Molecular Target Synopsis
Overview
Domains and Structures
Drugs and Clinical Candidates
Druggability
Chemistry
Ligand Efficiency Plot
Pathways
Family Cladogram
Interaction Network
Gene Expression
Gene Copy Number Variation
RNAi
Mutations
Germline Genetics

PIM3 (Q86V86) - Overview - Molecular Target Synopsis

Protein


PIM3, Serine/threonine-protein kinase pim-3
Enzyme Classification 2.7.11.1
UniProt Q86V86

Also Known as PIM3_HUMAN, PIM3

Proto-oncogene with serine/threonine kinase activity that can prevent apoptosis, promote cell survival and protein translation. 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. Interacts with BAD. Interacts with PPP2CA; this interaction promotes dephosphorylation of PIM3, ubiquitination and proteasomal degradation. Interacts with SOCS6.

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
326ENSG00000198355ENST00000360612ENSP00000353824Q86V86-1

Sub-cellular localization


UniProt: PIM3 is active in the following subcellular-locations: cytoplasm.
GO terms: PIM3 is active in the following subcellular-locations: cytoplasm, cytosol.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project PIM3 has gain in 3 cell-lines, loss in 2 cell-lines and no signal in 998 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: M14, SK_MEL_5, MDA_MB_435

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: FaDu, NCI-H1573, COLO 699

In Array Express (RNA-seq of long poly adenylated RNA and long non poly adenylated RNA from ENCODE cell lines), the highest expressing cell lines are: HUVEC, SK-N-SH, K562

(see details)

RNA Interference


PIM3 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: H358, OE19. (see details)

3D Structures


At greater than 50% identity similarity to PIM3 there are:
153 structures (161 chains) solved
149 are solved in complex with at least one small molecule ligand
3 are solved with an approved drug

PIM3 is solved in complex with the approved drug(s):

MIX/MITOXANTRONE (4I41_A),
ADN/ADENOSINE (1YI4_A),
AMP/ADENOSINE PHOSPHATE (1YXU_A, 1YXU_B, 1YXU_C, 1YXU_D).

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


PIM3 has been screened with 1924 compounds (2859 bioactivities), 910 compounds have bioactivities that show binding affinity of <= 500nM (983 bioactivities). (see details)