharmaceutical application in drugs for treatment of asthma. The biotechnological potential of N-demethylases therefore lies not only in general decaffeination purposes but also in specific product recovery from caffeine
geraniol 8-hydroxylase
pharmacology
co-overexpression of geraniol-10-hydroxylase and strictosidine synthase improves anti-cancer drug camptothecin accumulation in Ophiorrhiza pumila
trans-cinnamate 4-monooxygenase
pharmacology
trans-cinnamate 4-monooxygenase plays a key role in the ability of phenylpropanoid metabolism to channel carbon to produce the 4-methoxybenzoyl group on the disaccharide moiety of OSW-1 (3beta,16beta,17alpha-trihydroxycholest-5-en-22-one 16-O-[O-[2-O-(4-methoxybenzoyl)-beta-D-xylopyranosyl]-(1->3)-2-O-acetyl-alpha-L-arabinopyranoside]). OSW-1 is about 10-100 times more cytotoxic than clinically applied anticanceragents such as mitomycin C, adriamycin, cisplatin, camptothecin, and paclitaxel, but has a low toxicity towards normal cells. This potency, in combination with a unique mechanism of action and selectivity toward malignant tumor cells, gives OSW-1 and its analogues great potential as anticancer agents
benzoate 4-monooxygenase
pharmacology
the enzyme is involved in detoxification of benzoate, a key intermediate in aromatic compound metabolism in fungi. Because this enzyme is unique to fungi, it is a promising drug target in fungal pathogens of other eukaryotes. By identifying selected derivatives of cinnamic acid as possible antifungal drugs, and CYP53 family enzymes as their targets, a potential inhibitor-target system for antifungal drugs is developed
sterol 14alpha-demethylase
pharmacology
-
sterol 14alpha-demethylase
pharmacology
all known functional sterols lack a 14alpha-methyl group, and therefore the 14alpha-demethylation reaction has received much attention from the pharmaceutical and agriculture-chemical industry as a possible means to specifically control and inhibit sterol biosynthesis in mammals, fungi, and plant; target enzyme for azole antifungal agents. These specific inhibitors are of great importance as plant growth regulators, fungicides and herbicides in the agricultural and medical fields; target enzyme for the design of phyla-specific sterol 14alpha-demethylase inhibitors
sterol 14alpha-demethylase
pharmacology
target for cholesterol-lowering drugs
sterol 14alpha-demethylase
pharmacology
CYP51 is a key target for fungal antibiotic therapy
sterol 14alpha-demethylase
pharmacology
the chemotherapy of leishmaniasis is a serious problem in the field of neglected tropical diseases. Since the biosynthesis of specific sterols is vital for effective survival, normal proliferation and infectivity of Leishmania parasites, the sterol 14alpha-demethylase inhibitors obtained from azole antifungal drug discovery programs can be used in antileishmanial therapy
sterol 14alpha-demethylase
pharmacology
the enzyme constitutes an important biological target for the most popular class of antifungals
sterol 14alpha-demethylase
pharmacology
Chagas disease is caused by the protozoan parasite Trypanosoma cruzi, which depends on the production of endogenous sterols, and therefore can be blocked by sterol 14alpha-demethylase inhibitors
sterol 14alpha-demethylase
pharmacology
target enzyme for azole antifungal agents. These specific inhibitors are of great importance as plant growth regulators, fungicides and herbicides in the agricultural and medical fields
C-19 steroid 1alpha-hydroxylase
pharmacology
modification at the C-1 position of a steroid is of pharmaceutical interest. Biotransformation can overcome tedious multistep chemical synthesis
peptidylglycine monooxygenase
pharmacology
enzyme is an attractive target for development of anti-tumor compounds
tyrosinase
pharmacology
results indicate that the polyvinylpyrrolidone (PVP)-wrapped fullerene derivative (Radical Sponge) could be expected for its wide-ranged application as a whitening cosmetic material
tyrosinase
pharmacology
study of suicide inactivation and irreversible inhibition is important in the functional design of synthetic inactivators for therapeutic applications
tyrosinase
pharmacology
results of low cytotoxicity, high inhibition of melanin synthesis and lack of effect on gene expression suggest that p-hydroxybenzyl alcohol can be a potential agent for skin lightening to be used in cosmetic products
tyrosinase
pharmacology
(2R,3R)-taxifolin isolated from Benitade may possibly be a of new tyrosinase inhibitor alternative to cosmetic agents such as arbutin and kojic
tyrosinase
pharmacology
kurarinol, kuraridinol, and trifolirhizin are candidates as skin-whitening agents
stearoyl-CoA 9-desaturase
pharmacology
enhancing SCD1-mediated desaturation of saturated fatty acids and subsequent formation of neutral lipid droplets may become a promising therapeutic target to reduce saturated fatty acid-induced lipotoxicity in the pathogenesis of diabetic nephropathy
stearoyl-CoA 9-desaturase
pharmacology
targeting SCD1 in combination with sorafenib may be another therapeutic strategy against liver cancer. Clinically, SCD1 serves as a good predictive marker for patient responses to sorafenib treatment. Targeting SCD1 synergizes the effect of sorafenib both in vitro and in vivo
sphingolipid 4-desaturase
pharmacology
the cells capacity to biosynthesize dihydroceramides must be taken into account in proautophagic Des1 inhibitors-including therapies
tryptophan 5-halogenase
pharmacology
5-Br- and 5-Cl-tryptophan could presumably be applied as a pharmacologically attractive precursor of serotonin
(S)-stylopine synthase
pharmacology
a microbial system is established for producing a protoberberine-type alkaloid (stylopine) in Pichia cells
(S)-cheilanthifoline synthase
pharmacology
a microbial system is established for producing a protoberberine-type alkaloid (stylopine) in Pichia cells
mycocyclosin synthase
pharmacology
CYP121 is a potential target for the treatment of Mycobacterium tuberculosis infections
Results 1 - 100 of 585 > >>