Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TT2WR1T)

• DTT Name: Cationic trypsinogen (PRSS1)
• Synonyms: Trypsin-1; Trypsin I; TRYP1; TRY1; TRP1; Serine protease 1; Beta-trypsin
• Gene Name: PRSS1
• DTT Type: Successful target; [1]
• BioChemical Class: Peptidase
• UniProt ID: TRY1_HUMAN
• TTD ID: T27602
• EC Number: EC 3.4.21.4
• Sequence:
  MNPLLILTFVAAALAAPFDDDDKIVGGYNCEENSVPYQVSLNSGYHFCGGSLINEQWVVS
  AGHCYKSRIQVRLGEHNIEVLEGNEQFINAAKIIRHPQYDRKTLNNDIMLIKLSSRAVIN
  ARVSTISLPTAPPATGTKCLISGWGNTASSGADYPDELQCLDAPVLSQAKCEASYPGKIT
  SNMFCVGFLEGGKDSCQGDSGGPVVCNGQLQGVVSWGDGCAQKNKPGVYTKVYNYVKWIK
  NTIAANS
• Function: Has activity against the synthetic substrates Boc-Phe-Ser-Arg-Mec, Boc-Leu-Thr-Arg-Mec, Boc-Gln-Ala-Arg-Mec and Boc-Val-Pro-Arg-Mec. The single-chain form is more active than the two-chain form against all of these substrates.
• KEGG Pathway:
  Neuroactive ligand-receptor interaction (hsa04080)
  Pancreatic secretion (hsa04972)
  Protein digestion and absorption (hsa04974)
  Influenza A (hsa05164)
• Reactome Pathway:
  Cobalamin (Cbl, vitamin B12) transport and metabolism (R-HSA-196741)
  Activation of Matrix Metalloproteinases (R-HSA-1592389)

Molecular Interaction Atlas (MIA) of This DTT

1 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Bortezomib	DMNO38U	Leukemia		Approved	[1]

3 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
MELAGATRAN	DM4W8RE	N. A.	N. A.	Phase 3	[2]
Ulinastatin	DMIQCFG	Premature labour	JB00	Phase 3	[3]
Alpha-1 antitrypsin	DM5EFXZ	Coagulation defect	3B10.0	Phase 2	[4]

4 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Dermolastin	DM6WSU2	Atopic dermatitis	EA80	Discontinued in Phase 2	[5]
RWJ-56423	DM6BIHE	Asthma	CA23	Discontinued in Phase 1	[6]
BMY-44621	DM8R3N0	N. A.	N. A.	Terminated	[7]
Patamostat	DM6HBQJ	Hypotension	BA20-BA21	Terminated	[4]

30 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
1,3-Di-p-tolyl-[1,3]diazetidine-2,4-dione	DMHNUWG	Discovery agent	N.A.	Investigative	[8]
1,3-Dibenzyl-[1,3]diazetidine-2,4-dione	DM8NARQ	Discovery agent	N.A.	Investigative	[8]
1-(3-Amino-benzyl)-1H-indole-5-carboxamidine	DMEJZAC	Discovery agent	N.A.	Investigative	[9]
1-(3-Nitro-benzyl)-1H-indole-5-carboxamidine	DM3RGLE	Discovery agent	N.A.	Investigative	[9]
1-Benzyl-1H-indole-5-carboxamidine	DMW0Y92	Discovery agent	N.A.	Investigative	[9]
2-(2-Hydroxy-phenyl)-1H-indole-5-carboxamidine	DM3UMYD	Discovery agent	N.A.	Investigative	[10]
2-(2-Iodo-phenyl)-benzo[d][1,3]oxazin-4-one	DMPA4S0	Discovery agent	N.A.	Investigative	[11]
2-Propionyl-1H-indole-6-carboxamidine	DMORG3D	Discovery agent	N.A.	Investigative	[9]
4-(3,4-Diethoxy-benzylamino)-benzamidine	DMIZXYM	Discovery agent	N.A.	Investigative	[12]
4-(4-Benzyloxy-3-methoxy-benzylamino)-benzamidine	DME3PUT	Discovery agent	N.A.	Investigative	[12]
4-(5-Nitro-indol-1-ylmethyl)-benzamidine	DMUHQ0J	Discovery agent	N.A.	Investigative	[9]
4-Indol-1-ylmethyl-benzamidine	DMG9JSK	Discovery agent	N.A.	Investigative	[9]
6-Styryl-naphthalene-2-carboxamidine	DMDO13Y	Discovery agent	N.A.	Investigative	[13]
8-Bromo-6-styryl-naphthalene-2-carboxamidine	DMKU06T	Discovery agent	N.A.	Investigative	[13]
8-Furan-3-yl-6-styryl-naphthalene-2-carboxamidine	DMFNCG8	Discovery agent	N.A.	Investigative	[13]
ATF-HI-8	DMPJRHX	Discovery agent	N.A.	Investigative	[14]
Benzamidine	DM37GWL	Discovery agent	N.A.	Investigative	[15]
CVS-2139	DMT5R1Q	Discovery agent	N.A.	Investigative	[16]
CVS-2359	DM3KB4H	Discovery agent	N.A.	Investigative	[16]
GR-133686	DMQH8PK	Discovery agent	N.A.	Investigative	[17]
Grassystatin a	DM1PWX2	Discovery agent	N.A.	Investigative	[18]
JBP-1	DM0KMPN	Solid tumour/cancer	2A00-2F9Z	Investigative	[4]
L-375378	DMQWKPM	Discovery agent	N.A.	Investigative	[19]
Macrocyclic tripeptide motif	DMFULZO	Discovery agent	N.A.	Investigative	[20]
Piperidine-1-carboxamidine	DMKYF5U	Discovery agent	N.A.	Investigative	[21]
PMID3514912C9	DM3J746	Discovery agent	N.A.	Investigative	[22]
POP-1	DMVTKCX	Solid tumour/cancer	2A00-2F9Z	Investigative	[4]
recAAT, PPL Therapeutics/Bayer	DM1P830	Discovery agent	N.A.	Investigative	[23]
RWJ-50353	DMRPYGX	Discovery agent	N.A.	Investigative	[24]
Tert-butyloxy carbonyl-D-Phe-pro-Arg-H	DMQKOUZ	Discovery agent	N.A.	Investigative	[25]

References

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