Small molecule inhibitors targeting activator protein 1 (AP-1)

Na Ye, Ye Ding, Christopher Wild, Qiang Shen, Jia Zhou

Research output: Contribution to journalArticle

52 Citations (Scopus)

Abstract

Activator protein 1 (AP-1) is a pivotal transcription factor that regulates a wide range of cellular processes including proliferation, apoptosis, differentiation, survival, cell migration, and transformation. Accumulating evidence supports that AP-1 plays an important role in several severe disorders including cancer, fibrosis, and organ injury, as well as inflammatory disorders such as asthma, psoriasis, and rheumatoid arthritis. AP-1 has emerged as an actively pursued drug discovery target over the past decade. Excitingly, a selective AP-1 inhibitor T-5224 (51) has been investigated in phase II human clinical trials. Nevertheless, no effective AP-1 inhibitors have yet been approved for clinical use. Despite significant advances achieved in understanding AP-1 biology and function, as well as the identification of small molecules modulating AP-1 associated signaling pathways, medicinal chemistry efforts remain an urgent need to yield selective and efficacious AP-1 inhibitors as a viable therapeutic strategy for human diseases.

Original languageEnglish (US)
Pages (from-to)6930-6948
Number of pages19
JournalJournal of Medicinal Chemistry
Volume57
Issue number16
DOIs
StatePublished - 2014

Fingerprint

Transcription Factor AP-1
Phase II Clinical Trials
Pharmaceutical Chemistry
Drug Discovery
Psoriasis
Cell Movement
Rheumatoid Arthritis
Fibrosis
Transcription Factors
Asthma
Apoptosis
Survival
Wounds and Injuries

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

Cite this

Small molecule inhibitors targeting activator protein 1 (AP-1). / Ye, Na; Ding, Ye; Wild, Christopher; Shen, Qiang; Zhou, Jia.

In: Journal of Medicinal Chemistry, Vol. 57, No. 16, 2014, p. 6930-6948.

Research output: Contribution to journalArticle

Ye, Na ; Ding, Ye ; Wild, Christopher ; Shen, Qiang ; Zhou, Jia. / Small molecule inhibitors targeting activator protein 1 (AP-1). In: Journal of Medicinal Chemistry. 2014 ; Vol. 57, No. 16. pp. 6930-6948.
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