Details of the Drug Therapeutic Target (DTT)

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

DTT Name	PIM-3 protein kinase (PIM3)
Synonyms	Serine/threonine-protein kinase pim-3
Gene Name	PIM3
DTT Type	Patented-recorded target	[1]
BioChemical Class	Kinase
UniProt ID	PIM3_HUMAN
TTD ID	T16596
3D Structure	Download 2D Sequence (FASTA) Download 3D Structure (PDB) Download
EC Number	EC 2.7.11.1
Sequence	MLLSKFGSLAHLCGPGGVDHLPVKILQPAKADKESFEKAYQVGAVLGSGGFGTVYAGSRI ADGLPVAVKHVVKERVTEWGSLGGATVPLEVVLLRKVGAAGGARGVIRLLDWFERPDGFL LVLERPEPAQDLFDFITERGALDEPLARRFFAQVLAAVRHCHSCGVVHRDIKDENLLVDL RSGELKLIDFGSGALLKDTVYTDFDGTRVYSPPEWIRYHRYHGRSATVWSLGVLLYDMVC GDIPFEQDEEILRGRLLFRRRVSPECQQLIRWCLSLRPSERPSLDQIAAHPWMLGADGGV PESCDLRLCTLDPDDVASTTSSSESL
Function	May contribute to tumorigenesis through: the delivery of survival signaling through phosphorylation of BAD which induces release of the anti-apoptotic protein Bcl-X(L), the regulation of cell cycle progression, protein synthesis and by regulation of MYC transcriptional activity. Additionally to this role on tumorigenesis, can also negatively regulate insulin secretion by inhibiting the activation of MAPK1/3 (ERK1/2), through SOCS6. Involved also in the control of energy metabolism and regulation of AMPK activity in modulating MYC and PPARGC1A protein levels and cell growth. Proto-oncogene with serine/threonine kinase activity that can prevent apoptosis, promote cell survival and protein translation.

Molecular Interaction Atlas (MIA) of This DTT

Molecular Interaction Atlas (MIA)

Jump to Detail Molecular Interaction Atlas of This DTT

31 Patented Agent(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
BDBM50061601	DMQ4TUE	N. A.	N. A.	Patented	[2]
BDBM50061608	DM3MRD9	N. A.	N. A.	Patented	[2]
BDBM50061612	DMM8IDC	N. A.	N. A.	Patented	[2]
N-{4	DM6R34M	N. A.	N. A.	Patented	[3]
US8481586, 15	DMFEUMZ	N. A.	N. A.	Patented	[4]
US8481586, 40	DM6U3ZR	N. A.	N. A.	Patented	[4]
US8481586, 5	DM5W0A2	N. A.	N. A.	Patented	[4]
US8592455, 3	DMY8U6J	N. A.	N. A.	Patented	[3]
US8592455, 90	DMTE8QO	N. A.	N. A.	Patented	[3]
US8669361, 102	DM4G3OC	N. A.	N. A.	Patented	[5]
US8669361, 103	DMC67G4	N. A.	N. A.	Patented	[6]
US8669361, 105	DMIZWM6	N. A.	N. A.	Patented	[6]
US8669361, 107	DMF8MIB	N. A.	N. A.	Patented	[6]
US8759338, 1	DMRHNIL	N. A.	N. A.	Patented	[7]
US8759338, 12	DMXHN1V	N. A.	N. A.	Patented	[7]
US8759338, 2	DMSBRHJ	N. A.	N. A.	Patented	[7]
US8829193, 1	DMWKDET	N. A.	N. A.	Patented	[8]
US8829193, 2	DMBIAQD	N. A.	N. A.	Patented	[8]
US8829193, 3	DM5ZGK3	N. A.	N. A.	Patented	[8]
US8889696, Staurosporine	DMSYUHK	N. A.	N. A.	Patented	[9]
US8987457, 117	DM4MRP9	N. A.	N. A.	Patented	[10]
US8987457, 15	DMAGNEH	N. A.	N. A.	Patented	[10]
US8987457, 198	DM0O8WS	N. A.	N. A.	Patented	[10]
US9434725, 113	DMS842X	N. A.	N. A.	Patented	[11]
US9434725, 285	DM6Z01B	N. A.	N. A.	Patented	[11]
US9434725, 315	DM316FB	N. A.	N. A.	Patented	[11]
US9580418, Example 11	DMJ76RC	N. A.	N. A.	Patented	[12]
US9580418, Example 8	DMGH9B3	N. A.	N. A.	Patented	[12]
US9682991, 2	DMVGQXK	N. A.	N. A.	Patented	[13]
US9682991, 23	DMGTIP6	N. A.	N. A.	Patented	[13]
US9682991, 7	DM7SQKD	N. A.	N. A.	Patented	[13]
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⏷ Show the Full List of 31 Patented Agent(s)

3 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
PMID21982499C14k	DM0VOXN	Discovery agent	N.A.	Investigative	[1]
PMID22136433C20	DMI8217	Discovery agent	N.A.	Investigative	[14]
PMID24900749C1a	DMZPUSO	Discovery agent	N.A.	Investigative	[15]
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Molecular Expression Atlas (MEA) of This DTT

Molecular Expression Atlas (MEA)

Jump to Detail Molecular Expression Atlas of This DTT

Disease Name	ICD 11	Studied Tissue	p-value	Fold-Change	Z-score
Multiple myeloma	2C82	Bone marrow	7.86E-06	0.78	3.44
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References

1	7-(4H-1,2,4-Triazol-3-yl)benzo[c][2,6]naphthyridines: a novel class of Pim kinase inhibitors with potent cell antiproliferative activity. Bioorg Med Chem Lett. 2011 Nov 15;21(22):6687-92.
2	Azole compounds as PIM inhibitors. US9321756.
3	Kinase inhibitors and methods of their use. US8592455.
4	Pyrrolo[2,3-a] carbazoles and use thereof as PIM kinase inhibitors. US8481586.
5	Pyrazol-4-yl-heterocyclyl-carboxamide compounds and methods of use. US9573943.
6	Pyrazol-4-yl-heterocyclyl-carboxamide compounds and methods of use. US8669361.
7	Heterocyclic kinase inhibitors. US8759338.
8	PIM kinase inhibitors and methods of their use. US8829193.
9	Substituted pyrido[2,3-d]pyrimidin-7(8H)-ones and therapeutic uses thereof. US8889696.
10	Ring-substituted N-pyridinyl amides as kinase inhibitors. US8987457.
11	5-azaindazole compounds and methods of use. US9434725.
12	Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors. US9580418.
13	Tricyclic compounds for use as kinase inhibitors. US9682991.
14	7,8-dichloro-1-oxo-beta-carbolines as a versatile scaffold for the development of potent and selective kinase inhibitors with unusual binding modes. J Med Chem. 2012 Jan 12;55(1):403-13.
15	Structure and Property Based Design of Pyrazolo[1,5-a]pyrimidine Inhibitors of CK2 Kinase with Activity in Vivo. ACS Med Chem Lett. 2013 Jul 3;4(8):800-5.