Other PIKK family kinases

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Kinases (EC 2.7.x.x)
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Phosphatidyl inositol 3' kinase-related kinases (PIKK) family
Other PIKK family kinases

Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).

Enzymes

ATM (ATM serine/threonine kinase) Show summary »« Hide summary More detailed page go icon to follow link

Target Id

1934

Nomenclature

ATM serine/threonine kinase

Common abbreviation

ATM

Previous and unofficial names

A-T mutated homolog | ATC | ATD | ATDC | TEL1 | ataxia telangiectasia mutated

Genes

ATM (Hs), Atm (Mm), Atm (Rn)

Ensembl ID

ENSG00000149311 (Hs), ENSMUSG00000034218 (Mm), ENSRNOG00000029773 (Rn)

UniProtKB AC

Q13315 (Hs), Q62388 (Mm)

EC number

2.7.11.1

Inhibitors

KU-60019 pIC₅₀ 8.2 [3]

Selective inhibitors

AZD0156 pIC₅₀ 9.2 [5]

protein kinase, DNA-activated, catalytic subunit Show summary »« Hide summary More detailed page go icon to follow link

Target Id

2800

Nomenclature

protein kinase, DNA-activated, catalytic subunit

Previous and unofficial names

DNA-dependent protein kinase catalytic subunit | protein kinase | protein kinase, DNA activated, catalytic polypeptide | protein kinase, DNA-activated, catalytic polypeptide | DNA-PK

Genes

PRKDC (Hs), Prkdc (Mm), Prkdc (Rn)

Ensembl ID

ENSG00000253729 (Hs), ENSMUSG00000022672 (Mm), ENSRNOG00000025028 (Rn)

UniProtKB AC

P78527 (Hs), P97313 (Mm)

Inhibitors

KU-0060648 pIC₅₀ 8.3 [2]

NU-7441 pIC₅₀ 7.8 [4]

PP121 pIC₅₀ 7.2 [1]

References

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1. Apsel B, Blair JA, Gonzalez B, Nazif TM, Feldman ME, Aizenstein B, Hoffman R, Williams RL, Shokat KM, Knight ZA. (2008) Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Nat Chem Biol, 4 (11): 691-9. [PMID:18849971]

2. Cano C, Saravanan K, Bailey C, Bardos J, Curtin NJ, Frigerio M, Golding BT, Hardcastle IR, Hummersone MG, Menear KA et al.. (2013) 1-substituted (Dibenzo[b,d]thiophen-4-yl)-2-morpholino-4H-chromen-4-ones endowed with dual DNA-PK/PI3-K inhibitory activity. J Med Chem, 56 (16): 6386-401. [PMID:23855836]

3. Golding SE, Rosenberg E, Valerie N, Hussaini I, Frigerio M, Cockcroft XF, Chong WY, Hummersone M, Rigoreau L, Menear KA et al.. (2009) Improved ATM kinase inhibitor KU-60019 radiosensitizes glioma cells, compromises insulin, AKT and ERK prosurvival signaling, and inhibits migration and invasion. Mol Cancer Ther, 8 (10): 2894-902. [PMID:19808981]

4. Leahy JJ, Golding BT, Griffin RJ, Hardcastle IR, Richardson C, Rigoreau L, Smith GC. (2004) Identification of a highly potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor (NU7441) by screening of chromenone libraries. Bioorg Med Chem Lett, 14 (24): 6083-7. [PMID:15546735]

5. Pike KG, Barlaam B, Cadogan E, Campbell A, Chen Y, Colclough N, Davies NL, de-Almeida C, Degorce SL, Didelot M et al.. (2018) The Identification of Potent, Selective, and Orally Available Inhibitors of Ataxia Telangiectasia Mutated (ATM) Kinase: The Discovery of AZD0156 (8-{6-[3-(Dimethylamino)propoxy]pyridin-3-yl}-3-methyl-1-(tetrahydro-2 H-pyran-4-yl)-1,3-dihydro-2 H-imidazo[4,5- c]quinolin-2-one). J Med Chem, 61 (9): 3823-3841. [PMID:29683659]

How to cite this family page

Database page citation:

Other PIKK family kinases. Accessed on 26/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=598.

Concise Guide to PHARMACOLOGY citation:

Alexander SPH, Fabbro D, Kelly E, Mathie AA, Peters JA, Veale EL, Armstrong JF, Faccenda E, Harding SD, Davies JA et al. (2023) The Concise Guide to PHARMACOLOGY 2023/24: Enzymes. Br J Pharmacol. 180 Suppl 2:S289-373.