Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTRMX3V)

• DTT Name: Janus kinase 2 (JAK-2)
• Synonyms: Tyrosine-protein kinase JAK2
• Gene Name: JAK2
• DTT Type: Successful target; [1]
• Related Disease:
  Myeloproliferative neoplasm [ICD-11: 2A20]
  Rheumatoid arthritis [ICD-11: FA20]
  Thrombocytosis [ICD-11: 3B63]
• BioChemical Class: Kinase
• UniProt ID: JAK2_HUMAN
• TTD ID: T08391
• EC Number: EC 2.7.10.2
• Sequence:
  MGMACLTMTEMEGTSTSSIYQNGDISGNANSMKQIDPVLQVYLYHSLGKSEADYLTFPSG
  EYVAEEICIAASKACGITPVYHNMFALMSETERIWYPPNHVFHIDESTRHNVLYRIRFYF
  PRWYCSGSNRAYRHGISRGAEAPLLDDFVMSYLFAQWRHDFVHGWIKVPVTHETQEECLG
  MAVLDMMRIAKENDQTPLAIYNSISYKTFLPKCIRAKIQDYHILTRKRIRYRFRRFIQQF
  SQCKATARNLKLKYLINLETLQSAFYTEKFEVKEPGSGPSGEEIFATIIITGNGGIQWSR
  GKHKESETLTEQDLQLYCDFPNIIDVSIKQANQEGSNESRVVTIHKQDGKNLEIELSSLR
  EALSFVSLIDGYYRLTADAHHYLCKEVAPPAVLENIQSNCHGPISMDFAISKLKKAGNQT
  GLYVLRCSPKDFNKYFLTFAVERENVIEYKHCLITKNENEEYNLSGTKKNFSSLKDLLNC
  YQMETVRSDNIIFQFTKCCPPKPKDKSNLLVFRTNGVSDVPTSPTLQRPTHMNQMVFHKI
  RNEDLIFNESLGQGTFTKIFKGVRREVGDYGQLHETEVLLKVLDKAHRNYSESFFEAASM
  MSKLSHKHLVLNYGVCVCGDENILVQEFVKFGSLDTYLKKNKNCINILWKLEVAKQLAWA
  MHFLEENTLIHGNVCAKNILLIREEDRKTGNPPFIKLSDPGISITVLPKDILQERIPWVP
  PECIENPKNLNLATDKWSFGTTLWEICSGGDKPLSALDSQRKLQFYEDRHQLPAPKWAEL
  ANLINNCMDYEPDFRPSFRAIIRDLNSLFTPDYELLTENDMLPNMRIGALGFSGAFEDRD
  PTQFEERHLKFLQQLGKGNFGSVEMCRYDPLQDNTGEVVAVKKLQHSTEEHLRDFEREIE
  ILKSLQHDNIVKYKGVCYSAGRRNLKLIMEYLPYGSLRDYLQKHKERIDHIKLLQYTSQI
  CKGMEYLGTKRYIHRDLATRNILVENENRVKIGDFGLTKVLPQDKEYYKVKEPGESPIFW
  YAPESLTESKFSVASDVWSFGVVLYELFTYIEKSKSPPAEFMRMIGNDKQGQMIVFHLIE
  LLKNNGRLPRPDGCPDEIYMIMTECWNNNVNQRPSFRDLALRVDQIRDNMAG
• Function: Mediates essential signaling events in both innate and adaptive immunity. In the cytoplasm, plays a pivotal role in signal transduction via its association with type I receptors such as growth hormone (GHR), prolactin (PRLR), leptin (LEPR), erythropoietin (EPOR), thrombopoietin (THPO); or type II receptors including IFN-alpha, IFN-beta, IFN-gamma and multiple interleukins. Following ligand-binding to cell surface receptors, phosphorylates specific tyrosine residues on the cytoplasmic tails of the receptor, creating docking sites for STATs proteins. Subsequently, phosphorylates the STATs proteins once they are recruited to the receptor. Phosphorylated STATs then form homodimer or heterodimers and translocate to the nucleus to activate gene transcription. For example, cell stimulation with erythropoietin (EPO) during erythropoiesis leads to JAK2 autophosphorylation, activation, and its association with erythropoietin receptor (EPOR) that becomes phosphorylated in its cytoplasmic domain. Then, STAT5 (STAT5A or STAT5B) is recruited, phosphorylated and activated by JAK2. Once activated, dimerized STAT5 translocates into the nucleus and promotes the transcription of several essential genes involved in the modulation of erythropoiesis. Part of a signaling cascade that is activated by increased cellular retinol and that leads to the activation of STAT5 (STAT5A or STAT5B). In addition, JAK2 mediates angiotensin-2-induced ARHGEF1 phosphorylation. Plays a role in cell cycle by phosphorylating CDKN1B. Cooperates with TEC through reciprocal phosphorylation to mediate cytokine-driven activation of FOS transcription. In the nucleus, plays a key role in chromatin by specifically mediating phosphorylation of 'Tyr-41' of histone H3 (H3Y41ph), a specific tag that promotes exclusion of CBX5 (HP1 alpha) from chromatin. Non-receptor tyrosine kinase involved in various processes such as cell growth, development, differentiation or histone modifications.
• KEGG Pathway:
  Chemokine signaling pathway (hsa04062)
  PI3K-Akt signaling pathway (hsa04151)
  Signaling pathways regulating pluripotency of stem cells (hsa04550)
  Jak-STAT signaling pathway (hsa04630)
  Cholinergic synapse (hsa04725)
  Prolactin signaling pathway (hsa04917)
  Adipocytokine signaling pathway (hsa04920)
  Leishmaniasis (hsa05140)
  Toxoplasmosis (hsa05145)
  Tuberculosis (hsa05152)
  Measles (hsa05162)
  Influenza A (hsa05164)
  Herpes simplex infection (hsa05168)
• Reactome Pathway:
  MAPK3 (ERK1) activation (R-HSA-110056)
  MAPK1 (ERK2) activation (R-HSA-112411)
  GPVI-mediated activation cascade (R-HSA-114604)
  Prolactin receptor signaling (R-HSA-1170546)
  RMTs methylate histone arginines (R-HSA-3214858)
  G beta (R-HSA-392451)
  Interleukin-3, 5 and GM-CSF signaling (R-HSA-512988)
  RAF activation (R-HSA-5673000)
  RAF/MAP kinase cascade (R-HSA-5673001)
  Interferon gamma signaling (R-HSA-877300)
  Regulation of IFNG signaling (R-HSA-877312)
  Interleukin receptor SHC signaling (R-HSA-912526)
  Growth hormone receptor signaling (R-HSA-982772)
  Factors involved in megakaryocyte development and platelet production (R-HSA-983231)
  Interleukin-6 signaling (R-HSA-1059683)

Molecular Interaction Atlas (MIA) of This DTT

3 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Baricitinib	DM4ONW5	Rheumatoid arthritis	FA20	Approved	[2]
Fedratinib	DM4ZBK6	Myelofibrosis	2A20.2	Approved	[3]
Ruxolitinib	DM7Q98D	Essential thrombocythemia	3B63.1Z	Approved	[1]

15 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
ITF2357	DMFZBNE	Duchenne dystrophy	8C70	Phase 3	[4], [5]
Momelotinib	DMF98Q0	Myelofibrosis	2A20.2	Phase 3	[6], [7]
Pacritinib	DM1T6ZN	Myelofibrosis	2A20.2	Phase 3	[8]
XL019	DMJ6F5C	Solid tumour/cancer	2A00-2F9Z	Phase 3	[4]
AZD1480	DMLK59M	Myeloproliferative syndrome	2A22	Phase 2	[9]
BMS-911543	DMF46PD	Myelofibrosis	2A20.2	Phase 2	[10]
Cerdulatinib	DMSCR2H	B-cell lymphoma	2A86	Phase 2	[11]
CTP-543	DM3SYOK	Asthma	CA23	Phase 2	[12]
CTP-543	DMBT46Y	Alopecia	ED70	Phase 2	[13]
INCB039110	DMD9RV3	Malignant neoplasm	2A00-2F9Z	Phase 2	[14]
LY2784544	DMZASMP	Breast cancer	2C60-2C65	Phase 2	[15]
NS-018	DMU9BCD	Myelofibrosis	2A20.2	Phase 1/2	[16]
AC430	DMPS6U9	leukaemia	2A60-2B33	Phase 1	[2]
Peginterferon beta	DMQ4Z1P	Multiple sclerosis	8A40	Phase 1	[17]
SB-1578	DMXTKYR	Solid tumour/cancer	2A00-2F9Z	Phase 1	[2], [18]

76 Patented Agent(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
1,2,4-triazolo[1,5a]pyridine derivative 1	DMIUPSA	N. A.	N. A.	Patented	[19]
1,2,4-triazolo[1,5a]pyridine derivative 2	DMZFILT	N. A.	N. A.	Patented	[19]
Alkynyl-substituted pyrimidinyl-pyrrole derivative 1	DMK7DJ2	N. A.	N. A.	Patented	[20]
Aminooxazole carboxamide derivative 1	DMDHGPN	N. A.	N. A.	Patented	[20]
Aminotriazolopyridine derivative 1	DMW2LZ0	N. A.	N. A.	Patented	[19]
Aromatic bicyclic compound 1	DMVLQ2P	N. A.	N. A.	Patented	[21]
Aromatic bicyclic compound 2	DMKFV67	N. A.	N. A.	Patented	[21]
Aromatic bicyclic compound 3	DMRXN94	N. A.	N. A.	Patented	[21]
Aromatic bicyclic compound 4	DM3E75P	N. A.	N. A.	Patented	[21]
Aromatic bicyclic compound 5	DMALF06	N. A.	N. A.	Patented	[21]
Aromatic bicyclic compound 6	DM8L3KM	N. A.	N. A.	Patented	[21]
Benzimidazole derivative 7	DMDK4RI	N. A.	N. A.	Patented	[19]
Bis-aminopyrimidine derivative 1	DMQL34C	N. A.	N. A.	Patented	[19]
Bis-aminopyrimidine derivative 2	DMJXNO1	N. A.	N. A.	Patented	[19]
Bis-aminopyrimidine derivative 3	DMUNSYX	N. A.	N. A.	Patented	[19]
Bis-aminopyrimidine derivative 4	DMO1ZIG	N. A.	N. A.	Patented	[19]
Bis-aminopyrimidine derivative 5	DMWXLK1	N. A.	N. A.	Patented	[19]
Curcumin analog 1	DM4765M	N. A.	N. A.	Patented	[21]
Curcumin analog 2	DMZ8S6X	N. A.	N. A.	Patented	[21]
Cyanomethyl pypazole carboxamide derivative 1	DMD198F	N. A.	N. A.	Patented	[20]
Cyclic cyanoethypypazole derivative 1	DM2BZI0	N. A.	N. A.	Patented	[20]
Cycloalkyl nitrile pyrazole carboxamide derivative 1	DM3RK0S	N. A.	N. A.	Patented	[20]
Cycloalkyl nitrile pyrazolo pyridone derivative 1	DMD3LK1	N. A.	N. A.	Patented	[20]
Cycloalkyl nitrile pyrazolo pyridone derivative 2	DMW4JB0	N. A.	N. A.	Patented	[20]
Five-and-six-membered heterocyclic compound 1	DM7SK5Q	N. A.	N. A.	Patented	[20]
Geminally-substituted cyanoethylpypazolo pyridone derivative 1	DMK6RFS	N. A.	N. A.	Patented	[20]
Geminally-substituted cyanoethylpypazolo pyridone derivative 2	DMB2INX	N. A.	N. A.	Patented	[20]
Imidazo[4,5-c]pyridine derivative 2	DMFDRJT	N. A.	N. A.	Patented	[19]
Isoxazole derivative 1	DMUMPZX	N. A.	N. A.	Patented	[20]
Isoxazole derivative 2	DMT842O	N. A.	N. A.	Patented	[20]
N-(cyanomethyl)-4-(2-(phenylamino)pyrimidin-4-yl)benzamide derivative 1	DM0OMAL	N. A.	N. A.	Patented	[19]
PMID27774822-Compound-Figure10Compound12	DMFAGOZ	N. A.	N. A.	Patented	[20]
PMID27774822-Compound-Figure10Compound4	DMMJVTW	N. A.	N. A.	Patented	[20]
PMID27774822-Compound-Figure10Example1	DMCTXPQ	N. A.	N. A.	Patented	[20]
PMID27774822-Compound-Figure10Example19	DMNXYZP	N. A.	N. A.	Patented	[20]
PMID27774822-Compound-Figure11Example5	DMAHFXV	N. A.	N. A.	Patented	[20]
PMID27774822-Compound-Figure1Example20	DMCL19N	N. A.	N. A.	Patented	[20]
PMID27774822-Compound-Figure2Example1-1left	DM86M7D	N. A.	N. A.	Patented	[20]
PMID27774822-Compound-Figure2Example1-1right	DM2YPLF	N. A.	N. A.	Patented	[20]
PMID27774822-Compound-Figure3CompoundI-165	DMOENP4	N. A.	N. A.	Patented	[20]
PMID27774822-Compound-Figure7Example63	DMF5IWB	N. A.	N. A.	Patented	[20]
PMID27774822-Compound-Figure8Example5	DMRHZF3	N. A.	N. A.	Patented	[20]
PMID27774824-Compound-Figure11Example1up	DMH1W8F	N. A.	N. A.	Patented	[19]
PMID27774824-Compound-Figure2Example4	DMQHYMJ	N. A.	N. A.	Patented	[19]
PMID27774824-Compound-Figure3Example18	DMYZ6XQ	N. A.	N. A.	Patented	[19]
PMID27774824-Compound-Figure6Example12	DM1CM7S	N. A.	N. A.	Patented	[19]
PMID27774824-Compound-Figure6Example6	DMB18V5	N. A.	N. A.	Patented	[19]
PMID27774824-Compound-Figure7Example10	DMT85AH	N. A.	N. A.	Patented	[19]
PMID27774824-Compound-Figure8Example22	DM6OCSJ	N. A.	N. A.	Patented	[19]
PMID27774824-Compound-Figure8Example99	DM1VOPH	N. A.	N. A.	Patented	[19]
PMID27774824-Compound-Figure9Example2down	DMXAV42	N. A.	N. A.	Patented	[19]
PMID27774824-Compound-Figure9Example2up	DME3TMS	N. A.	N. A.	Patented	[19]
Pyrazolopyridine derivative 3	DM2VQ4P	N. A.	N. A.	Patented	[20]
Pyrazolopyridine derivative 4	DMX7RWV	N. A.	N. A.	Patented	[20]
Pyrazolopyridine derivative 6	DM5OH8D	N. A.	N. A.	Patented	[19]
Pyrazolopyridine derivative 7	DMCTQ9O	N. A.	N. A.	Patented	[19]
Pyrazolo[4,3-c]pyridine derivative 2	DMCDFLQ	N. A.	N. A.	Patented	[19]
Pyrimidopyridazinone derivative 1	DM32N7D	N. A.	N. A.	Patented	[19]
Pyrimidopyridazinone derivative 2	DMD1RT0	N. A.	N. A.	Patented	[19]
Pyrrole derivative 7	DMZCERW	N. A.	N. A.	Patented	[20]
Pyrrole six-membered heteroaryl ring derivative 1	DM1A0VB	N. A.	N. A.	Patented	[20]
Pyrrolo-pyridine derivative 3	DMSNQEJ	N. A.	N. A.	Patented	[20]
Pyrrolo-pyridone derivative 1	DMR6QCE	N. A.	N. A.	Patented	[20]
Pyrrolo-pyridone derivative 2	DMCZ8UV	N. A.	N. A.	Patented	[20]
Pyrrolo[2,3-d]pyrimidine derivative 11	DM983CY	N. A.	N. A.	Patented	[19]
Pyrrolo[2,3-d]pyrimidine derivative 6	DM3D1L6	N. A.	N. A.	Patented	[20]
Pyrrolo[2,3-d]pyrimidine derivative 7	DM30Y8M	N. A.	N. A.	Patented	[20]
Pyrrolo[2,3-d]pyrimidine derivative 8	DMAW6KU	N. A.	N. A.	Patented	[20]
Ruxolitinib derivative 2	DMSJWZ3	N. A.	N. A.	Patented	[19]
Triazolo-pyridine derivative 1	DM0Q9VY	N. A.	N. A.	Patented	[20]
Tricyclic compound 1	DMLBR4F	N. A.	N. A.	Patented	[19]
Tricyclic compound 11	DMJAZ7D	N. A.	N. A.	Patented	[20]
Tricyclic heterocycle derivative 1	DMXLJH4	N. A.	N. A.	Patented	[20]
Tricyclic heterocycle derivative 2	DM1W02D	N. A.	N. A.	Patented	[19]
Tricyclic heterocycle derivative 5	DMG1ESV	N. A.	N. A.	Patented	[20]
Tricyclic pyrrolopyridine compound 1	DMFIXW4	N. A.	N. A.	Patented	[20]

1 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
AG490	DM3WKO5	Multiple myeloma	2A83	Terminated	[22], [23]

14 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
1,2,3,4,5,6-hexabromocyclohexane	DMVD702	Liver cancer	2C12	Investigative	[24]
5-phenyl-1H-indazol-3-amine	DMJBEIF	Discovery agent	N.A.	Investigative	[25]
AMG-JAK2-01	DMSQ49N	Myeloproliferative syndrome	2A22	Investigative	[14]
Atropisomer 1	DML3R5Z	Discovery agent	N.A.	Investigative	[26]
AZ960	DM95Y82	Discovery agent	N.A.	Investigative	[27]
BVB-808	DM10UHA	Solid tumour/cancer	2A00-2F9Z	Investigative	[14]
CMP-6	DM241YW	Discovery agent	N.A.	Investigative	[28]
K-454	DMYSMWI	Solid tumour/cancer	2A00-2F9Z	Investigative	[14]
NSC-1771	DMNXDGQ	Discovery agent	N.A.	Investigative	[29]
ON-044580	DMWOHDV	Solid tumour/cancer	2A00-2F9Z	Investigative	[30]
PMID21493067C1d	DMFUQIT	Discovery agent	N.A.	Investigative	[31]
PMID24359159C19a	DM26JYS	Discovery agent	N.A.	Investigative	[32]
SGI-1252	DMZ20A5	Solid tumour/cancer	2A00-2F9Z	Investigative	[14]
WHI-P154	DMYHWS1	Diffuse large B-cell lymphoma	2A81	Investigative	[33]

Molecular Expression Atlas (MEA) of This DTT

Disease Name	ICD 11	Studied Tissue	p-value	Fold-Change	Z-score
Polycythemia vera	2C82	Whole blood	8.41E-07	0.36	1.03
Multiple myeloma	2C82	Bone marrow	9.53E-04	0.27	1.44
Psoriasis	EA90	Skin	4.84E-01	-0.03	-0.07
Acute myelocytic leukaemia	2C82	Bone marrow	1.46E-10	-0.5	-0.82
Shwachman-Diamond syndrome	3B64	Bone marrow	2.46E-01	-0.41	-0.6
Rheumatoid arthritis	FA20	Synovial tissue	1.76E-01	0.47	0.49

References

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• [3] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
• [4] Emerging drugs for the therapy of primary and post essential thrombocythemia, post polycythemia vera myelofibrosis. Expert Opin Emerg Drugs. 2009 Sep;14(3):471-9.
• [5] Emerging therapies for multiple myeloma. Expert Opin Emerg Drugs. 2009 Mar;14(1):99-127.
• [6] Genetic determinants of response and survival in momelotinib-treated patients with myelofibrosis.Leukemia.2015 Mar;29(3):741-4.
• [7] CYT387, a novel JAK2 inhibitor, induces hematologic responses and normalizes inflammatory cytokines in murine myeloproliferative neoplasms.Blood.2010 Jun 24;115(25):5232-40.
• [8] National Cancer Institute Drug Dictionary (drug id 609888).
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• [16] Effect of NS-018, a selective JAK2V617F inhibitor, in a murine model of myelofibrosis. Blood Cancer J. 2014 Jan 10;4:e174.
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• [18] SB1578, a novel inhibitor of JAK2, FLT3, and c-Fms for the treatment of rheumatoid arthritis. J Immunol. 2012 Oct 15;189(8):4123-34.
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• [20] Inhibitors of JAK-family kinases: an update on the patent literature 2013-2015, part 2.Expert Opin Ther Pat. 2017 Feb;27(2):145-161.
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• [23] The JAK2 inhibitor AG490 predominantly abrogates the growth of human B-precursor leukemic cells with 11q23 translocation or Philadelphia chromosome. Leukemia. 2001 Nov;15(11):1758-68.
• [24] Identification of 1,2,3,4,5,6-hexabromocyclohexane as a small molecule inhibitor of jak2 tyrosine kinase autophosphorylation [correction of autophophorylation]. J Med Chem. 2005 Apr 7;48(7):2526-33.
• [25] The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
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• [27] Effects of the JAK2 inhibitor, AZ960, on Pim/BAD/BCL-xL survival signaling in the human JAK2 V617F cell line SET-2. J Biol Chem. 2008 Nov 21;283(47):32334-43.
• [28] Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor. Bioorg Med Chem Lett. 2002 Apr 22;12(8):1219-23.
• [29] In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2). Bioorg Med Chem Lett. 2010 Dec 15;20(24):7331-6.
• [30] A Non-ATP-Competitive Dual Inhibitor of JAK2 and BCR-ABL Kinases: Elucidation of a Novel Therapeutic Spectrum Based on Substrate Competitive Inhibition. Genes Cancer. 2010 Apr;1(4):331-45.
• [31] In vitro and in vivo evaluation of 6-aminopyrazolyl-pyridine-3-carbonitriles as JAK2 kinase inhibitors. Bioorg Med Chem Lett. 2011 May 15;21(10):2958-61.
• [32] Discovery of 1-methyl-1H-imidazole derivatives as potent Jak2 inhibitors. J Med Chem. 2014 Jan 9;57(1):144-58.
• [33] The specificity of JAK3 kinase inhibitors. Blood. 2008 Feb 15;111(4):2155-7.