P2X7 Receptor Mediated Increase In Cell Membrane Permeability

Year 2018, Volume: 71 Issue: 1, 31 - 34, 16.10.2018

Kemal Sayar

Abstract

Purinergic receptors consist of two main families; P2X and P2Y. P2Y receptors are G protein coupled receptors (GPCR), whereas P2X receptors are non-selective cation channels. P2X7 receptors which is a member of P2X receptors, have been found myriad types of cells including immune cells. The activation of this receptor leads to IL-1β release and caspase activation as well as an increase in membranepermeability to big molecules. Spectroscopic and electrophysiologic methods have been used to investigate membrane permeability. Different hypotheses have been proposed as an explanation for big permeability. One of them proposes that P2X7 channel itself dilates and becomes permeable to big molecules, whereas the other proposes participation of another channels to big permeability. Since it has been demonstrated that P2X7 receptor has a role in many disease processes including inflamation, pain, cancer and Alzheimer’s disease, its antagonists and modulators have been regarded as a good drug target. The uncovering of its activation mechanism is important for treatment of many diseases.

Keywords

P2X7 Receptor , Membrane Permeability , YoPro-1 , Lucifer Yellow

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P2X7 Reseptörü Aracılı Hücre Membran Geçirgenlik Artıșı

Abstract

Pürinerjik reseptörler P2X ve P2Y olmak üzere iki ana aileden olușmaktadır. P2Y reseptörleri G-proteini kenetli reseptörler (GPKR), P2X reseptörleri seçici olmayan katyon kanallarıdır. P2X reseptörlerinin 7 üyesinden biri olan P2X7 reseptörü immün hücreler bașta olmak üzere birçok tip hücrede bulunmaktadır. IL-1β salınımı, kaspaz aktivasyonu gibi hücre içinde birçok sinyal yolağını aktive etmekle beraber, diğer üyelerden farklı olarak membranda büyük bir geçirgenlik aktive etmektedir. Membran geçirgenliğini incelemek için spektroskopik ve elektrofizyolojik yöntemler kullanılmaktadır. Büyük geçirgenliğin mekanizmasını açıklamak için çeșitli hipotezler öne sürülmektedir. Bunlardan biri P2X7 kanalının genișleyerek büyük moleküllere geçirgen hale geldiği, diğeri ise geçirgenliğin bașka bir protein aracılığıyla olduğudur. P2X7 reseptörü inflamasyon, ağrı, kanser ve Alzhzeimer gibi birçok hastalıkta rolü olduğu gösterilen bir reseptör olduğu için antagonistleri ve modülatörleri iyi birer ilaç hedefi olarak görülmektedir. Aktivasyon mekanizmasının aydınlatılması da birçok hastalığın tedavisi için önem tașımaktadır.

Keywords

P2X7 Reseptörü , Membran Geçirgenliği , YoPro-1 , Lusifer Yellow

Ethical Statement

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Supporting Institution

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Project Number

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Thanks

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