Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTELIN2)

• DTT Name: PTPN1 messenger RNA (PTPN1 mRNA)
• Synonyms: Tyrosine-protein phosphatase non-receptor type 1 (mRNA); PTP-1B (mRNA)
• Gene Name: PTPN1
• DTT Type: Successful target; [1]
• BioChemical Class: mRNA target
• UniProt ID: PTN1_HUMAN
• TTD ID: T89529
• EC Number: EC 3.1.3.48
• Sequence:
  MEMEKEFEQIDKSGSWAAIYQDIRHEASDFPCRVAKLPKNKNRNRYRDVSPFDHSRIKLH
  QEDNDYINASLIKMEEAQRSYILTQGPLPNTCGHFWEMVWEQKSRGVVMLNRVMEKGSLK
  CAQYWPQKEEKEMIFEDTNLKLTLISEDIKSYYTVRQLELENLTTQETREILHFHYTTWP
  DFGVPESPASFLNFLFKVRESGSLSPEHGPVVVHCSAGIGRSGTFCLADTCLLLMDKRKD
  PSSVDIKKVLLEMRKFRMGLIQTADQLRFSYLAVIEGAKFIMGDSSVQDQWKELSHEDLE
  PPPEHIPPPPRPPKRILEPHNGKCREFFPNHQWVKEETQEDKDCPIKEEKGSPLNAAPYG
  IESMSQDTEVRSRVVGGSLRGAQAASPAKGEPSLPEKDEDHALSYWKPFLVNMCVATVLT
  AGAYLCYRFLFNSNT
• Function: Mediates dephosphorylation of EIF2AK3/PERK; inactivating the protein kinase activity of EIF2AK3/PERK. May play an important role in CKII- and p60c-src-induced signal transduction cascades. May regulate the EFNA5-EPHA3 signaling pathway which modulates cell reorganization and cell-cell repulsion. May also regulate the hepatocyte growth factor receptor signaling pathway through dephosphorylation of MET. Tyrosine-protein phosphatase which acts as a regulator of endoplasmic reticulum unfolded protein response.
• KEGG Pathway:
  Adherens junction (hsa04520)
  Insulin signaling pathway (hsa04910)
• Reactome Pathway:
  Regulation of IFNG signaling (R-HSA-877312)
  Regulation of IFNA signaling (R-HSA-912694)
  Growth hormone receptor signaling (R-HSA-982772)
  Integrin alphaIIb beta3 signaling (R-HSA-354192)

Molecular Interaction Atlas (MIA) of This DTT

2 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Hydrogen peroxide	DM1NG5W	Infectious disease	1A00-CA43.1	Approved	[2]
TRYPAN BLUE	DM4NTMO	Ophthalmic surgery injury	PK97	Approved	[1]

3 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
ISIS 113715	DMUPD4G	Type-2 diabetes	5A11	Phase 2	[3]
ISIS-PTP1Brx	DMJGVXT	Type-2 diabetes	5A11	Phase 2	[4]
URSOLIC ACID	DM4SOAW	Metabolic syndrome x	5C50-5D2Z	Phase 2	[5]

1 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
ERTIPROTAFIB	DMJXEV7	Type-2 diabetes	5A11	Terminated	[6]

105 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
1,2,3,4,6-penta-O-galloyl-D-glucopyranose	DM9ICSA	Discovery agent	N.A.	Investigative	[7]
1,2,5-THIADIAZOLIDIN-3-ONE-1,1-DIOXIDE	DM9VYOI	Discovery agent	N.A.	Investigative	[8]
1,2-NAPHTHOQUINONE	DMYXELH	Discovery agent	N.A.	Investigative	[9]
1-Iodyl-3-nitro-benzene	DMYIQDE	Discovery agent	N.A.	Investigative	[2]
1-Iodyl-4-nitro-benzene	DMF1WA6	Discovery agent	N.A.	Investigative	[2]
1-METHYL-3-PHENYL-1H-PYRAZOL-5-YLSULFAMIC ACID	DMICQWN	Discovery agent	N.A.	Investigative	[10]
16-alphaH,17-isovaleryloxy-ent-kauran-19-oic acid	DMI49D0	Discovery agent	N.A.	Investigative	[11]
18alpha-Glycyrrhetic acid	DMYS6DB	Discovery agent	N.A.	Investigative	[12]
18beta-Glycyrrhetic acid	DMFMRN8	Discovery agent	N.A.	Investigative	[12]
19alpha,24-dihydroxyurs-12-en-3-on-28-oic acid	DMP168O	Discovery agent	N.A.	Investigative	[13]
2-(Oxalyl-Amino)-Benzoic Acid	DM7LOHK	Discovery agent	N.A.	Investigative	[14]
2-Methyl-2,4-Pentanediol	DMD45CU	Discovery agent	N.A.	Investigative	[14]
24-hydroxyursolic acid	DMVY271	Discovery agent	N.A.	Investigative	[13]
3,9-Dihydroxy-4-prenyl-[6aR,11aR]pterocarpan	DMK53AT	Discovery agent	N.A.	Investigative	[5]
3-(4,5-Bis-biphenyl-4-yl-1H-imidazol-2-yl)-phenol	DMGXPJV	Discovery agent	N.A.	Investigative	[15]
3-(Oxalyl-Amino)-Naphthalene-2-Carboxylic Acid	DMMRV1N	Discovery agent	N.A.	Investigative	[14]
3-epi-masilinic acid	DM1UOWB	Discovery agent	N.A.	Investigative	[16]
3-Iodyl-benzoic acid	DMJSLVT	Discovery agent	N.A.	Investigative	[2]
3-isopropyl-4-(phenylthio)naphthalene-1,2-dione	DMJZEMB	Discovery agent	N.A.	Investigative	[17]
3-oxoolean-12-en-27-oic acid	DM6JYWQ	Discovery agent	N.A.	Investigative	[12]
3alpha,24-dihydroxyolean-12-en-27-oic acid	DM3ZR7A	Discovery agent	N.A.	Investigative	[12]
3beta,6beta-dihydroxyolean-12-en-27-oic acid	DMLEXWC	Discovery agent	N.A.	Investigative	[12]
3beta-acetoxyolean-12-en-27-oic acid	DMOZAHB	Discovery agent	N.A.	Investigative	[12]
3beta-hydroxyolean-12-en-27-oic acid	DMF6VGK	Discovery agent	N.A.	Investigative	[12]
3beta-hydroxyurs-12-en-27-oic acid	DM6NFO0	Discovery agent	N.A.	Investigative	[12]
4'-((2-butylbenzofuran-3-yl)methyl)biphenyl-4-ol	DMCRWTH	Discovery agent	N.A.	Investigative	[18]
4'-(2-butylbenzofuran-3-yl)biphenyl-4-ol	DM2MSEF	Discovery agent	N.A.	Investigative	[18]
4-(p-toluidino)-3-isopropylnaphthalene-1,2-dione	DMQA0EJ	Discovery agent	N.A.	Investigative	[17]
4-Iodyl-benzoic acid	DMQ95EG	Discovery agent	N.A.	Investigative	[2]
5-deoxyabyssinin II	DM1Q0BF	Discovery agent	N.A.	Investigative	[19]
6-(Oxalyl-Amino)-1h-Indole-5-Carboxylic Acid	DM1LY0S	Discovery agent	N.A.	Investigative	[14]
Abyssinin I	DMC02FP	Discovery agent	N.A.	Investigative	[19]
Abyssinin II	DMR7IGZ	Discovery agent	N.A.	Investigative	[19]
Abyssinoflavanone VI	DMEYQF9	Discovery agent	N.A.	Investigative	[19]
Abyssinoflavanone VII	DMTVQSL	Discovery agent	N.A.	Investigative	[19]
Abyssinone-IV	DM9YAVX	Discovery agent	N.A.	Investigative	[20]
Abyssinone-VI-4-O-methyl ether	DMZUY93	Discovery agent	N.A.	Investigative	[20]
Acetate Ion	DMD08RH	Discovery agent	N.A.	Investigative	[14]
ALBAFURAN A	DMO1ZC2	Discovery agent	N.A.	Investigative	[21]
Augustic acid	DMKVDAN	Discovery agent	N.A.	Investigative	[16]
B-Octylglucoside	DMMO75G	Discovery agent	N.A.	Investigative	[14]
BURTTINONE	DMJP0QT	Discovery agent	N.A.	Investigative	[22]
CAULERPIN	DM4QKVN	Discovery agent	N.A.	Investigative	[23]
CHROMOTROPATE	DM5JHUN	Discovery agent	N.A.	Investigative	[1]
Cysteine Sulfenic Acid	DM4GZUJ	N. A.	N. A.	Investigative	[10]
Cysteinesulfonic Acid	DMXI8FP	Discovery agent	N.A.	Investigative	[14]
Double Oxidized Cysteine	DM6TU84	Discovery agent	N.A.	Investigative	[14]
DYSIDINE	DMNYQL9	Discovery agent	N.A.	Investigative	[24]
Erybreadin b	DM27FRY	Discovery agent	N.A.	Investigative	[5]
Erybreadin C	DMNS976	Discovery agent	N.A.	Investigative	[5]
Erybreadin D	DMYG7BM	Discovery agent	N.A.	Investigative	[5]
Erysubin E	DMXWK1A	Discovery agent	N.A.	Investigative	[5]
ERYTHRIBYSSIN A	DM5GEUN	Discovery agent	N.A.	Investigative	[5]
FOLITENOL	DMSBQL0	Discovery agent	N.A.	Investigative	[5]
FORMYLCHROMONE	DMFOU92	Discovery agent	N.A.	Investigative	[25]
Iodyl-benzene	DMO73M9	Discovery agent	N.A.	Investigative	[2]
ISIS 107772	DM37VYR	Discovery agent	N.A.	Investigative	[26]
ISIS 107773	DMA3ZGH	Discovery agent	N.A.	Investigative	[26]
ISIS 107774	DMFOTQY	Discovery agent	N.A.	Investigative	[26]
ISIS 107775	DMLBX9Z	Discovery agent	N.A.	Investigative	[26]
ISIS 107776	DMNHBGJ	Discovery agent	N.A.	Investigative	[26]
ISIS 107791	DMVTU63	Discovery agent	N.A.	Investigative	[26]
ISIS 107792	DMV87MP	Discovery agent	N.A.	Investigative	[26]
Isochroman mono-carboxylic acid	DMUB187	Discovery agent	N.A.	Investigative	[25]
ISOTHIAZOLIDINONE ANALOG	DMKTBEH	Discovery agent	N.A.	Investigative	[8]
Isoxazolecarboxylic acid	DMPZURH	Discovery agent	N.A.	Investigative	[25]
KR61639	DMIEKJ4	Discovery agent	N.A.	Investigative	[27]
Kuwanon J	DMFSUJB	Discovery agent	N.A.	Investigative	[21]
Kuwanon L	DMX4D1Q	Discovery agent	N.A.	Investigative	[28]
Kuwanon R	DMEZOT9	Discovery agent	N.A.	Investigative	[21]
Kuwanon V	DM84M20	Discovery agent	N.A.	Investigative	[21]
LICOAGROCHACONE A	DMWY0TN	Discovery agent	N.A.	Investigative	[29]
LICOAGROCHALCONE A	DMY65ZP	Discovery agent	N.A.	Investigative	[19]
MASLINIC ACID	DMN9UX3	Discovery agent	N.A.	Investigative	[16]
Methyl 3beta-hydroxyolean-12-en-28-oate	DMWG9BE	Discovery agent	N.A.	Investigative	[12]
Methyl3beta-hydroxyolean-12-en-27-oate	DMOA54M	Discovery agent	N.A.	Investigative	[12]
Mulberrofuran C	DMYV49C	Discovery agent	N.A.	Investigative	[28]
Mulberrofuran D	DMMKH72	Discovery agent	N.A.	Investigative	[21]
Mulberrofuran W	DMTV9P3	Discovery agent	N.A.	Investigative	[21]
NEORAUTENOL	DM5GMOJ	Discovery agent	N.A.	Investigative	[5]
Novo Nordisk a/S Compound	DM3C2VA	Discovery agent	N.A.	Investigative	[14]
OHIOENSIN A	DMZMTLB	Discovery agent	N.A.	Investigative	[30]
Ohioensin C	DMNUGTL	Discovery agent	N.A.	Investigative	[30]
Ohioensin F	DMCT348	Discovery agent	N.A.	Investigative	[30]
Ohioensin G	DMLJBVP	Discovery agent	N.A.	Investigative	[30]
OLEANOLIC_ACID	DMWDMJ3	Discovery agent	N.A.	Investigative	[31]
Oleanonic acid	DMYPJC3	Discovery agent	N.A.	Investigative	[13]
Oxalylaminobenzoic acid	DMT7XYE	Discovery agent	N.A.	Investigative	[25]
PARA-(BENZOYL)-PHENYLALANINE	DM2JUTB	Discovery agent	N.A.	Investigative	[8]
PHELLIGRIDIN I	DMAP04X	Discovery agent	N.A.	Investigative	[32]
PNU177836	DMM0EYR	Discovery agent	N.A.	Investigative	[14]
Pomolic acid	DM1GV7K	Discovery agent	N.A.	Investigative	[13]
RK-682	DM5CI2P	Discovery agent	N.A.	Investigative	[33]
Rotungenic acid	DM751OH	Discovery agent	N.A.	Investigative	[13]
Sanggenon C	DMSF5DW	Discovery agent	N.A.	Investigative	[28]
Sanggenon G	DMNHUOD	Discovery agent	N.A.	Investigative	[28]
SIGMOIDIN A	DMB70NK	Discovery agent	N.A.	Investigative	[19]
SIGMOIDIN B	DMVH5WK	Discovery agent	N.A.	Investigative	[19]
Sigmoidin F	DM8E62L	Discovery agent	N.A.	Investigative	[19]
Sp7343-Sp7964	DML2V1I	Discovery agent	N.A.	Investigative	[14]
Spathodic acid	DMJ6WNK	Discovery agent	N.A.	Investigative	[13]
USIMINE A	DMCQ8AL	Discovery agent	N.A.	Investigative	[34]
USNIC ACID	DMGOURX	Discovery agent	N.A.	Investigative	[34]
UVAOL	DMAFQE1	Discovery agent	N.A.	Investigative	[13]
[[4-(Aminomethyl)Phenyl]Amino]Oxo-Acetic Acid,	DMU9F2P	Discovery agent	N.A.	Investigative	[14]

Molecular Expression Atlas (MEA) of This DTT

Disease Name	ICD 11	Studied Tissue	p-value	Fold-Change	Z-score
Type 2 diabetes	5A11	Liver tissue	9.44E-01	7.21E-03	0.08

References

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• [4] Clinical pipeline report, company report or official report of ISIS Pharmaceuticals.
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• [7] Bioactivity-guided isolation of 1,2,3,4,6-Penta-O-galloyl-D-glucopyranose from Paeonia lactiflora roots as a PTP1B inhibitor. J Nat Prod. 2010 Sep 24;73(9):1578-81.
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