Binding of the 7SK snRNA turns the HEXIM1 protein into a P-TEFb (CDK9/cyclin T) inhibitor

EMBO J. 2004 Jul 7;23(13):2608-19. doi: 10.1038/sj.emboj.7600275. Epub 2004 Jun 17.

Abstract

The positive transcription elongation factor b (P-TEFb) plays a pivotal role in productive elongation of nascent RNA molecules by RNA polymerase II. Core active P-TEFb is composed of CDK9 and cyclin T. In addition, mammalian cell extracts contain an inactive P-TEFb complex composed of four components, CDK9, cyclin T, the 7SK snRNA and the MAQ1/HEXIM1 protein. We now report an in vitro reconstitution of 7SK-dependent HEXIM1 association to purified P-TEFb and subsequent CDK9 inhibition. Yeast three-hybrid tests and gel-shift assays indicated that HEXIM1 binds 7SK snRNA directly and a 7SK snRNA-recognition motif was identified in the central part of HEXIM1 (amino acids (aa) 152-155). Data from yeast two-hybrid and pull-down assay on GST fusion proteins converge to a direct binding of P-TEFb to the HEXIM1 C-terminal domain (aa 181-359). Consistently, point mutations in an evolutionarily conserved motif (aa 202-205) were found to suppress P-TEFb binding and inhibition without affecting 7SK recognition. We propose that the RNA-binding domain of HEXIM1 mediates its association with 7SK and that P-TEFb then enters the complex through association with HEXIM1.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Amino Acid Motifs
  • Amino Acid Sequence
  • Cyclin T
  • Cyclin-Dependent Kinase 9 / metabolism*
  • Cyclins / metabolism*
  • Electrophoretic Mobility Shift Assay
  • Escherichia coli / genetics
  • Glutathione Transferase / metabolism
  • HeLa Cells
  • Humans
  • Models, Biological
  • Molecular Sequence Data
  • Mutation
  • Positive Transcriptional Elongation Factor B / antagonists & inhibitors
  • Positive Transcriptional Elongation Factor B / genetics
  • Positive Transcriptional Elongation Factor B / metabolism*
  • Precipitin Tests
  • Protein Structure, Tertiary
  • RNA, Small Nuclear / metabolism*
  • RNA-Binding Proteins / chemistry
  • RNA-Binding Proteins / genetics
  • RNA-Binding Proteins / isolation & purification
  • RNA-Binding Proteins / metabolism*
  • Recombinant Fusion Proteins / chemistry
  • Recombinant Fusion Proteins / isolation & purification
  • Recombinant Fusion Proteins / metabolism
  • Transcription Factors
  • Two-Hybrid System Techniques

Substances

  • CCNT1 protein, human
  • Cyclin T
  • Cyclins
  • HEXIM1 protein, human
  • RNA, Small Nuclear
  • RNA-Binding Proteins
  • Recombinant Fusion Proteins
  • Transcription Factors
  • Glutathione Transferase
  • Positive Transcriptional Elongation Factor B
  • Cyclin-Dependent Kinase 9