| Id: | acc2102 |
| Group: | 2sens |
| Protein: | histone H3 |
| Gene Symbol: | H3C1 |
| Protein Id: | P68431 |
| Protein Name: | H31_HUMAN |
| PTM: | phosphorylation |
| Site: | Ser10 |
| Site Sequence: | MARTKQTARKSTGGKAPRKQL |
| Disease Category: | Cancer |
| Disease: | Breast Cancer |
| Disease Subtype: | TNBC |
| Disease Cellline: | MDA-MB-468 |
| Disease Info: | |
| Drug: | BOS172722 |
| Drug Info: | "BOS-172722: A small molecule inhibitor with potential research applications, currently referenced in scientific product listings but lacking detailed publicly available pharmacological or clinical data. " |
| Effect: | modulate |
| Effect Info: | "BOS172722 can effectively inhibit the spindle assembly checkpoint induced by paclitaxel in the TNBC human tumor xenograft model, specifically manifested as inhibiting the phosphorylation of histone H3 and the phosphorylation of MPS1 substrate KNL1." |
| Note: | histone |
| Score: | 3.0 |
| Pubmed(PMID): | 31575759 |
| Sentence Index: | 31575759_3-4 |
| Sentence: | "BOS172722 synergizes with paclitaxel to induce gross chromosomal segregation defects caused by MPS1 inhibitor-mediated abrogation of the mitotic delay induced by paclitaxel treatment. In in vivo pharmacodynamic experiments, BOS172722 potently inhibits the spindle assembly checkpoint induced by paclitaxel in human tumor xenograft models of TNBC, as measured by inhibition of the phosphorylation of histone H3 and the phosphorylation of the MPS1 substrate, KNL1." |
Sequence & Structure:
MARTKQTARKSTGGKAPRKQLATKAARKSAPATGGVKKPHRYRPGTVALREIRRYQKSTELLIRKLPFQRLVREIAQDFKTDLRFQSSAVMALQEACEAYLVGLFEDTNLCAIHAKRVTIMPKDIQLARRIRGERA
Select PDB:
No data.
Protein Tractability:
source: Open TargetsNo data.
PTM Intensity:
source: CPTACNo data.
PTM-Disease Association:
source: PTMD| Residue | Position | State | Disease | Class | PMID |
|---|---|---|---|---|---|
| S | 10 | D | Breast cancer | Phosphorylation | 21146603 |
| S | 10 | U | Breast adenocarcinoma | Phosphorylation | 16461563 |
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: DecryptMNo data.
Function score:
source: funscoRNo data.
