General Information of Drug Therapeutic Target (DTT) (ID: TTS78AZ)

DTT Name Prostate specific antigen (KLK3)
Synonyms Seminin; Semenogelase; Prostate-specific antigen; PSA; P-30 antigen; Kallikrein-3; Gamma-seminoprotein; APS
Gene Name KLK3
DTT Type
Clinical trial target
[1]
BioChemical Class
Peptidase
UniProt ID
KLK3_HUMAN
TTD ID
T36935
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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EC Number
EC 3.4.21.77
Sequence
MWVPVVFLTLSVTWIGAAPLILSRIVGGWECEKHSQPWQVLVASRGRAVCGGVLVHPQWV
LTAAHCIRNKSVILLGRHSLFHPEDTGQVFQVSHSFPHPLYDMSLLKNRFLRPGDDSSHD
LMLLRLSEPAELTDAVKVMDLPTQEPALGTTCYASGWGSIEPEEFLTPKKLQCVDLHVIS
NDVCAQVHPQKVTKFMLCAGRWTGGKSTCSGDSGGPLVCNGVLQGITSWGSEPCALPERP
SLYTKVVHYRKWIKDTIVANP
Function Hydrolyzes semenogelin-1 thus leading to the liquefaction of the seminal coagulum.
KEGG Pathway
Pathways in cancer (hsa05200 )
Prostate cancer (hsa05215 )
Reactome Pathway
Activated PKN1 stimulates transcription of AR (androgen receptor) regulated genes KLK2 and KLK3 (R-HSA-5625886 )
Regulation of Insulin-like Growth Factor (IGF) transport and uptake by Insulin-like Growth Factor Binding Proteins (IGFBPs) (R-HSA-381426 )

Molecular Interaction Atlas (MIA) of This DTT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DTT
6 Clinical Trial Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
Motexafin lutetium DM8K5Z6 Artery stenosis BD52 Phase 3 [1]
ProstaVac DM5FZH4 Prostate hyperplasia GA90 Phase 3 [2]
PRX-302 DMEH641 Prostate cancer 2C82.0 Phase 3 [3]
Rilimogene galvacirepvec DMGTCI0 Prostate cancer 2C82.0 Phase 3 [4]
ADXS-PSA DMOPVET Prostate cancer 2C82.0 Phase 1/2 [2]
MVA-BN Breast DMFMW5C Prostate cancer 2C82.0 Phase 1 [5]
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⏷ Show the Full List of 6 Clinical Trial Drug(s)
4 Investigative Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
Anti-PSA mabs DMO21T7 Prostate cancer 2C82.0 Investigative [2]
PMID23692593C20 DM1T9LJ Discovery agent N.A. Investigative [6]
ProstaRex DM9GFOM Prostate cancer 2C82.0 Investigative [2]
VTT-201 DMT967L Prostate cancer 2C82.0 Investigative [2]
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Molecular Expression Atlas (MEA) of This DTT

Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This DTT
Disease Name ICD 11 Studied Tissue p-value Fold-Change Z-score
Prostate cancer 2C82 Prostate 2.01E-01 -0.04 -0.09
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References

1 Motexafin lutetium-photodynamic therapy of prostate cancer: short- and long-term effects on prostate-specific antigen. Clin Cancer Res. 2008 Aug 1;14(15):4869-76.
2 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2373).
3 Phase 1 and 2 studies demonstrate the safety and efficacy of intraprostatic injection of PRX302 for the targeted treatment of lower urinary tract symptoms secondary to benign prostatic hyperplasia. Eur Urol. 2011 May;59(5):747-54.
4 Overall survival analysis of a phase II randomized controlled trial of a Poxviral-based PSA-targeted immunotherapy in metastatic castration-resistant prostate cancer. J Clin Oncol. 2010 Mar 1;28(7):1099-105.
5 Exosome targeting of tumor antigens expressed by cancer vaccines can improve antigen immunogenicity and therapeutic efficacy. Cancer Res. 2011 Aug 1;71(15):5235-44.
6 Structural optimization, biological evaluation, and application of peptidomimetic prostate specific antigen inhibitors. J Med Chem. 2013 Jun 13;56(11):4224-35.