GABA cloning

Figure 11.4 Blockers of GABA transport.The upper panel shows the structure of several GABA analogues that inhibit GABA transport into neurons or glia (see text). The lower panels show more recently developed compounds that exhibit selectivity for various cloned GABA transporters...

Cutting, GR, Lu, L, O Hara, BF, Kasch, LM, Montrose-Rafizadeh, C, Donovan, DM, Shimada, S, Antonarakis, SE, Guggino, WB, Uhl, GR et al. (1991) Cloning of the y-aminobutyric acid (GABA) rho 1 cDNA a GABA receptor subunit highly expressed in the retina. Proc. Natl. Acad. Sci. USA 88 2673-2677. 

The GABAb receptor is not a single 7TM receptor but rather a heterodimer formed by two 7TM receptors from family C. The GABAb-R1 receptor, which was initially cloned, binds the ligand GABA, but when expressed alone it is to a large extent retained in the endoplasmic reticulum,... 

GABAb receptors are heterodimers. Two GABAb receptor subunits have been cloned, R1 and R2. Neither of these appears to express functional receptors on their own, but they are active when coexpressed, suggesting that a dimer is trafficked to the cell surface and forms an active complex. Evidence shows that the R1 subunit contains the GABA binding site while the R2 subunit interacts with the G protein [14]. 

Mager, S Naeve, J., Quick, M., Labarca, C., Davidson, N., and Lester, H. A. (1993) Steady states, charge movements, and rates for a cloned GABA transporter expressed in Xenopus oocytes. Neuron 10,177-188. 

Common Nomenclature Used for Cloned GABA Transporters From Human, Rat, and Mouse... 

This, together with the previous demonstration that SNAP-5114 has higher affinity for GAT4 than for the other cloned transporters (44), shows that lipophilic, bulky molecules that do not contain a strict GABA mimetic moiety can be used to distinguish between the different cloned GABA transporters. 

Sarup, A., Larsson, O. M., Bolvig, T., Frplund, B Krogsgaard-Larsen, P., and Schousboe, A. (2003) Effects of 3-hydroxy-4-amino-4,5,6,7-tetrahydro-l,2-benzisoxazol (exoTHPO) and its N-substituted analogs on GABA transport in cultured neurons and astrocytes and by the four cloned mouse GABA transporters. Neurochem. Int. 43,445 151. 

Nelson, H., Mandiyan, S., and Nelson, N. (1990) Cloning of the human brain GABA transporter. FEBSLett. 269,181-184. 

Borden, L. A., Dhar, T. G., Smith, K. E Branchek, T. A., Gluchowski, C., and Wein-shank, R. L. (1994) Cloning of the human homologue of the GABA transporter GAT-3 and identification of a novel inhibitor with selectivity for this site. Receptors Charm. 2, 207-213. 

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