| Id: | acc0724 |
| Group: | 2sens |
| Protein: | histone H3 |
| Gene Symbol: | H3C1 |
| Protein Id: | P68431 |
| Protein Name: | H31_HUMAN |
| PTM: | acetylation |
| Site: | Lys9 |
| Site Sequence: | -MARTKQTARKSTGGKAPRKQ |
| Disease Category: | Cancer |
| Disease: | Colorectal Cancer |
| Disease Subtype: | |
| Disease Cellline: | HCT116 |
| Disease Info: | |
| Drug: | CUDC-907 |
| Drug Info: | "CUDC-907 is a dual inhibitor of PI3K (phosphoinositide 3-kinase) and HDAC (histone deacetylase), targeting PI3Kalpha/beta/delta with IC50 values of 19/54/39 nM and HDAC1/2/3/10 with IC50 values of 1.7/5.0/1.8/2.8 nM, currently in Phase 1 clinical development for anticancer therapy. " |
| Effect: | enhance |
| Effect Info: | "CUDC-907 promotes histone H3 lysine 9 acetylation (H3K9ac) and inhibits AKT phosphorylation (Ser473), thereby suppressing tumors. CUDC-907 sensitizes CRC cells to 5-FU-induced cell death." |
| Note: | "drug comb, histone" |
| Score: | 4.0 |
| Pubmed(PMID): | 28139498 |
| Sentence Index: | 28139498_10-11 |
| Sentence: | "Furthermore, CRC cells treated with CUDC-907 exhibited a higher degree of histone H3 lysine 9 acetylation (H3K9ac) and reduced AKT phosphorylation (Ser473). CONCLUSION: Our data revealed, for the first time, the enhanced inhibitory effect of CUDC-907 against CRC cells when combined with 5-FU, supporting the application of this combination as a potential therapeutic strategy in CRC treatment." |
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 |
|---|---|---|---|---|---|
| K | 9 | D | Diabetes mellitus | Acetylation | 23423566 |
| K | 9 | D | Friedreich's ataxia | Acetylation | 18045775 |
| K | 9 | D | Prostate cancer | Acetylation | 19885564 |
| K | 9 | D | Systemic lupus erythematosus | Acetylation | 36165173 |
| K | 9 | D | Prostate cancer | Methylation | 19739128 |
| K | 9 | D | Pancreatic carcinoma | Methylation | 20142597 |
| K | 9 | U | Prostate cancer | Acetylation | 19935671 |
| K | 9 | U | Diabetes mellitus | Acetylation | 23423566 |
| K | 9 | U | Gastric adenocarcinoma | Acetylation | 18470569 |
| K | 9 | U | Type 2 diabetes | Acetylation | 34944721 |
| K | 9 | U | Breast cancer | Methylation | 19943104 |
| K | 9 | U | Friedreich's ataxia | Methylation | 18045775 |
| K | 9 | U | Friedreich's ataxia | Methylation | 18045775 |
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.
