Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTTI53X)

• DTT Name: Kruppel like factor 4 (KLF4)
• Synonyms: Krueppellike factor 4; Krueppel-like factor 4; Gutenriched krueppellike factor; Gut-enriched krueppel-like factor; GKLF; Epithelial zinc finger protein EZF; EZF
• Gene Name: KLF4
• DTT Type: Clinical trial target; [1]
• UniProt ID: KLF4_HUMAN
• TTD ID: T81916
• Sequence:
  MRQPPGESDMAVSDALLPSFSTFASGPAGREKTLRQAGAPNNRWREELSHMKRLPPVLPG
  RPYDLAAATVATDLESGGAGAACGGSNLAPLPRRETEEFNDLLDLDFILSNSLTHPPESV
  AATVSSSASASSSSSPSSSGPASAPSTCSFTYPIRAGNDPGVAPGGTGGGLLYGRESAPP
  PTAPFNLADINDVSPSGGFVAELLRPELDPVYIPPQQPQPPGGGLMGKFVLKASLSAPGS
  EYGSPSVISVSKGSPDGSHPVVVAPYNGGPPRTCPKIKQEAVSSCTHLGAGPPLSNGHRP
  AAHDFPLGRQLPSRTTPTLGLEEVLSSRDCHPALPLPPGFHPHPGPNYPSFLPDQMQPQV
  PPLHYQGQSRGFVARAGEPCVCWPHFGTHGMMLTPPSSPLELMPPGSCMPEEPKPKRGRR
  SWPRKRTATHTCDYAGCGKTYTKSSHLKAHLRTHTGEKPYHCDWDGCGWKFARSDELTRH
  YRKHTGHRPFQCQKCDRAFSRSDHLALHMKRHF
• Function: Binds the 5'-CACCC-3' core sequence. Binds to the promoter region of its own gene and can activate its own transcription. Regulates the expression of key transcription factors during embryonic development. Plays an important role in maintaining embryonic stem cells, and in preventing their differentiation. Required for establishing the barrier function of the skin and for postnatal maturation and maintenance of the ocular surface. Involved in the differentiation of epithelial cells and may also function in skeletal and kidney development. Contributes to the down-regulation of p53/TP53 transcription. Transcription factor; can act both as activator and as repressor.
• KEGG Pathway: Signaling pathways regulating pluripotency of stem cells (hsa04550)
• Reactome Pathway:
  Transcriptional regulation of pluripotent stem cells (R-HSA-452723)
  Transcriptional regulation of white adipocyte differentiation (R-HSA-381340)

Molecular Interaction Atlas (MIA) of This DTT

1 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
APTO-253	DMXIKYR	Solid tumour/cancer	2A00-2F9Z	Phase 1	[1]

References

• [1] Phase 1 study of APTO-253 HCl, an inducer of KLF4, in patients with advanced or metastatic solid tumors. Invest New Drugs. 2015 Oct;33(5):1086-92.