184 Copyright © 1998 Elsevier Science Ltd. All rights reserved. 0962-8924/98/$19.00 trends in CELL BIOLOGY (Vol. 8) May 1998 PII: S0962-8924(98)01248-3 Our current understanding of the dynamics of nuclear import has evolved from the initial identification of the ‘classical nuclear localization signal’ (cNLS), which consists of a short sequence rich in basic amino-acid residues 1 . Transport of proteins bearing this signal into the nucleus is mediated by a karyopherin 1 heterodimeric complex plus additional factors such as the GTPase Ran and its associated protein p10 (NTF2) (reviewed in Refs 2 and 3). The nomenclature for the 1 complex remains confusing, owing to its almost coincident identification by several labora- tories (see Table 1). Here, we use the general term karyopherin [from the Greek terms karyon meaning nucleus and pher(ein) meaning to bring to or to carry from 4 ] for it most accurately describes a family of re- ceptors that are able to recognize substrates, in either (or both) the nucleoplasm or cytoplasm, and assist in their transport into and out of the nucleus. In the prototypical case, the karyopherin subunit of the 1 dimer binds to the cNLS, and the complex then docks at the nuclear pore complex (NPC) in an energy-independent manner through interactions between karyopherin 1 and (at least) cytoplasmically exposed NPC proteins (nucleoporins) containing characteristic peptide repeats. Subsequent translo- cation through the NPC and termination of import require energy and the GTPase Ran (see the accom- panying hypothesis article by Melchior and Gerace). Ran appears to play a crucial role in maintaining vectorial cargo transport and in regulating the bind- ing and release steps that occur during translocation through the NPC. Ran exists in the cell in two forms, either as Ran–GTP or Ran–GDP. Because of the sub- cellular localization of several proteins that alter the nucleotide-bound state of Ran, it is likely that the predominant form of Ran in the cytosol is Ran–GDP, whereas in the nucleus the major form is Ran–GTP. Such a gradient of Ran could establish directional transport by creating separate environments in which transport complexes are either assembled or dis- assembled (reviewed in Refs 5 and 6). Consistent with this idea, the karyopherin 1––cNLS complex is stable in the presence of Ran–GDP (i.e. in the cytosol), whereas Ran–GTP promotes its disassembly and the release of substrate (i.e. in the nucleus). In addition to these more global effects, Ran also acts as a molecular switch at sites within the NPC. Here, it is thought that, in concert with p10 (Ref. 7), conversion of the nucleotide-bound state of Ran modulates interactions between the NPC and 1, and the cNLS-containing cargo in what has been proposed to be a series of association and dissociation reactions that occur as these components step their way through the NPC 8 . While the karyopherin 1 heterodimer is likely to account for the import of cNLS-containing cargo, it has recently been established that an extended family of karyopherin 1-related nuclear transport factors exists. This article describes recent progress in characterizing these proteins. Some members of this family have been shown to be involved directly in transporting specific classes of macromolecules into and out of the nucleus, whereas others have been implicated indirectly in nuclear transport. Karyopherin 2 and mRNP proteins Two very different, but complementary, approaches led to the identification of the first alternative karyo- pherin in both Saccharomyces cerevisiae (Kap104p 9 ) and mammalian cells (transportin 10 ). Because of their similarity to karyopherin 1, here these are generi- cally termed karyopherin 2 11,12 . The mammalian karyopherin 2 (transportin) was identified by its interaction with a 38-amino-acid residue sequence (termed M9) found within the het- erogeneous nuclear ribonuclear protein (hnRNP) A1 (Ref. 10). A1 is a shuttling protein that exits the nucleus bound to mRNA and re-enters the nucleus after it is shed from the mRNA in the cytoplasm 13 . The M9 sequence is sufficient to act as both an NLS and a nuclear export signal (NES) on a reporter pro- tein, and it is thought to be the signal respon- sible for the shuttling activity of A1 14,15 . The nuclear import leg of this journey was shown, in an in vitro assay, to require karyopherin 2 10–12,16 . The import is energy dependent and separate from the cNLS pathway 10–12,16 . 2 also interacts with several other hnRNPs, suggesting that they too are imported by this pathway 17 . Yeast karyopherin 2 was identified by its homol- ogy to 1 (Ref. 9). It is a mainly cytosolic protein that also binds directly to repeat-containing nucleoporins and to a cytosolic pool of at least two major mRNA- binding proteins – Nab2p and Hrp1p (Nab4p) 9 . Inter- estingly, Hrp1p is the closest structural homologue to hnRNP A1 in yeast 18 . Temperature-sensitive mu- tants in 2 cause redistribution of Nab2p from its REVIEWS Karyopherins and kissing cousins Richard W. Wozniak, Michael P. Rout and John D. Aitchison In eukaryotic cells, a regulated flux of molecules between the cytoplasm and the nucleus maintains two very different environments while allowing the controlled exchange of macromolecules necessary for their individual functions. Molecules entering or leaving the nucleus use nuclear localization signals or nuclear export signals to pass through selective channels in the nuclear envelope formed by nuclear pore complexes. The recognition of signal-bearing cargo, its interaction with the nuclear pore complex and its translocation through the pore complex are mediated by soluble transport factors. Recently, the list of potential transport factors has grown rapidly, suggesting a previously unanticipated level of complexity for nuclear transport. Richard Wozniak and John Aitchison are in the Dept of Cell Biology and Anatomy, University of Alberta, Edmonton, Alberta, Canada T6G 2H7; and Michael Rout is at The Rockefeller University, New York, NY 10021, USA. E-mails: rwozniak@anat. med.ualberta.ca rout@rockvax. rockefeller.edu john.aitchison@ ualberta.ca