Target Information

Target General Infomation
Target ID
T36935
Former ID
TTDR00503
Target Name
Prostate specific antigen
Gene Name
KLK3
Synonyms
Gamma-seminoprotein; Kallikrein 3; P-30 antigen; PSA; Prostate-specific antigen; Semenogelase; Seminin; KLK3
Target Type
Clinical Trial
Disease Prostate cancer [ICD9: 185; ICD10: C61]
Prostate hyperplasia [ICD10: N40]
Restenosis [ICD10: I51.89]
Function
Hydrolyzes semenogelin-1 thus leadingto the liquefaction of the seminal coagulum.
BioChemical Class
Peptidase
UniProt ID
P07288
EC Number
EC 3.4.21.77
Sequence
MWVPVVFLTLSVTWIGAAPLILSRIVGGWECEKHSQPWQVLVASRGRAVCGGVLVHPQWV
LTAAHCIRNKSVILLGRHSLFHPEDTGQVFQVSHSFPHPLYDMSLLKNRFLRPGDDSSHD
LMLLRLSEPAELTDAVKVMDLPTQEPALGTTCYASGWGSIEPEEFLTPKKLQCVDLHVIS
NDVCAQVHPQKVTKFMLCAGRWTGGKSTCSGDSGGPLVCNGVLQGITSWGSEPCALPERP
SLYTKVVHYRKWIKDTIVANP
Drugs and Mode of Action
Drug(s) Motexafin lutetium Drug Info Phase 3 Restenosis [529626]
ProstaVac Drug Info Phase 3 Prostate hyperplasia [544259]
PRX-302 Drug Info Phase 3 Prostate cancer [524482]
Rilimogene galvacirepvec Drug Info Phase 3 Prostate cancer [530657]
Modulator ADXS-PSA Drug Info [543613]
Motexafin lutetium Drug Info [529626]
ProstaRex Drug Info [543613]
PRX-302 Drug Info [531283]
Rilimogene galvacirepvec Drug Info [530657]
VTT-201 Drug Info [543613]
Inhibitor compound 20 Drug Info [532367]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Pathways in cancer
Prostate cancer
Pathway Interaction Database Coregulation of Androgen receptor activity
Regulation of Androgen receptor activity
FOXA1 transcription factor network
Reactome Regulation of Insulin-like Growth Factor (IGF) transport and uptake by Insulin-like Growth Factor Binding Proteins (IGFBPs)
Activated PKN1 stimulates transcription of AR (androgen receptor) regulated genes KLK2 and KLK3
WikiPathways Prostate Cancer
Androgen receptor signaling pathway
References
Ref 524482ClinicalTrials.gov (NCT01966614) Randomized, Double-Blind, Vehicle-Controlled, Multicenter Safety and Efficacy Study of Intraprostatic PRX302 for LUTS BPH. U.S. National Institutes of Health.
Ref 529626Motexafin 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.
Ref 530657Overall 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.
Ref 544259Prostvac-VF: a vector-based vaccine targeting PSA in prostate cancer. Expert Opin Investig Drugs. 2009 July; 18(7): 1001-1011.
Ref 529626Motexafin 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.
Ref 530657Overall 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.
Ref 531283Phase 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.
Ref 532367Structural optimization, biological evaluation, and application of peptidomimetic prostate specific antigen inhibitors. J Med Chem. 2013 Jun 13;56(11):4224-35.
Ref 543613(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).

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