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target has curated data in GtoImmuPdb
Target id: 1515
Nomenclature: large tumor suppressor kinase 1
Abbreviated Name: LATS1
Family: NDR family
Gene and Protein Information | ||||||
Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
Human | - | 1130 | 6q25.1 | LATS1 | large tumor suppressor kinase 1 | |
Mouse | - | 1129 | 10 A1 | Lats1 | large tumor suppressor | |
Rat | - | 1130 | 1p13 | Lats1 | large tumor suppressor kinase 1 |
Previous and Unofficial Names |
Large tumor suppressor homologue 1 | WARTS |
Database Links | |
Alphafold | O95835 (Hs), Q8BYR2 (Mm) |
BRENDA | 2.7.11.1 |
ChEMBL Target | CHEMBL6167 (Hs) |
Ensembl Gene | ENSG00000131023 (Hs), ENSMUSG00000040021 (Mm), ENSRNOG00000014916 (Rn) |
Entrez Gene | 9113 (Hs), 16798 (Mm), 308265 (Rn) |
Human Protein Atlas | ENSG00000131023 (Hs) |
KEGG Enzyme | 2.7.11.1 |
KEGG Gene | hsa:9113 (Hs), mmu:16798 (Mm), rno:308265 (Rn) |
OMIM | 603473 (Hs) |
Pharos | O95835 (Hs) |
RefSeq Nucleotide | NM_001270519 (Hs), NM_010690 (Mm), NM_001134543 (Rn) |
RefSeq Protein | NP_004681 (Hs), NP_034820 (Mm), NP_001128015 (Rn) |
UniProtKB | O95835 (Hs), Q8BYR2 (Mm) |
Wikipedia | LATS1 (Hs) |
Enzyme Reaction | ||||
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Download all structure-activity data for this target as a CSV file
Inhibitors | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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DiscoveRx KINOMEscan® screen | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform. http://www.discoverx.com/services/drug-discovery-development-services/kinase-profiling/kinomescan Reference: 2,6 |
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Target used in screen: LATS1 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Displaying the top 10 most potent ligands View all ligands in screen » |
Immunopharmacology Comments |
LATS1 and LATS2 are included in the GToImmuPdb because of their crucial role in Hipo signalling, a major mammalian signalling cascade that has recently been identified as playing an important role in shaping the innate immune response [1-2,4]. |
General Comments |
This Ser/Thr kinase is a member of the large tumor suppressor (LATS) family. It participates in the Hippo signalling pathway that regulates organ development, growth and regeneration, and some aspects of cell contact. Dysregulated expression and/or function of LATS1 has been detected in some cancers. |
1. Behnke D, Berenshteyn F, Hao X, Hoffman T, Jin Q, Lacoste A, Lee C, Liu J, Liu Y, Maibaum JK et al.. (2018) 6-6 fused bicyclic heteroaryl compounds and their use as lats inhibitors. Patent number: WO2018198077A2. Assignee: Novartis Ag. Priority date: 26/04/2018. Publication date: 01/11/2018.
2. Davis MI, Hunt JP, Herrgard S, Ciceri P, Wodicka LM, Pallares G, Hocker M, Treiber DK, Zarrinkar PP. (2011) Comprehensive analysis of kinase inhibitor selectivity. Nat Biotechnol, 29 (11): 1046-51. [PMID:22037378]
3. Kastan N, Gnedeva K, Alisch T, Petelski AA, Huggins DJ, Chiaravalli J, Aharanov A, Shakked A, Tzahor E, Nagiel A et al.. (2021) Small-molecule inhibition of Lats kinases may promote Yap-dependent proliferation in postmitotic mammalian tissues. Nat Commun, 12 (1): 3100. [PMID:34035288]
4. Klaeger S, Heinzlmeir S, Wilhelm M, Polzer H, Vick B, Koenig PA, Reinecke M, Ruprecht B, Petzoldt S, Meng C et al.. (2017) The target landscape of clinical kinase drugs. Science, 358 (6367). [PMID:29191878]
5. Narayan S, Ramisetti S, Jaiswal AS, Law BK, Singh-Pillay A, Singh P, Amin S, Sharma AK. (2019) ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. Eur J Med Chem, 161: 456-467. [PMID:30384048]
6. Wodicka LM, Ciceri P, Davis MI, Hunt JP, Floyd M, Salerno S, Hua XH, Ford JM, Armstrong RC, Zarrinkar PP et al.. (2010) Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry. Chem Biol, 17 (11): 1241-9. [PMID:21095574]
7. Zarrinkar PP, Gunawardane RN, Cramer MD, Gardner MF, Brigham D, Belli B, Karaman MW, Pratz KW, Pallares G, Chao Q et al.. (2009) AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). Blood, 114 (14): 2984-92. [PMID:19654408]
NDR family: large tumor suppressor kinase 1. Last modified on 09/05/2023. Accessed on 12/11/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1515.