| Id: | acc3585 |
| Group: | 2sens |
| Protein: | MCL-1 |
| Gene Symbol: | MCL1 |
| Protein Id: | Q07820 |
| Protein Name: | MCL1_HUMAN |
| PTM: | phosphorylation |
| Site: | Ser159 |
| Site Sequence: | SGNNTSTDGSLPSTPPPAEEE |
| Disease Category: | Cancer |
| Disease: | Leukemia |
| Disease Subtype: | Acute Myeloid Leukemia |
| Disease Cellline: | |
| Disease Info: | |
| Drug: | Venetoclax + Gilteritinib |
| Drug Info: | Venetoclax is a drug used in certain cancer treatments | Gilteritinib is also a medication that plays a role in treating specific types of cancers. |
| Effect: | modulate |
| Effect Info: | "Enhanced phosphorylation of Ser159 is associated with the ubiquitination and degradation of MCL - 1 protein, promoting apoptosis." |
| Note: | |
| Score: | 4.0 |
| Pubmed(PMID): | 35857899 |
| Sentence Index: | 35857899_10-11 |
| Sentence: | "MCL-1 downregulation was associated with increased MCL-1 phosphorylation of serine 159, decreased phosphorylation of threonine 161 and proteasomal degradation. Gilteritinib and venetoclax were active in a FLT3 wildtype AML PDX model with TP53 mutation and reduced leukemic burden in four FLT3 wildtype AML patients receiving venetoclax-gilteritinib off-label after developing refractory disease under venetoclax-azacitidine." |
Sequence & Structure:
MFGLKRNAVIGLNLYCGGAGLGAGSGGATRPGGRLLATEKEASARREIGGGEAGAVIGGSAGASPPSTLTPDSRRVARPPPIGAEVPDVTATPARLLFFAPTRRAAPLEEMEAPAADAIMSPEEELDGYEPEPLGKRPAVLPLLELVGESGNNTSTDGSLPSTPPPAEEEEDELYRQSLEIISRYLREQATGAKDTKPMGRSGATSRKALETLRRVGDGVQRNHETAFQGMLRKLDIKNEDDVKSLSRVMIHVFSDGVTNWGRIVTLISFGAFVAKHLKTINQESCIEPLAESITDVLVRTKRDWLVKQRGWDGFVEFFHVEDLEGGIRNVLLAFAGVAGVGAGLAYLIR
Select PDB:
| Target | Drug name | MOA | Phase | Status | Disease | Source |
|---|---|---|---|---|---|---|
| MCL1 | OBATOCLAX | Induced myeloid leukemia cell differentiation protein Mcl-1 inhibitor | 3 | Withdrawn | small cell lung carcinoma | ClinicalTrials |
| MCL1 | OBATOCLAX MESYLATE | Induced myeloid leukemia cell differentiation protein Mcl-1 inhibitor | 3 | Withdrawn | small cell lung carcinoma | ClinicalTrials |
| MCL1 | OBATOCLAX MESYLATE | Induced myeloid leukemia cell differentiation protein Mcl-1 inhibitor | 2 | Completed | Hodgkins lymphoma | ClinicalTrials |
| MCL1 | OBATOCLAX | Induced myeloid leukemia cell differentiation protein Mcl-1 inhibitor | 2 | Completed | Hodgkins lymphoma | ClinicalTrials |
| MCL1 | OBATOCLAX | Induced myeloid leukemia cell differentiation protein Mcl-1 inhibitor | 2 | Completed | myelodysplastic syndrome | ClinicalTrials |
| MCL1 | OBATOCLAX | Induced myeloid leukemia cell differentiation protein Mcl-1 inhibitor | 2 | Completed | acute myeloid leukemia | ClinicalTrials |
| MCL1 | OBATOCLAX MESYLATE | Induced myeloid leukemia cell differentiation protein Mcl-1 inhibitor | 2 | Completed | myelodysplastic syndrome | ClinicalTrials |
| MCL1 | OBATOCLAX MESYLATE | Induced myeloid leukemia cell differentiation protein Mcl-1 inhibitor | 2 | Completed | follicular lymphoma | ClinicalTrials |
| MCL1 | OBATOCLAX | Induced myeloid leukemia cell differentiation protein Mcl-1 inhibitor | 2 | Completed | follicular lymphoma | ClinicalTrials |
| MCL1 | OBATOCLAX | Induced myeloid leukemia cell differentiation protein Mcl-1 inhibitor | 2 | Completed | myelofibrosis | ClinicalTrials |
| MCL1 | OBATOCLAX MESYLATE | Induced myeloid leukemia cell differentiation protein Mcl-1 inhibitor | 2 | Completed | myelofibrosis | ClinicalTrials |
| MCL1 | OBATOCLAX MESYLATE | Induced myeloid leukemia cell differentiation protein Mcl-1 inhibitor | 1 | Completed | chronic lymphocytic leukemia | ClinicalTrials |
| MCL1 | OBATOCLAX | Induced myeloid leukemia cell differentiation protein Mcl-1 inhibitor | 1 | Completed | chronic lymphocytic leukemia | ClinicalTrials |
| MCL1 | OBATOCLAX MESYLATE | Induced myeloid leukemia cell differentiation protein Mcl-1 inhibitor | 1 | Terminated | chronic lymphocytic leukemia | ClinicalTrials ClinicalTrials |
| MCL1 | OBATOCLAX | Induced myeloid leukemia cell differentiation protein Mcl-1 inhibitor | 1 | Terminated | chronic lymphocytic leukemia | ClinicalTrials ClinicalTrials |
| MCL1 | OBATOCLAX MESYLATE | Induced myeloid leukemia cell differentiation protein Mcl-1 inhibitor | 1 | Terminated | diffuse large B-cell lymphoma | ClinicalTrials |
| MCL1 | OBATOCLAX | Induced myeloid leukemia cell differentiation protein Mcl-1 inhibitor | 1 | Terminated | diffuse large B-cell lymphoma | ClinicalTrials |
| MCL1 | OBATOCLAX MESYLATE | Induced myeloid leukemia cell differentiation protein Mcl-1 inhibitor | 1 | Completed | small cell lung carcinoma | ClinicalTrials |
| MCL1 | OBATOCLAX | Induced myeloid leukemia cell differentiation protein Mcl-1 inhibitor | 1 | Completed | small cell lung carcinoma | ClinicalTrials ClinicalTrials |
| MCL1 | OBATOCLAX | Induced myeloid leukemia cell differentiation protein Mcl-1 inhibitor | 1 | Terminated | multiple myeloma | ClinicalTrials |
| MCL1 | OBATOCLAX MESYLATE | Induced myeloid leukemia cell differentiation protein Mcl-1 inhibitor | 1 | Terminated | multiple myeloma | ClinicalTrials |
| MCL1 | OBATOCLAX MESYLATE | Induced myeloid leukemia cell differentiation protein Mcl-1 inhibitor | 1 | Completed | lymphoid neoplasm | ClinicalTrials |
| MCL1 | OBATOCLAX | Induced myeloid leukemia cell differentiation protein Mcl-1 inhibitor | 1 | Completed | lymphoid neoplasm | ClinicalTrials |
| MCL1 | OBATOCLAX | Induced myeloid leukemia cell differentiation protein Mcl-1 inhibitor | 1 | Terminated | metastatic melanoma | ClinicalTrials |
| MCL1 | OBATOCLAX MESYLATE | Induced myeloid leukemia cell differentiation protein Mcl-1 inhibitor | 1 | Terminated | metastatic melanoma | ClinicalTrials |
Note: Only show clinically investigational or approved drugs with protein targets.
Protein Tractability:
source: Open TargetsPTM Intensity:
source: CPTAC| MCL1-Ser159 | |
|---|---|
| Cancer | Intensity |
| BRCA | |
| COAD | -0.489 |
| HGSC | |
| ccRCC | -1.174 |
| GBM | |
| HNSC | 0.807 |
| LUAD | 0.856 |
| LUSC | |
| non_ccRCC | |
| PDAC | |
| UCEC | |
PTM-Disease Association:
source: PTMDNo data.
PTM-Drug Perturbation Response:
source: DecryptMNo data.
Function score:
source: funscoRNo data.
