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

TNK1 (Q13470) - Overview - Molecular Target Synopsis

Protein


TNK1, Non-receptor tyrosine-protein kinase TNK1
Enzyme Classification 2.7.10.2
UniProt Q13470

Also Known as TNK1_HUMAN, TNK1

Involved in negative regulation of cell growth. Has tumor suppressor properties. Plays a negative regulatory role in the Ras-MAPK pathway. May function in signaling pathways utilized broadly during fetal development and more selectively in adult tissues and in cells of the lymphohematopoietic system. Could specifically be involved in phospholipid signal transduction. Interacts with the SH3 domain of PLCG1 via its Pro-rich domain.

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: TNK1 is active in the following subcellular-locations: cytoplasm, membrane.
GO terms: TNK1 is active in the following subcellular-locations: cytoplasm, cytosol, membrane.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project TNK1 has gain in 1 cell-lines, loss in 7 cell-lines and no signal in 997 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: HCC_2998, HCT_116, SK_OV_3

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: DOK, PE/CA-PJ15, NCI-H820

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: HMEC, HeLa-S3, K562

(see details)

RNA Interference


TNK1 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: ZR7530, BT474. (see details)

3D Structures


At greater than 35% identity similarity to TNK1 there are:
171 structures (250 chains) solved
148 are solved in complex with at least one small molecule ligand
12 are solved with an approved drug

TNK1 is solved in complex with the approved drug(s):

AQ4/ERLOTINIB (1M17_A, 4HJO_A),
FMM/LAPATINIB (1XKK_A, 3BBT_B, 3BBT_D),
IRE/GEFITINIB (2ITO_A, 2ITY_A, 2ITZ_A, 3UG2_A, 4I22_A, 4WKQ_A),
YY3/OSIMERTINIB (4ZAU_A),
0WM/AFATINIB (4G5J_A).

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


TNK1 has been screened with 500 compounds (917 bioactivities), 15 compounds have bioactivities that show binding affinity of <= 500nM (22 bioactivities). (see details)