Disrupting the RNA polymerase II transcription cycle through CDK7 inhibition ameliorates inflammatory arthritis

Sci Transl Med. 2024 Nov 20;16(774):eadq5091. doi: 10.1126/scitranslmed.adq5091. Epub 2024 Nov 20.

Abstract

Macrophages are key drivers of inflammation and tissue damage in autoimmune diseases including rheumatoid arthritis. The rate-limiting step for transcription of more than 70% of inducible genes in macrophages is RNA polymerase II (Pol II) promoter-proximal pause release; however, the specific role of Pol II early elongation control in inflammation, and whether it can be modulated therapeutically, is unknown. Genetic ablation of a pause-stabilizing negative elongation factor (NELF) in macrophages did not affect baseline Pol II occupancy but enhanced the transcriptional response of paused anti-inflammatory genes to lipopolysaccharide followed by secondary attenuation of inflammatory signaling in vitro and in the K/BxN serum transfer mouse model of arthritis. To pharmacologically disrupt the Pol II transcription cycle, we used two covalent inhibitors of the transcription factor II H-associated cyclin-dependent kinase 7 (CDK7), THZ1 and YKL-5-124. Both reduced Pol II pausing in murine and human macrophages, broadly suppressed induction of pro- but not anti-inflammatory genes, and rapidly reversed preestablished inflammatory macrophage polarization. In mice, CDK7 inhibition ameliorated both acute and chronic progressive inflammatory arthritis. Lastly, CDK7 inhibition down-regulated a pathogenic gene expression signature in synovial explants from patients with rheumatoid arthritis. We propose that interfering with Pol II early elongation by targeting CDK7 represents a therapeutic opportunity for rheumatoid arthritis and other inflammatory diseases.

MeSH terms

  • Animals
  • Arthritis / drug therapy
  • Arthritis / metabolism
  • Arthritis / pathology
  • Arthritis, Rheumatoid / drug therapy
  • Arthritis, Rheumatoid / metabolism
  • Arthritis, Rheumatoid / pathology
  • Cyclin-Dependent Kinase-Activating Kinase*
  • Cyclin-Dependent Kinases* / antagonists & inhibitors
  • Cyclin-Dependent Kinases* / metabolism
  • Humans
  • Inflammation* / pathology
  • Lipopolysaccharides
  • Macrophages* / drug effects
  • Macrophages* / metabolism
  • Mice
  • Mice, Inbred C57BL
  • Phenylenediamines / pharmacology
  • Phenylenediamines / therapeutic use
  • Protein Kinase Inhibitors / pharmacology
  • Protein Kinase Inhibitors / therapeutic use
  • Pyrimidines / pharmacology
  • Pyrimidines / therapeutic use
  • RNA Polymerase II* / metabolism
  • Transcription Factors
  • Transcription, Genetic* / drug effects

Substances

  • RNA Polymerase II
  • Cyclin-Dependent Kinase-Activating Kinase
  • Cyclin-Dependent Kinases
  • Phenylenediamines
  • negative elongation factor
  • THZ1 compound
  • Pyrimidines
  • Lipopolysaccharides
  • Protein Kinase Inhibitors
  • Transcription Factors