| Id: | acc0760 |
| Group: | 2sens |
| Protein: | BTK |
| Gene Symbol: | Btk |
| Protein Id: | P35991 |
| Protein Name: | BTK_MOUSE |
| PTM: | phosphorylation |
| Site: | Tyr223 |
| Site Sequence: | TELKKVVALYDYMPMNANDLQ |
| Disease Category: | Cancer |
| Disease: | Leukemia |
| Disease Subtype: | CLL |
| Disease Cellline: | |
| Disease Info: | |
| Drug: | acalabrutinib |
| Drug Info: | "Acalabrutinib is a second-generation Bruton's tyrosine kinase (BTK) inhibitor, approved for the treatment of adults with chronic lymphocytic leukemia (CLL), small lymphocytic lymphoma (SLL), and mantle cell lymphoma (MCL), and it is administered orally as capsules or tablets, developed and marketed by AstraZeneca Pharmaceuticals. " |
| Effect: | modulate |
| Effect Info: | "Acalabrutinib targets to reduce the phosphorylation of PLCgamma2 and ERK, and significantly inhibits the proliferation of CLL cells." |
| Note: | |
| Score: | 4.0 |
| Pubmed(PMID): | 27903679 |
| Sentence Index: | 27903679_6-7 |
| Sentence: | "Results: Utilizing biochemical assays, we demonstrate that acalabrutinib is a highly selective BTK inhibitor as compared with ibrutinib. In the human CLL NSG xenograft model, treatment with acalabrutinib demonstrated on-target effects, including decreased phosphorylation of PLCgamma2, ERK, and significant inhibition of CLL cell proliferation." |
Sequence & Structure:
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVIPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPTAAPISTTELKKVVALYDYMPMNANDLQLRKGEEYFILEESNLPWWRARDKNGQEGYIPSNYITEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVFAKSTGEPQGVIRHYVVCSTPQSQYYLAEKHLFSTIPELINYHQHNSAGLISRLKYPVSKQNKNAPSTAGLGYGSWEIDPKDLTFLKELGTGQFGVVKYGKWRGQYDVAIKMIREGSMSEDEFIEEAKVMMNLSHEKLVQLYGVCTKQRPIFIITEYMANGCLLNYLREMRHRFQTQQLLEMCKDVCEAMEYLESKQFLHRDLAARNCLVNDQGVVKVSDFGLSRYVLDDEYTSSVGSKFPVRWSPPEVLMYSKFSSKSDIWAFGVLMWEIYSLGKMPYERFTNSETAEHIAQGLRLYRPHLASERVYTIMYSCWHEKADERPSFKILLSNILDVMDEES
Select PDB:
No data.
Protein Tractability:
source: Open TargetsNo data.
PTM Intensity:
source: CPTACNo data.
PTM-Disease Association:
source: PTMDNo data.
PTM-Drug Perturbation Response:
source: DecryptMNo data.
Function score:
source: funscoRNo data.
