Kanamycin kinase (original) (raw)

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Aminoglycoside-3'-phosphotransferase (APH(3')), also known as aminoglycoside kinase, is an enzyme that primarily catalyzes the addition of phosphate from ATP to the 3'-hydroxyl group of a 4,6-disubstituted aminoglycoside, such as kanamycin. However, APH(3') has also been found to phosphorylate at the 5'-hydroxyl group in 4,5-disubstituted aminoglycosides, which lack a 3'-hydroxyl group, and to diphosphorylate hydroxyl groups in aminoglycosides that have both 3'- and 5'-hydroxyl groups. Primarily positively charged at biological conditions, aminoglycosides bind to the negatively charged backbone of nucleic acids to disrupt protein synthesis, effectively inhibiting bacterial cell growth. APH(3') mediated phosphorylation of aminoglycosides effectively disrupts their mechanism of action, intro

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dbo:abstract Aminoglycoside-3'-phosphotransferase (APH(3')), also known as aminoglycoside kinase, is an enzyme that primarily catalyzes the addition of phosphate from ATP to the 3'-hydroxyl group of a 4,6-disubstituted aminoglycoside, such as kanamycin. However, APH(3') has also been found to phosphorylate at the 5'-hydroxyl group in 4,5-disubstituted aminoglycosides, which lack a 3'-hydroxyl group, and to diphosphorylate hydroxyl groups in aminoglycosides that have both 3'- and 5'-hydroxyl groups. Primarily positively charged at biological conditions, aminoglycosides bind to the negatively charged backbone of nucleic acids to disrupt protein synthesis, effectively inhibiting bacterial cell growth. APH(3') mediated phosphorylation of aminoglycosides effectively disrupts their mechanism of action, introducing a phosphate group that reduces their binding affinity due to steric hindrances and unfavorable electrostatic interactions. APH(3') is primarily found in certain species of gram-positive bacteria. This enzyme belongs to the family of transferases, specifically those transferring phosphorus-containing groups (phosphotransferases) with an alcohol group as acceptor. The systematic name of this enzyme class is ATP:kanamycin 3'-O-phosphotransferase. This enzyme is also called neomycin-kanamycin phosphotransferase. (en) カナマイシンキナーゼ（kanamycin kinase、EC 2.7.1.95）は、以下の化学反応を触媒する酵素である。 ATP + カナマイシン ADP + カナマイシン-3'-リン酸 従って、この酵素の基質はATPとカナマイシンの2つ、生成物はADPとの2つである。 この酵素は転移酵素、特にアルコールを受容体とするに分類される。この酵素の系統名は、ATP:カナマイシン 3'-O-ホスホトランスフェラーゼ（ATP:kanamycin 3'-O-phosphotransferase）である。ネオマイシン-カナマイシンホスホトランスフェラーゼ（neomycin-kanamycin phosphotransferase）とも呼ばれる。 この酵素はカナマイシンだけでなく、4,6-二置換アミノグリコシドの3'-ヒドロキシル基に対してリン酸基の付加を触媒するため、アミノグリコシド-3'-ホスホトランスフェラーゼ（aminoglycoside-3'-phosphotransferase、APH(3')）またはアミノグリコシドキナーゼ（aminoglycoside kinase）とも呼ばれる。APH(3')はさらに、3'-ヒドロキシル基が存在しない4,5-二置換アミノグリコシドに対しては5'-ヒドロキシル基のリン酸化を行い、3'-ヒドロキシル基、5'-ヒドロキシル基の双方を持つアミノグリコシドに対してはその双方のリン酸化を行う。アミノグリコシドは生物学的条件下で主に正に帯電しているため、負に帯電した核酸の主鎖に結合してタンパク質合成を阻害し、細菌の細胞成長を効果的に阻害する。APH(3')はアミノグリコシドにリン酸基を導入し、立体障害と静電的反発によって結合親和性を低下させることでアミノグリコシドの作用を効果的に阻害する。 APH(3')は、主に特定種のグラム陽性菌に存在する。 (ja)
dbo:ecNumber 2.7.1.95
dbo:thumbnail wiki-commons:Special:FilePath/APHStructure.png?width=300
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dbo:wikiPageWikiLink dbr:Aminoglycoside dbr:List_of_enzymes dbr:Metaphosphate dbr:Antimicrobial_resistance dbr:Antiparallel_(biochemistry) dbr:Vector_(molecular_biology) dbr:Ligand_(biochemistry) dbr:Kanamycin dbr:Nucleic_acids dbc:EC_2.7.1 dbc:Enzymes_of_known_structure dbr:Enzyme dbr:Genetic_engineering dbr:Protein_kinases dbr:Magnesium dbr:Protein_biosynthesis dbr:Mutagenesis dbr:Active_site dbr:Dissociative_substitution dbr:Steric_effects dbr:Adenosine_triphosphate dbr:Amino_acid dbr:Gram-positive_bacteria dbr:Protein_conformation dbr:Stem-loop dbr:Disulfide_bonds dbr:C-terminus dbr:Phosphate dbr:Polymer dbr:Neomycin dbr:Catalysis dbr:X-ray_crystallography dbr:Hydroxyl dbr:N-terminus dbr:Phosphotransferase dbr:Transferase dbr:Alpha-helix dbr:Beta-sheet dbr:File:APHActiveSite.png dbr:File:APHNegativeBindinPocket.png dbr:File:APHReactionMechanism.png dbr:File:APHRxnScheme.png
dbp:caption Structure of APH, taken from 1L8T (en)
dbp:casNumber 62213 (xsd:integer)
dbp:ecNumber 2.700000 (xsd:double)
dbp:goCode 8910 (xsd:integer)
dbp:iubmbEcNumber 2 (xsd:integer)
dbp:name kanamycin kinase (en)
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gold:hypernym dbr:Enzyme
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rdfs:comment Aminoglycoside-3'-phosphotransferase (APH(3')), also known as aminoglycoside kinase, is an enzyme that primarily catalyzes the addition of phosphate from ATP to the 3'-hydroxyl group of a 4,6-disubstituted aminoglycoside, such as kanamycin. However, APH(3') has also been found to phosphorylate at the 5'-hydroxyl group in 4,5-disubstituted aminoglycosides, which lack a 3'-hydroxyl group, and to diphosphorylate hydroxyl groups in aminoglycosides that have both 3'- and 5'-hydroxyl groups. Primarily positively charged at biological conditions, aminoglycosides bind to the negatively charged backbone of nucleic acids to disrupt protein synthesis, effectively inhibiting bacterial cell growth. APH(3') mediated phosphorylation of aminoglycosides effectively disrupts their mechanism of action, intro (en) カナマイシンキナーゼ（kanamycin kinase、EC 2.7.1.95）は、以下の化学反応を触媒する酵素である。 ATP + カナマイシン ADP + カナマイシン-3'-リン酸 従って、この酵素の基質はATPとカナマイシンの2つ、生成物はADPとの2つである。 この酵素は転移酵素、特にアルコールを受容体とするに分類される。この酵素の系統名は、ATP:カナマイシン 3'-O-ホスホトランスフェラーゼ（ATP:kanamycin 3'-O-phosphotransferase）である。ネオマイシン-カナマイシンホスホトランスフェラーゼ（neomycin-kanamycin phosphotransferase）とも呼ばれる。 (ja)
rdfs:label Kanamycin kinase (en) カナマイシンキナーゼ (ja)
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foaf:depiction wiki-commons:Special:FilePath/APHActiveSite.png wiki-commons:Special:FilePath/APHNegativeBindinPocket.png wiki-commons:Special:FilePath/APHReactionMechanism.png wiki-commons:Special:FilePath/APHRxnScheme.png wiki-commons:Special:FilePath/APHStructure.png
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