Details of the Drug Therapeutic Target (DTT)

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

• DTT Name: E2F transcription factor 1 (E2F1)
• Synonyms: pRB-binding protein E2F-1; Transcription factor E2F1; Retinoblastoma-binding protein 3; Retinoblastoma-associated protein 1; RBBP3; RBBP-3; RBAP-1; PBR3; E2F-1
• Gene Name: E2F1
• DTT Type: Clinical trial target; [1]
• UniProt ID: E2F1_HUMAN
• TTD ID: T57059
• Sequence:
  MALAGAPAGGPCAPALEALLGAGALRLLDSSQIVIISAAQDASAPPAPTGPAAPAAGPCD
  PDLLLFATPQAPRPTPSAPRPALGRPPVKRRLDLETDHQYLAESSGPARGRGRHPGKGVK
  SPGEKSRYETSLNLTTKRFLELLSHSADGVVDLNWAAEVLKVQKRRIYDITNVLEGIQLI
  AKKSKNHIQWLGSHTTVGVGGRLEGLTQDLRQLQESEQQLDHLMNICTTQLRLLSEDTDS
  QRLAYVTCQDLRSIADPAEQMVMVIKAPPETQLQAVDSSENFQISLKSKQGPIDVFLCPE
  ETVGGISPGKTPSQEVTSEEENRATDSATIVSPPPSSPPSSLTTDPSQSLLSLEQEPLLS
  RMGSLRAPVDEDRLSPLVAADSLLEHVREDFSGLLPEEFISLSPPHEALDYHFGLEEGEG
  IRDLFDCDFGDLTPLDF
• Function: The DRTF1/E2F complex functions in the control of cell-cycle progression from G1 to S phase. E2F1 binds preferentially RB1 in a cell-cycle dependent manner. It can mediate both cell proliferation and TP53/p53-dependent apoptosis. Blocks adipocyte differentiation by binding to specific promoters repressing CEBPA binding to its target gene promoters. Positively regulates transcription of RRP1B. Transcription activator that binds DNA cooperatively with DP proteins through the E2 recognition site, 5'-TTTC[CG]CGC-3' found in the promoter region of a number of genes whose products are involved in cell cycle regulation or in DNA replication.
• KEGG Pathway:
  Cell cycle (hsa04110)
  Hepatitis B (hsa05161)
  HTLV-I infection (hsa05166)
  Pathways in cancer (hsa05200)
  MicroRNAs in cancer (hsa05206)
  Pancreatic cancer (hsa05212)
  Glioma (hsa05214)
  Prostate cancer (hsa05215)
  Melanoma (hsa05218)
  Bladder cancer (hsa05219)
  Chronic myeloid leukemia (hsa05220)
  Small cell lung cancer (hsa05222)
  Non-small cell lung cancer (hsa05223)
• Reactome Pathway:
  E2F mediated regulation of DNA replication (R-HSA-113510)
  Activation of PUMA and translocation to mitochondria (R-HSA-139915)
  G0 and Early G1 (R-HSA-1538133)
  Pre-NOTCH Transcription and Translation (R-HSA-1912408)
  Oxidative Stress Induced Senescence (R-HSA-2559580)
  Oncogene Induced Senescence (R-HSA-2559585)
  CDC6 association with the ORC (R-HSA-68689)
  G2 Phase (R-HSA-68911)
  G1/S-Specific Transcription (R-HSA-69205)
  Cyclin D associated events in G1 (R-HSA-69231)
  Association of licensing factors with the pre-replicative complex (R-HSA-69298)
  Activation of NOXA and translocation to mitochondria (R-HSA-111448)

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
ARQ-171	DM1FTEC	Solid tumour/cancer	2A00-2F9Z	Phase 1	[1]

References

• [1] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025396)