Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTPRO7W)

• DTT Name: Suppressor of tumorigenicity 14 protein (ST14)
• Synonyms: Tumor-associated differentially-expressed gene 15 protein; Tumor associated differentially-expressed gene-15 protein; TADG15; Serine protease TADG-15; Serine protease 14; SNC19; Prostamin; PRSS14; Membrane-type serine protease 1; Membrane type serine protease 1; Matriptase; MT-SP1
• Gene Name: ST14
• DTT Type: Patented-recorded target; [1]
• BioChemical Class: Peptidase
• UniProt ID: ST14_HUMAN
• TTD ID: T31543
• EC Number: EC 3.4.21.109
• Sequence:
  MGSDRARKGGGGPKDFGAGLKYNSRHEKVNGLEEGVEFLPVNNVKKVEKHGPGRWVVLAA
  VLIGLLLVLLGIGFLVWHLQYRDVRVQKVFNGYMRITNENFVDAYENSNSTEFVSLASKV
  KDALKLLYSGVPFLGPYHKESAVTAFSEGSVIAYYWSEFSIPQHLVEEAERVMAEERVVM
  LPPRARSLKSFVVTSVVAFPTDSKTVQRTQDNSCSFGLHARGVELMRFTTPGFPDSPYPA
  HARCQWALRGDADSVLSLTFRSFDLASCDERGSDLVTVYNTLSPMEPHALVQLCGTYPPS
  YNLTFHSSQNVLLITLITNTERRHPGFEATFFQLPRMSSCGGRLRKAQGTFNSPYYPGHY
  PPNIDCTWNIEVPNNQHVKVRFKFFYLLEPGVPAGTCPKDYVEINGEKYCGERSQFVVTS
  NSNKITVRFHSDQSYTDTGFLAEYLSYDSSDPCPGQFTCRTGRCIRKELRCDGWADCTDH
  SDELNCSCDAGHQFTCKNKFCKPLFWVCDSVNDCGDNSDEQGCSCPAQTFRCSNGKCLSK
  SQQCNGKDDCGDGSDEASCPKVNVVTCTKHTYRCLNGLCLSKGNPECDGKEDCSDGSDEK
  DCDCGLRSFTRQARVVGGTDADEGEWPWQVSLHALGQGHICGASLISPNWLVSAAHCYID
  DRGFRYSDPTQWTAFLGLHDQSQRSAPGVQERRLKRIISHPFFNDFTFDYDIALLELEKP
  AEYSSMVRPICLPDASHVFPAGKAIWVTGWGHTQYGGTGALILQKGEIRVINQTTCENLL
  PQQITPRMMCVGFLSGGVDSCQGDSGGPLSSVEADGRIFQAGVVSWGDGCAQRNKPGVYT
  RLPLFRDWIKENTGV
• Function: Proposed to play a role in breast cancer invasion and metastasis. Exhibits trypsin-like activity as defined by cleavage of synthetic substrates with Arg or Lys as the P1 site. Involved in the terminal differentiation of keratinocytes through prostasin (PRSS8) activation and filaggrin (FLG) processing. Degrades extracellular matrix.
• KEGG Pathway: MicroRNAs in cancer (hsa05206)
• Reactome Pathway: Formation of the cornified envelope (R-HSA-6809371)

Molecular Interaction Atlas (MIA) of This DTT

4 Patented Agent(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
US8569313, Inhibitor 14	DMZV6YT	N. A.	N. A.	Patented	[2]
US8569313, Inhibitor 15	DMTMG02	N. A.	N. A.	Patented	[2]
US8569313, Inhibitor 18	DMXTCGM	N. A.	N. A.	Patented	[2]
US8569313, Inhibitor 19	DMLXG43	N. A.	N. A.	Patented	[2]

6 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
2-nas-phe(3-am)-4-(2-guanidinoethyl)piperidine	DMFXKN1	Discovery agent	N.A.	Investigative	[3]
3-tapap	DMKSUV9	Discovery agent	N.A.	Investigative	[3]
Benzamidine	DM37GWL	Discovery agent	N.A.	Investigative	[4]
Inhibitor 1 [Colombo et al., 2012]	DMUQHMP	Discovery agent	N.A.	Investigative	[1]
PMID23849879C3	DMUW3MT	Discovery agent	N.A.	Investigative	[5]
PMID25489658C4d	DMWZJT0	Discovery agent	N.A.	Investigative	[6]

References

• [1] 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: 2418).
• [2] Meta-substituted phenyl sulfonyl amides of secondary amino acid amides, the production thereof, and use thereof as matriptase inhibitors. US8569313.
• [3] Secondary amides of sulfonylated 3-amidinophenylalanine. New potent and selective inhibitors of matriptase. J Med Chem. 2006 Jul 13;49(14):4116-26.
• [4] How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
• [5] 1,2,4-Triazole derivatives as transient inactivators of kallikreins involved in skin diseases. Bioorg Med Chem Lett. 2013 Aug 15;23(16):4547-51.
• [6] Toward the first class of suicide inhibitors of kallikreins involved in skin diseases. J Med Chem. 2015 Jan 22;58(2):598-612.