Details of the Drug-Related molecule(s) Interaction Atlas

General Information of DTT (ID: TT2WR1T)

• DTT Name: Cationic trypsinogen (PRSS1) DTT Info
• Gene Name: PRSS1

Molecule-Related Drug & Molecule List

1 Approved Drug(s) Transported by This DTP

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

3 Clinical Trial Drug(s) Transported by This DTP

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) Transported by This DTP

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) Transported by This DTP

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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• [2] Orally active thrombin inhibitors. Part 1: optimization of the P1-moiety. Bioorg Med Chem Lett. 2006 May 15;16(10):2641-7.
• [3] Intravenous administration of ulinastatin (human urinary trypsin inhibitor) in severe sepsis: a multicenter randomized controlled study. Intensive Care Med. 2014 Jun;40(6):830-8.
• [4] US patent application no. 2012,0251,516, PHARMACEUTICAL COMPOSITION FOR TREATING CANCER COMPRISING TRYPSINOGEN AND/OR CHYMOTRYPSINOGEN AND AN ACTIVE AGENT SELECTED FROM A SELENIUM COMPOUND, A VANILLOID COMPOUND AND A CYTOPLASMIC GLYCOLYSIS REDUCTION AGENT.
• [5] Arriva-ProMetic recombinant alpha 1-antitrypsin (rAAT) moves into the clinic for dermatology applications. ProMetic Life Sciences. 2009.
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• [11] 2-amino-4H-3,1-benzoxazin-4-ones as inhibitors of C1r serine protease. J Med Chem. 1998 Mar 26;41(7):1060-7.
• [12] Design of selective phenylglycine amide tissue factor/factor VIIa inhibitors. Bioorg Med Chem Lett. 2005 Feb 1;15(3):817-22.
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• [14] Inhibitory effect of a conjugate between human urokinase and urinary trypsin inhibitor on tumor cell invasion in vitro. J Biol Chem. 1995 Apr 7;270(14):8361-6.
• [15] How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
• [16] Non-covalent thrombin inhibitors featuring P(3)-heterocycles with P(1)-monocyclic arginine surrogates. Bioorg Med Chem Lett. 2002 Apr 22;12(8):1203-8.
• [17] 5,5-trans lactone-containing inhibitors of serine proteases: identification of a novel, acylating thrombin inhibitor. Bioorg Med Chem Lett. 1998 Nov 3;8(21):2955-60.
• [18] Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation. J Med Chem. 2009 Sep 24;52(18):5732-47.
• [19] Small, low nanomolar, noncovalent thrombin inhibitors lacking a group to fill the 'distal binding pocket'. Bioorg Med Chem Lett. 2003 Jan 20;13(2):161-4.
• [20] Novel thrombin inhibitors that are based on a macrocyclic tripeptide motif, Bioorg. Med. Chem. Lett. 6(24):2947-2952 (1996).
• [21] GRID/CPCA: a new computational tool to design selective ligands. J Med Chem. 2000 Aug 10;43(16):3033-44.
• [22] Synthesis and inhibition of human acrosin and trypsin and acute toxicity of aryl 4-guanidinobenzoates. J Med Chem. 1986 Apr;29(4):514-9.
• [23] Reduction in neutrophil elastase concentration by recombinant alphal-antitrypsin (recAAT) does not alter bacterial loading in the sputum of cystic ... Br J Biomed Sci. 2004;61(3):146-7.
• [24] In-depth study of tripeptide-based alpha-ketoheterocycles as inhibitors of thrombin. Effective utilization of the S1' subsite and its implications ... J Med Chem. 2005 Mar 24;48(6):1984-2008.
• [25] Structure-activity study of tripeptide thrombin inhibitors using alpha-alkyl amino acids and other conformationally constrained amino acid substitu... J Med Chem. 1995 Oct 27;38(22):4446-53.