Exploring the gating mechanisms of aquaporin-3: new clues for the design of inhibitors?

被引：27

作者：

de Almeida, A. ^{[1
]}

Martins, A. P. ^{[2
,3
]}

Mosca, A. F. ^{[2
,3
]}

Wijma, H. J. ^{[4
]}

Prista, C. ^{[5
]}

Soveral, G. ^{[2
,3
]}

Casini, A. ^{[1
,6
]}

机构：

[1] Univ Groningen, Groningen Res Inst Pharm, Dept Pharmacokinet Toxicol & Targeting, A Deusinglaan 1, NL-9713 AV Groningen, Netherlands

[2] Univ Lisbon, Fac Pharm, Res Inst Med IMed ULisboa, P-1649003 Lisbon, Portugal

[3] Univ Lisbon, Fac Pharm, Dept Bioquim & Biol Humana, P-1649003 Lisbon, Portugal

[4] Univ Groningen, Dept Biochem, Groningen Biomol Sci & Biotechnol Inst, Nijenborgh 4, NL-9747 AG Groningen, Netherlands

[5] Univ Lisbon, Inst Super Agron, Res Ctr Linking Landscape Environm Agr & Food LEA, P-1349017 Lisbon, Portugal

[6] Cardiff Univ, Sch Chem, Main Bldg,Pk Pl, Cardiff CF10 3AT, S Glam, Wales

来源：

MOLECULAR BIOSYSTEMS | 2016年 / 12卷 / 05期

关键词：

WATER PERMEABILITY; GLYCEROL; CHANNEL; PH; TRANSPORT; YEAST;

D O I：

10.1039/c6mb00013d

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The pH gating of human AQP3 and its effects on both water and glycerol permeabilities have been fully characterized for the first time using a human red blood cell model (hRBC). For comparison, the effects of pH on the gating of rat AQP3 have also been characterized in yeast. The obtained results highlight similarities as well as differences between the two isoforms. In addition, we investigated the molecular mechanism of hAQP3 pH gating in silico, which may disclose new pathways to AQP regulation by small molecule inhibitors, and therefore may be important for drug development.

引用

页码：1564 / 1573

页数：10

共 50 条

[1] Yeast reveals unexpected roles and regulatory features of aquaporins and aquaglyceroporins [J].