| Id: | acc0754 |
| Group: | 2sens |
| Protein: | PLCgamma2 |
| Gene Symbol: | PLCG2 |
| Protein Id: | P16885 |
| Protein Name: | PLCG2_HUMAN |
| PTM: | phosphorylation |
| Site: | Tyr759 |
| Site Sequence: | NSLYDVSRMYVDPSEINPSMP |
| 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:
MSTTVNVDSLAEYEKSQIKRALELGTVMTVFSFRKSTPERRTVQVIMETRQVAWSKTADKIEGFLDIMEIKEIRPGKNSKDFERAKAVRQKEDCCFTILYGTQFVLSTLSLAADSKEDAVNWLSGLKILHQEAMNASTPTIIESWLRKQIYSVDQTRRNSISLRELKTILPLINFKVSSAKFLKDKFVEIGAHKDELSFEQFHLFYKKLMFEQQKSILDEFKKDSSVFILGNTDRPDASAVYLHDFQRFLIHEQQEHWAQDLNKVRERMTKFIDDTMRETAEPFLFVDEFLTYLFSRENSIWDEKYDAVDMQDMNNPLSHYWISSSHNTYLTGDQLRSESSPEAYIRCLRMGCRCIELDCWDGPDGKPVIYHGWTRTTKIKFDDVVQAIKDHAFVTSSFPVILSIEEHCSVEQQRHMAKAFKEVFGDLLLTKPTEASADQLPSPSQLREKIIIKHKKLGPRGDVDVNMEDKKDEHKQQGELYMWDSIDQKWTRHYCAIADAKLSFSDDIEQTMEEEVPQDIPPTELHFGEKWFHKKVEKRTSAEKLLQEYCMETGGKDGTFLVRESETFPNDYTLSFWRSGRVQHCRIRSTMEGGTLKYYLTDNLTFSSIYALIQHYRETHLRCAEFELRLTDPVPNPNPHESKPWYYDSLSRGEAEDMLMRIPRDGAFLIRKREGSDSYAITFRARGKVKHCRINRDGRHFVLGTSAYFESLVELVSYYEKHSLYRKMRLRYPVTPELLERYNMERDINSLYDVSRMYVDPSEINPSMPQRTVKALYDYKAKRSDELSFCRGALIHNVSKEPGGWWKGDYGTRIQQYFPSNYVEDISTADFEELEKQIIEDNPLGSLCRGILDLNTYNVVKAPQGKNQKSFVFILEPKQQGDPPVEFATDRVEELFEWFQSIREITWKIDTKENNMKYWEKNQSIAIELSDLVVYCKPTSKTKDNLENPDFREIRSFVETKADSIIRQKPVDLLKYNQKGLTRVYPKGQRVDSSNYDPFRLWLCGSQMVALNFQTADKYMQMNHALFSLNGRTGYVLQPESMRTEKYDPMPPESQRKILMTLTVKVLGARHLPKLGRSIACPFVEVEICGAEYDNNKFKTTVVNDNGLSPIWAPTQEKVTFEIYDPNLAFLRFVVYEEDMFSDPNFLAHATYPIKAVKSGFRSVPLKNGYSEDIELASLLVFCEMRPVLESEEELYSSCRQLRRRQEELNNQLFLYDTHQNLRNANRDALVKEFSVNENQLQLYQEKCNKRLREKRVSNSKFYS
Select PDB:
No data.
Protein Tractability:
source: Open TargetsPTM Intensity:
source: CPTACNo intensity data of this site,
show all other sites!
| PLCG2-Ser1236 | |||||||||
|---|---|---|---|---|---|---|---|---|---|
| Cancer | Intensity | ||||||||
| BRCA | |||||||||
| COAD | |||||||||
| HGSC | |||||||||
| ccRCC | -1.628 | ||||||||
| GBM | |||||||||
| HNSC | |||||||||
| LUAD | -0.12 | ||||||||
| LUSC | 0.827 | ||||||||
| non_ccRCC | 0.122 | ||||||||
| PDAC | |||||||||
| UCEC | 0.798 | ||||||||
| PLCG2-Ser677 | |||||||||
|---|---|---|---|---|---|---|---|---|---|
| Cancer | Intensity | ||||||||
| BRCA | |||||||||
| COAD | |||||||||
| HGSC | |||||||||
| ccRCC | -0.365 | ||||||||
| GBM | |||||||||
| HNSC | |||||||||
| LUAD | |||||||||
| LUSC | -0.109 | ||||||||
| non_ccRCC | 1.408 | ||||||||
| PDAC | |||||||||
| UCEC | -0.934 | ||||||||
| PLCG2-Ser785 | |||||||||
|---|---|---|---|---|---|---|---|---|---|
| Cancer | Intensity | ||||||||
| BRCA | |||||||||
| COAD | |||||||||
| HGSC | |||||||||
| ccRCC | -0.836 | ||||||||
| GBM | |||||||||
| HNSC | |||||||||
| LUAD | 0.74 | ||||||||
| LUSC | -0.887 | ||||||||
| non_ccRCC | 0.983 | ||||||||
| PDAC | |||||||||
| UCEC | |||||||||
| PLCG2-Ser800 | |||||||||
|---|---|---|---|---|---|---|---|---|---|
| Cancer | Intensity | ||||||||
| BRCA | |||||||||
| COAD | |||||||||
| HGSC | |||||||||
| ccRCC | -0.707 | ||||||||
| GBM | |||||||||
| HNSC | |||||||||
| LUAD | |||||||||
| LUSC | |||||||||
| non_ccRCC | 0.707 | ||||||||
| PDAC | |||||||||
| UCEC | |||||||||
| PLCG2-Ser871 | |||||||||
|---|---|---|---|---|---|---|---|---|---|
| Cancer | Intensity | ||||||||
| BRCA | |||||||||
| COAD | |||||||||
| HGSC | |||||||||
| ccRCC | -0.707 | ||||||||
| GBM | |||||||||
| HNSC | |||||||||
| LUAD | |||||||||
| LUSC | |||||||||
| non_ccRCC | 0.707 | ||||||||
| PDAC | |||||||||
| UCEC | |||||||||
| PLCG2-Ser9 | |||||||||
|---|---|---|---|---|---|---|---|---|---|
| Cancer | Intensity | ||||||||
| BRCA | |||||||||
| COAD | |||||||||
| HGSC | |||||||||
| ccRCC | -0.707 | ||||||||
| GBM | |||||||||
| HNSC | |||||||||
| LUAD | |||||||||
| LUSC | |||||||||
| non_ccRCC | |||||||||
| PDAC | |||||||||
| UCEC | 0.707 | ||||||||
| PLCG2-Ser957 | |||||||||
|---|---|---|---|---|---|---|---|---|---|
| Cancer | Intensity | ||||||||
| BRCA | |||||||||
| COAD | |||||||||
| HGSC | |||||||||
| ccRCC | -0.707 | ||||||||
| GBM | |||||||||
| HNSC | |||||||||
| LUAD | |||||||||
| LUSC | |||||||||
| non_ccRCC | 0.707 | ||||||||
| PDAC | |||||||||
| UCEC | |||||||||
| PLCG2-Tyr482 | |
|---|---|
| Cancer | Intensity |
| BRCA | |
| COAD | |
| HGSC | |
| ccRCC | -0.33 |
| GBM | |
| HNSC | |
| LUAD | 0.43 |
| LUSC | |
| non_ccRCC | 1.112 |
| PDAC | |
| UCEC | -1.212 |
PTM-Disease Association:
source: PTMD| Residue | Position | State | Disease | Class | PMID |
|---|---|---|---|---|---|
| Y | 759 | U | Chronic lymphocytic leukemia | Phosphorylation | 35597428 |
State Note: Based on the distinct PTM states in diseases, PTMD classified all disease-associated PTMs into six classes, including whether the up-regulation (U) or down-regulation (D) of PTM levels, the absence (A) or presence (P) of PTMs, and the creation (C) or disruption (N) of PTM sites are associated with diseases.
PTM-Drug Perturbation Response:
source: DecryptM| Protein | Gene | PTM | Position | Modified sequence | Cell | Drug | pEC50 | Regulation | Experiment |
|---|---|---|---|---|---|---|---|---|---|
| P16885 | PLCG2 | P | Tyr759 | MY(ph)VDPSEINPSMPQR | SU-DHL-4 | Rituximab | -1.8913 | - | |
| P16885 | PLCG2 | P | Tyr759 | MY(ph)VDPSEINPSMPQR | SU-DHL-4 | Rituximab | -1.3451 | - | |
| P16885 | PLCG2 | P | Tyr759 | MY(ph)VDPSEINPSMPQR | SU-DHL-4 | Rituximab | -2.2333 | - | |
| P16885 | PLCG2 | P | Tyr759 | MY(ph)VDPSEINPSMPQR | SU-DHL-4 | Rituximab | -2.0121 | - | |
| P16885 | PLCG2 | P | Tyr759 | MY(ph)VDPSEINPSMPQR | SU-DHL-4 | Rituximab | -3.6863 | - |
pEC50 Note: pEC50 is the negative logarithm of EC50 (half-maximal effective concentration, dosage unit Mol), calculated as pEC50 = -log10(EC50), which quantifies the potency of a drug or compound.
Function score:
source: funscoRNo data.
