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Apramicin

Izvor: Wikipedija

Apramicin
(IUPAC) ime
(2R,3R,4R,5S,6R)-5-amino-2- [((1R,2R,3R,4R,6R,8R)-8-amino-9- [(1R,2S,3R,4R,6R)-4,6-diamino-2,3- dihidroksi-cikloheksil]oksi-2-hidroksi- 3-metilamino-5,10- dioksabiciklo[4.4.0]dec-4-il)oksi]-6- (hidroksimetil)oksan-3,4-diol
Klinički podaci
AHFS/Drugs.com Internacionalno ime leka
Identifikatori
CAS broj 37321-09-8
ATCvet kod QA07AA92 QJ01GB90 QJ51GB90
PubChem[1][2] 3081545
DrugBank DB04626
ChemSpider[3] 2339128
UNII 388K3TR36Z DaY
KEGG[4] D02322 DaY
ChEBI CHEBI:2790 DaY
ChEMBL[5] CHEMBL1230961 DaY
Hemijski podaci
Formula C21H41N5O11 
Mol. masa 539,58 g/mol
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća ?
Pravni status

Apramicin (Nebramicin II) je aminoglikozidni antibiotik koji se koristi u veterini. Njega proizvodi Streptomyces tenebrarius.[6]

Mehanizam dejstva

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Apramicin je jedistven među aminoglikozidima po svom mehanizmu dejstva koji je baziran na blokiranju translokacije, i njegovoj sposobnosti vezivanja i za eukariotska mesta dekodiranja uprkos razlika u ključnim aminokiselinskim ostacima neophodnim za prepoznavanje bakterijke mete. Lek se vezuje duboko u žlebu RNK čime se formira kontinuirano naslagani heliks koji se sastoji od nekanoničkih C.A i G.A baznih parova i iskrivljenog adenina. Mod vezivanja apramicina na ljudskom mestu dekodiranja RNK se razlikuje od načina prepoznavanja aminoglikozida u bakterijskoj meti.

Reference

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  1. Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519.  edit
  2. Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1. 
  3. Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846.  edit
  4. Joanne Wixon, Douglas Kell (2000). „Website Review: The Kyoto Encyclopedia of Genes and Genomes — KEGG”. Yeast 17 (1): 48–55. DOI:10.1002/(SICI)1097-0061(200004)17:1<48::AID-YEA2>3.0.CO;2-H. 
  5. Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). „ChEMBL: a large-scale bioactivity database for drug discovery”. Nucleic Acids Res 40 (Database issue): D1100-7. DOI:10.1093/nar/gkr777. PMID 21948594.  edit
  6. Ryden, R; Moore (1977). „BJ”. J Antimicrob Chemother 3 (6): 609–613. DOI:10.1093/jac/3.6.609. PMID 340441. 
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Apramicin
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