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UK-18,892：对氨基糖苷类失活酶修饰具有抗性。

UK-18,892: resistance to modification by aminoglycoside-inactivating enzymes.

作者信息

Andrews R J, Brammer K W, Cheeseman H E, Jevons S

出版信息

Antimicrob Agents Chemother. 1978 Dec;14(6):846-50. doi: 10.1128/AAC.14.6.846.

DOI:10.1128/AAC.14.6.846
PMID:742872
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC352568/
Abstract

UK-18,892, a new semisynthetic aminoglycoside, was active against bacteria possessing aminoglycoside-inactivating enzymes, with the exception of some known to possess AAC(6') or AAD(4') enzymes. This activity has been rationalized by using cell-free extracts of bacteria containing known inactivating enzymes, where it was shown that UK-18,892 was not a substrate for the APH(3'), AAD(2''), AAC(3), and AAC(2') enzymes. It was also demonstrated that UK-18,892 protected mice against lethal infections caused by organisms possessing aminoglycoside-inactivating enzymes.

摘要

UK-18892是一种新型半合成氨基糖苷类药物，对具有氨基糖苷类失活酶的细菌具有活性，但已知具有AAC(6')或AAD(4')酶的细菌除外。通过使用含有已知失活酶的细菌无细胞提取物，对这种活性进行了合理的解释，结果表明UK-18892不是APH(3')、AAD(2'')、AAC(3)和AAC(2')酶的底物。还证明了UK-18892能保护小鼠免受具有氨基糖苷类失活酶的生物体引起的致命感染。

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1
UK-18,892: resistance to modification by aminoglycoside-inactivating enzymes.UK-18,892：对氨基糖苷类失活酶修饰具有抗性。
Antimicrob Agents Chemother. 1978 Dec;14(6):846-50. doi: 10.1128/AAC.14.6.846.
2
In vitro studies with UK-18,892, a new aminoglycoside antibiotic.使用新型氨基糖苷类抗生素UK-18,892进行的体外研究。
Antimicrob Agents Chemother. 1978 Sep;14(3):277-80. doi: 10.1128/AAC.14.3.277.
3
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引用本文的文献

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Aminoglycoside research 1975-1985: prospects for development of improved agents.1975 - 1985年氨基糖苷类药物研究：改进型药物的开发前景
Antimicrob Agents Chemother. 1986 Apr;29(4):543-8. doi: 10.1128/AAC.29.4.543.

本文引用的文献

1
R-factor mediated gentamicin resistance: A new enzyme which modifies aminoglycoside antibiotics.R 因子介导的庆大霉素耐药性：一种修饰氨基糖苷类抗生素的新酶。
FEBS Lett. 1971 May 20;14(5):293-296. doi: 10.1016/0014-5793(71)80282-x.
2
Enzymatic acetylation of aminoglycoside antibiotics by Escherichia coli carrying an R factor.携带R因子的大肠杆菌对氨基糖苷类抗生素的酶促乙酰化作用。
Biochemistry. 1971 May 11;10(10):1787-96. doi: 10.1021/bi00786a009.
3
Aminoglycoside antibiotics: inactivation by phosphorylation in Escherichia coli carrying R factors.氨基糖苷类抗生素：在携带R因子的大肠杆菌中通过磷酸化作用而失活
J Bacteriol. 1969 Nov;100(2):1144-6. doi: 10.1128/jb.100.2.1144-1146.1969.
4
Aminoglycoside resistance in bacteria medicated by gentamicin acetyltransferase II, an enzyme modifying the 2'-amino group of aminoglycoside antibiotics.由庆大霉素乙酰转移酶II介导的细菌对氨基糖苷类抗生素的耐药性，该酶可修饰氨基糖苷类抗生素的2'-氨基基团。
Biochemistry. 1974 Jan 29;13(3):598-603. doi: 10.1021/bi00700a030.
5
Mechanisms of antibiotic resistance in bacteria.细菌中的抗生素耐药机制。
Annu Rev Biochem. 1973;42:471-506. doi: 10.1146/annurev.bi.42.070173.002351.
6
Activity of BB-K8 (amikacin) against clinical isolates resistant to one or more aminoglycoside antibiotics.BB-K8（阿米卡星）对耐一种或多种氨基糖苷类抗生素的临床分离株的活性。
Antimicrob Agents Chemother. 1974 Feb;5(2):143-52. doi: 10.1128/AAC.5.2.143.
7
Improved acetylating radioenzymatic assay of amikacin, tobramycin, and sisomicin in serum.血清中阿米卡星、妥布霉素和西索米星的改进乙酰化放射酶法测定
Antimicrob Agents Chemother. 1975 Mar;7(3):374-6. doi: 10.1128/AAC.7.3.374.
8
New plasmid-mediated nucleotidylation of aminoglycoside antibiotics in Staphlococcus aureus.金黄色葡萄球菌中氨基糖苷类抗生素新的质粒介导的核苷酸化作用
Antimicrob Agents Chemother. 1976 Aug;10(2):258-64. doi: 10.1128/AAC.10.2.258.
9
Synthesis and antibacterial activities of 1-N [(S)-omega-amino-2-hydroxyalkyl] kanamycin A derivatives.
J Antibiot (Tokyo). 1977 Oct;30(10):843-6. doi: 10.7164/antibiotics.30.843.
10
Aminoglycoside-modifying enzymes.氨基糖苷类修饰酶
Methods Enzymol. 1975;43:611-28. doi: 10.1016/0076-6879(75)43124-x.