Serine/threonine-protein kinase PLK1
Named enzymes, including the metabolising cytochromes and the monoamine oxidases.
- Measurements
- 5
- Compounds
- 5
- Binding constants
- 0
- Median pX
- —
I · Identity
What this target is
Its function as UniProt states it, where in a cell the protein is found, and which cell types and tissues transcribe its gene.
Serine/threonine-protein kinase PLK1
Serine/threonine-protein kinase that performs several important functions throughout M phase of the cell cycle, including the regulation of centrosome maturation and spindle assembly, the removal of cohesins from chromosome arms, the inactivation of anaphase-promoting complex/cyclosome (APC/C) inhibitors, and the regulation of mitotic exit and cytokinesis11202906,12207013,12447691,12524548,12738781,12852856,12939256,14532005,14734534,15070733,15148369,15469984,16198290,16247472,16980960,17081991,17351640,17376779,17617734,18174154,18331714,18418051,18477460,18521620,18615013,19160488,19351716,19468300,19468302,19473992,19509060,19597481,23455478,23509069,28512243,8991084. Polo-like kinase proteins act by binding and phosphorylating proteins that are already phosphorylated on a specific motif recognized by the POLO box domains11202906,12207013,12447691,12524548,12738781,12852856,12939256,14532005,14734534,15070733,15148369,15469984,16198290,16247472,16980960,17081991,17351640,17376779,17617734,18174154,18331714,18418051,18477460,18521620,18615013,19160488,19351716,19468300,19468302,19473992,19509060,19597481,23455478,23509069,28512243,8991084. Phosphorylates BORA, BUB1B/BUBR1, CCNB1, CDC25C, CEP55, ECT2, ERCC6L, FBXO5/EMI1, FOXM1, KIF20A/MKLP2, CENPU, NEDD1, NINL, NPM1, NUDC, PKMYT1/MYT1, KIZ, MRE11, PPP1R12A/MYPT1, POLQ, PRC1, RACGAP1/CYK4, RAD51, RHNO1, SGO1, STAG2/SA2, TEX14, TOPORS, p73/TP73, TPT1, WEE1 and HNRNPU11202906,12207013,12447691,12524548,12738781,12852856,12939256,14532005,14734534,15070733,15148369,15469984,16198290,16247472,16980960,17081991,17218258,17351640,17376779,17617734,18174154,18331714,18418051,18477460,18521620,18615013,19160488,19351716,19468300,19468302,19473992,19509060,19597481,22325354,23455478,23509069,25986610,26811421,28512243,37440612,37674080,8991084. Plays a key role in centrosome functions and the assembly of bipolar spindles by phosphorylating KIZ, NEDD1 and NINL16980960,19509060. NEDD1 phosphorylation promotes subsequent targeting of the gamma-tubulin ring complex (gTuRC) to the centrosome, an important step for spindle formation19509060. Phosphorylation of NINL component of the centrosome leads to NINL dissociation from other centrosomal proteins12852856. Involved in mitosis exit and cytokinesis by phosphorylating CEP55, ECT2, KIF20A/MKLP2, CENPU, PRC1 and RACGAP112939256,16247472,17351640,19468300,19468302. Recruited at the central spindle by phosphorylating and docking PRC1 and KIF20A/MKLP2; creates its own docking sites on PRC1 and KIF20A/MKLP2 by mediating phosphorylation of sites subsequently recognized by the POLO box domains12939256,17351640. Phosphorylates RACGAP1, thereby creating a docking site for the Rho GTP exchange factor ECT2 that is essential for the cleavage furrow formation19468300,19468302. Promotes the central spindle recruitment of ECT216247472. Plays a central role in G2/M transition of mitotic cell cycle by phosphorylating CCNB1, CDC25C, FOXM1, CENPU, PKMYT1/MYT1, PPP1R12A/MYPT1 and WEE111202906,12447691,12524548,19160488. Part of a regulatory circuit that promotes the activation of CDK1 by phosphorylating the positive regulator CDC25C and inhibiting the negative regulators WEE1 and PKMYT1/MYT111202906. Also acts by mediating phosphorylation of cyclin-B1 (CCNB1) on centrosomes in prophase12447691,12524548. Phosphorylates FOXM1, a key mitotic transcription regulator, leading to enhance FOXM1 transcriptional activity19160488. Involved in kinetochore functions and sister chromatid cohesion by phosphorylating BUB1B/BUBR1, FBXO5/EMI1 and STAG2/SA215148369,15469984,17376779,18331714. PLK1 is high on non-attached kinetochores suggesting a role of PLK1 in kinetochore attachment or in spindle assembly checkpoint (SAC) regulation17617734. Required for kinetochore localization of BUB1B17376779. Regulates the dissociation of cohesin from chromosomes by phosphorylating cohesin subunits such as STAG2/SA2 (By similarity). Phosphorylates SGO1: required for spindle pole localization of isoform 3 of SGO1 and plays a role in regulating its centriole cohesion function18331714. Mediates phosphorylation of FBXO5/EMI1, a negative regulator of the APC/C complex during prophase, leading to FBXO5/EMI1 ubiquitination and degradation by the proteasome15148369,15469984. Acts as a negative regulator of p53 family members: phosphorylates TOPORS, leading to inhibit the sumoylation of p53/TP53 and simultaneously enhance the ubiquitination and subsequent degradation of p53/TP5319473992. Phosphorylates the transactivation domain of the transcription factor p73/TP73, leading to inhibit p73/TP73-mediated transcriptional activation and pro-apoptotic functions. Phosphorylates BORA, and thereby promotes the degradation of BORA18521620. Contributes to the regulation of AURKA function18615013,18662541. Also required for recovery after DNA damage checkpoint and entry into mitosis18615013,18662541. Phosphorylates MISP, leading to stabilization of cortical and astral microtubule attachments required for proper spindle positioning23509069. Together with MEIKIN, acts as a regulator of kinetochore function during meiosis I: required both for mono-orientation of kinetochores on sister chromosomes and protection of centromeric cohesin from separase-mediated cleavage (By similarity). Phosphorylates CEP68 and is required for its degradation25503564. Regulates nuclear envelope breakdown during prophase by phosphorylating DCTN1 resulting in its localization in the nuclear envelope20679239. Phosphorylates the heat shock transcription factor HSF1, promoting HSF1 nuclear translocation upon heat shock15661742. Phosphorylates HSF1 also in the early mitotic period; this phosphorylation regulates HSF1 localization to the spindle pole, the recruitment of the SCF(BTRC) ubiquitin ligase complex induicing HSF1 degradation, and hence mitotic progression18794143. Regulates mitotic progression by phosphorylating RIOK221880710. Through the phosphorylation of DZIP1 regulates the localization during mitosis of the BBSome, a ciliary protein complex involved in cilium biogenesis27979967. Regulates DNA repair during mitosis by mediating phosphorylation of POLQ and RHNO1, thereby promoting POLQ recruitment to DNA damage sites37440612,37674080. Phosphorylates ATXN10 which may play a role in the regulation of cytokinesis and may stimulate the proteasome-mediated degradation of ATXN1021857149
Quoted from UniProt’s FUNCTION annotation for P53350 (reviewed). The superscript numbers are UniProt’s own PubMed citations, kept in the sentence and in order, each linking to the paper it names.
What it acts with
STRING’s highest-confidence human functional partners. The combined score mixes several kinds of evidence, so each channel is shown separately — a partner supported by experiment is a different claim from one supported only by text mining, and for a receptor this is where its coupling appears as evidence rather than as assertion.
Where it sits in the cell
UniProt, curated Nucleus · Chromosome, centromere, kinetochore · Cytoplasm, cytoskeleton, microtubule organizing center, centrosome · Cytoplasm, cytoskeleton, spindle · Midbody
Expression by cell type
Single cell type RNA, the 12 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.
- Late primary spermatocytes180.3 nCPM
- Early spermatids110.7 nCPM
- Monocyte progenitors108.1 nCPM
- Extravillous trophoblasts58.9 nCPM
- Enteric transient amplifying cells55.1 nCPM
- Migrating cytotrophoblasts51.4 nCPM
- Esophageal basal cells41.5 nCPM
- Erythrocyte progenitors39.7 nCPM
- Megakaryocyte progenitors36.9 nCPM
- Cytotrophoblasts36.7 nCPM
- Hofbauer cells32.1 nCPM
- Paneth cells30.9 nCPM
Expression by tissue
The tissues this gene is enriched in, by consensus RNA. A tissue absent from this list is one the Atlas does not call specific for this gene, which is not the same as absent from it.
- lymphoid tissue40.9 nTPM
- testis31.5 nTPM
- bone marrow30.2 nTPM
IV · Evidence
Every measurement at this target
Each row links to the ChEMBL assay it came from.
Functional readouts 1
IC₅₀, EC₅₀, AC₅₀ and potency. Assay-dependent, and not interchangeable with a binding constant.
| Target | Class | Type | Value (nM) | pX | Organism | Assay |
|---|---|---|---|---|---|---|
| Serine/threonine-protein kinase PLK1 | Enzymes | Potency | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL3215278 |
Other measurements 4
Everything else ChEMBL recorded for this compound — percentage inhibition, efficacy, half-life, cytotoxicity. Reported in the assay's own units, which is why no value is converted here.
| Target | Class | Type | Value (nM) | pX | Organism | Assay |
|---|---|---|---|---|---|---|
| Serine/threonine-protein kinase PLK1 | Enzymes | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1052115 |
| Serine/threonine-protein kinase PLK1 | Enzymes | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1052115 |
| Serine/threonine-protein kinase PLK1 | Enzymes | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1052115 |
| Serine/threonine-protein kinase PLK1 | Enzymes | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1052115 |