P-glikoprotein

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ATP-vezujuća kaseta, potfamilija B (MDR/TAP), član 1

Kristalografska struktura MDR3 proteina miša. Aproksimativna pozicija proteina u ćelijskoj membrani je obeležena plavim (ekstracelularno lice) i crvenim (citoplazmatično lice) linijama. Protein je prikaza u bojama duge (N-terminus = plavo, C-terminus = crveno). Ciklični peptidni inhibitor QZ59 je prikazan kao prostorno popunjavajući model.[1]
Dostupne strukture
3G5U, 3G60, 3G61
Identifikatori
SimboliABCB1; ABC20; CD243; CLCS; GP170; MDR1; P-GP; PGY1
Vanjski IDOMIM171050 MGI97570 HomoloGene55496 GeneCards: ABCB1 Gene
EC broj3.6.3.44
Pregled RNK izražavanja
podaci
Ortolozi
VrstaČovekMiš
Entrez524318671
EnsemblENSG00000085563ENSMUSG00000040584
UniProtP08183P21447
RefSeq (mRNA)NM_000927.4NM_011076.2
RefSeq (protein)NP_000918.2NP_035206.2
Lokacija (UCSC)Chr 7:
87.13 - 87.34 Mb
Chr 5:
8.66 - 8.75 Mb
PubMed pretraga[1][2]

P-glikoprotein 1 (glikoprotein permeabilnosti, P-gp, Pgp, protein otpornosti na višestruke lekove 1, MDR1, ATP-vezujuća kaseta potfamilija B član 1, ABCB1, klaster of diferencijacije 243, CD243) je glikoprotein koji je kod ljudi kodiran ABCB1 genom.[2] P-gp dobro poznati ABC-transporter (koji transportuje široki opseg supstrata kroz ekstra- i intracelularne membrane). On je član MDR/TAP familije.[3]

Pgp je široko rasprostranjen i izražen u interstinalnom epitelu, hepatocitima, renalno proksimalno tubularnim ćelijama, nadbubrežnoj žlezdi i kapilarnim endotelnim ćelijama od kojih je formirana krvno-moždana i krvno-testikularna barijera.

Reference[uredi | uredi kod]

  1. PDB 3G60; Aller SG, Yu J, Ward A, Weng Y, Chittaboina S, Zhuo R, Harrell PM, Trinh YT, Zhang Q, Urbatsch IL, Chang G (March 2009). „Structure of P-glycoprotein reveals a molecular basis for poly-specific drug binding”. Science 323 (5922): 1718–22. DOI:10.1126/science.1168750. PMC 2720052. PMID 19325113. 
  2. Ueda K, Clark DP, Chen CJ, Roninson IB, Michael M. Gottesman, Pastan I (January 1987). „The human multidrug resistance (mdr1) gene. cDNA cloning and transcription initiation”. J. Biol. Chem. 262 (2): 505–8. PMID 3027054. Arhivirano iz originala na datum 2008-07-26. Pristupljeno 2014-05-27. 
  3. Dean, Michael (1. 11. 2002.). „The Human ATP-Binding Cassette (ABC) Transporter Superfamily”. National Library of Medicine (US), NCBI. Pristupljeno 2. 3. 2008. 

Literatura[uredi | uredi kod]

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  • Akiyama S (2002). „[Mechanisms of drug resistance and reversal of the resistance]”. Hum. Cell 14 (4): 257–60. PMID 11925925. 
  • Brinkmann U (2002). „Functional polymorphisms of the human multidrug resistance (MDR1) gene: correlation with P glycoprotein expression and activity in vivo”. Novartis Found. Symp.. Novartis Foundation Symposia 243: 207–10; discussion 210–2, 231–5. DOI:10.1002/0470846356.ch15. ISBN 978-0-470-84635-3. PMID 11990778. 
  • Váradi A, Szakács G, Bakos E, Sarkadi B (2002). „P glycoprotein and the mechanism of multidrug resistance”. Novartis Found. Symp.. Novartis Foundation Symposia 243: 54–65; discussion 65–8, 180–5. DOI:10.1002/0470846356.ch5. ISBN 978-0-470-84635-3. PMID 11990782. 
  • Hegedus T, Orfi L, Seprodi A, et al. (2002). „Interaction of tyrosine kinase inhibitors with the human multidrug transporter proteins, MDR1 and MRP1”. Biochim. Biophys. Acta 1587 (2–3): 318–25. PMID 12084474. 
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  • Ambudkar SV, Kimchi-Sarfaty C, Sauna ZE, Michael M. Gottesman (2003). „P-glycoprotein: from genomics to mechanism”. Oncogene 22 (47): 7468–85. DOI:10.1038/sj.onc.1206948. PMID 14576852. 
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  • Ishikawa T, Onishi Y, Hirano H, et al. (2005). „Pharmacogenomics of drug transporters: a new approach to functional analysis of the genetic polymorphisms of ABCB1 (P-glycoprotein/MDR1)”. Biol. Pharm. Bull. 27 (7): 939–48. DOI:10.1248/bpb.27.939. PMID 15256718. 
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  • Orlowski S, Martin S, Escargueil A (2006). „P-glycoprotein and 'lipid rafts': some ambiguous mutual relationships (floating on them, building them or meeting them by chance?)”. Cell. Mol. Life Sci. 63 (9): 1038–59. DOI:10.1007/s00018-005-5554-9. PMID 16721513. 
  • Annese V, Valvano MR, Palmieri O, et al. (2006). „Multidrug resistance 1 gene in inflammatory bowel disease: a meta-analysis”. World J. Gastroenterol. 12 (23): 3636–44. PMID 16773678. 
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  • Kumar YS, Adukondalu D, Sathish D, Vishnu YV, Ramesh G, Latha AB, Reddy PC, Sarangapani M, Rao YM (2010). „P-Glycoprotein- and cytochrome P-450-mediated herbal drug interactions”. Drug Metabol Drug Interact 25 (1-4): 3–16. DOI:10.1515/DMDI.2010.006. PMID 21417789. 

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