Estévez R, Camps M, Rojas A M, Testar X, Devés R, Hediger M A, Zorzano A, Palacín M
Department of Biochemistry and Molecular Biology, Faculty of Biology, University of Barcelona, Barcelona-08028,
FASEB J. 1998 Oct;12(13):1319-29. doi: 10.1096/fasebj.12.13.1319.
4F2hc is an almost ubiquitous transmembrane protein in mammalian cells; upon expression in Xenopus laevis oocytes, it induces amino acid transport with characteristics of system y+L. Indirect evidence fostered speculation that function requires the association of 4F2hc with another protein endogenous to oocytes and native tissues. We show that expression of system y+L-like amino acid transport activity by 4F2hc in oocytes is limited by an endogenous factor and that direct covalent modification of external cysteine residue(s) of an oocyte membrane protein blocks system y+L/4F2hc transport activity, based on the following. 1) Induction of system y+L-like activity saturates at very low doses of human 4F2hc cRNA (0.1 ng/oocyte). This saturation occurs with very low expression of 4F2hc at the oocyte surface, and further increased expression of the protein at the cell surface does not result in higher induction of system y+L-like activity. 2) Human 4F2hc contains only two cysteine residues (C109 and C330). We mutated these residues, singly and in combination, to serine (C109S; CS1, C330S; CS2 and C109S-C330S, Cys-less). Mutation CS2 had no effect on the expressed system y+L-like transport activity, whereas C109S-containing mutants (CS1 and Cys-less) retained only partial y+L-like transport activity (30 to 50% of wild type). 3) Hg2+, the organic mercury compounds pCMB, and the membrane-impermeant pCMBS almost completely inactivated system y+L-like induced by human 4F2hc wild type and all the mutants studied. This was reversed by ss-mercaptoethanol, indicating that external cysteine residue(s) are the target of this inactivation. 4) Sensitivity to Hg2+ inactivation is increased by pretreatment of oocytes with ss-mercaptoethanol or in the C109S-containing mutants (CS1 and Cys-less). The increased Hg2+ reactivity of C109S-containing mutants supports the possibility that C109 may be linked by a disulfide bond to the Hg2+-targeted cysteine residue of the associated protein. These results indicate that 4F2hc is intimately associated with a membrane oocyte protein for the expression of system y+L amino acid transport activity. To our knowledge, this is the first direct evidence for a heteromultimeric protein structure of an organic solute carrier in mammals.
4F2hc是一种在哺乳动物细胞中几乎普遍存在的跨膜蛋白;在非洲爪蟾卵母细胞中表达时,它能诱导出具有y+L系统特征的氨基酸转运。间接证据促使人们推测,其功能需要4F2hc与卵母细胞和天然组织中的另一种内源性蛋白结合。我们发现,4F2hc在卵母细胞中表达的y+L系统样氨基酸转运活性受到一种内源性因子的限制,并且基于以下几点,对卵母细胞膜蛋白外部半胱氨酸残基的直接共价修饰会阻断y+L系统/4F2hc转运活性。1)y+L系统样活性的诱导在极低剂量的人4F2hc cRNA(0.1 ng/卵母细胞)时就达到饱和。这种饱和在卵母细胞表面4F2hc表达非常低的情况下就会出现,并且细胞表面该蛋白表达的进一步增加并不会导致y+L系统样活性的更高诱导。2)人4F2hc仅含有两个半胱氨酸残基(C109和C330)。我们将这些残基单独或组合突变为丝氨酸(C109S;CS1,C330S;CS2以及C109S - C330S,无半胱氨酸)。突变体CS2对表达的y+L系统样转运活性没有影响,而含C109S的突变体(CS1和无半胱氨酸)仅保留了部分y+L样转运活性(野生型的30%至50%)。3)Hg2+、有机汞化合物pCMB以及不能透过膜的pCMBS几乎完全使由人4F2hc野生型和所有研究的突变体诱导的y+L系统样活性失活。这可被β-巯基乙醇逆转,表明外部半胱氨酸残基是这种失活的靶点。4)用β-巯基乙醇预处理卵母细胞或在含C109S的突变体(CS1和无半胱氨酸)中,对Hg2+失活的敏感性会增加。含C109S的突变体对Hg2+反应性的增加支持了C109可能通过二硫键与相关蛋白的Hg2+靶向半胱氨酸残基相连的可能性。这些结果表明,4F2hc与一种卵母细胞膜蛋白密切相关,以表达y+L系统氨基酸转运活性。据我们所知,这是哺乳动物中有机溶质载体异源多聚体蛋白结构的首个直接证据。