Plk1(PBD)

Polo-like kinase 1 polo-box domain

Reviewed UniProt entries for Plk1(PBD) and its protein partners


UniProt code UniProt Name Protein Name Gene Name Organism Length
Q2TA25 PLK1_BOVIN Serine/threonine-protein kinase PLK1 (EC 2.7.11.21) (Polo-like kinase 1) (PLK-1) PLK1 Bos taurus (Bovine) 602
P34331 PLK1_CAEEL Serine/threonine-protein kinase plk-1 (EC 2.7.11.21) (Polo-like kinase 1) plk-1 plc1 C14B9.4 Caenorhabditis elegans 649
P53350 PLK1_HUMAN Serine/threonine-protein kinase PLK1 (EC 2.7.11.21) (Polo-like kinase 1) (PLK-1) (Serine/threonine-protein kinase 13) (STPK13) PLK1 PLK Homo sapiens (Human) 603
Q07832 PLK1_MOUSE Serine/threonine-protein kinase PLK1 (EC 2.7.11.21) (Polo-like kinase 1) (PLK-1) (Serine/threonine-protein kinase 13) (STPK13) Plk1 Plk Mus musculus (Mouse) 603
Q62673 PLK1_RAT Serine/threonine-protein kinase PLK1 (EC 2.7.11.21) (Polo-like kinase 1) (PLK-1) Plk1 Plk Rattus norvegicus (Rat) 603
P70032 PLK1_XENLA Serine/threonine-protein kinase PLK1 (EC 2.7.11.21) (Plx1) (Polo-like kinase 1) (PLK-1) plk1 plx1 Xenopus laevis (African clawed frog) 598
P62205 PLK1_XENTR Serine/threonine-protein kinase PLK1 (EC 2.7.11.21) (Plx1) (Polo-like kinase 1) (PLK-1) plk1 Xenopus tropicalis (Western clawed frog) (Silurana tropicalis) 598

Small molecules tested in Plk1(PBD) binding assays:

2 datapoints for 2 distinct small molecules


Name Poloxime
Affinity None
Assay description None
-- Direct single protein target assigned: PLK1_HUMAN (Expert curation) --
DOI http://pubs.acs.org/doi/abs/10.1021/cb3004379
Doc title Thymoquinone Blocks pSer/pThr Recognition by Plk1 Polo-Box Domain As a Phosohate Mimic
PDB 4H71 - (PXE)

Name Thymoquinone
Affinity None
Assay description None
-- Direct single protein target assigned: PLK1_HUMAN (Expert curation) --
DOI http://pubs.acs.org/doi/abs/10.1021/cb3004379
Doc title Thymoquinone Blocks pSer/pThr Recognition by Plk1 Polo-Box Domain As a Phosohate Mimic
PDB 4HCO - (IMW)

40 PDB entries for Plk1(PBD) and its protein partners


1Q4K
The crystal structure of the human polo-like kinase-1 polo box domain and its phospho-peptide complex.

Entity type Code Description
polypeptide(L) P53350 Serine/threonine-protein kinase PLK
polypeptide(L) 1Q4K Phospho-peptide sequence Met.Gln.Ser.pThr.Pro.Leu

1Q4O
The crystal structure of the human polo-like kinase-1 polo box domain and its phospho-peptide complex.

Entity type Code Description
polypeptide(L) P53350 Serine/threonine-protein kinase PLK

1UMW
The Molecular Basis for Phosphodependent Substrate Targeting and Regulation of Plks by the Polo-Box Domain

Entity type Code Description
polypeptide(L) P53350 SERINE/THREONINE-PROTEIN KINASE PLK
polypeptide(L) 1UMW PEPTIDE

2OGQ
Molecular and structural basis of polo-like kinase 1 substrate recognition: Implications in centrosomal localization.

Entity type Code Description
polypeptide(L) P53350 Serine/threonine-protein kinase PLK1

2OJX
Molecular and structural basis of polo-like kinase 1 substrate recognition: Implications in centrosomal localization.

Entity type Code Description
polypeptide(L) P53350 Serine/threonine-protein kinase PLK1
polypeptide(L) 2OJX Synthetic peptide

2OU7
Structure of the catalytic domain of human polo-like kinase 1.

Entity type Code Description
polypeptide(L) P53350 Serine/threonine-protein kinase PLK1
Ligand ANP PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER

2OWB
Structure of the catalytic domain of human polo-like kinase 1.

Entity type Code Description
polypeptide(L) P53350 Serine/threonine-protein kinase PLK1
Ligand 626 4-(4-METHYLPIPERAZIN-1-YL)-N-[5-(2-THIENYLACETYL)-1,5-DIHYDROPYRROLO[3,4-C]PYRAZOL-3-YL]BENZAMIDE

2RKU
Selectivity-determining residues in Plk1.

Entity type Code Description
polypeptide(L) P53350 Serine/threonine-protein kinase PLK1
Ligand R78 4-{[(7R)-8-CYCLOPENTYL-7-ETHYL-5-METHYL-6-OXO-5,6,7,8-TETRAHYDROPTERIDIN-2-YL]AMINO}-3-METHOXY-N-(1-METHYLPIPERIDIN-4-YL)BENZAMIDE
Ligand TLA L(+)-TARTARIC ACID
Ligand SRT S,R MESO-TARTARIC ACID
Ligand TAR D(-)-TARTARIC ACID

2V5Q
Structure Pf Wild-Type Plk-1 Kinase Domain in Complex with a Selective Darpin

Entity type Code Description
polypeptide(L) 2V5Q SERINE/THREONINE-PROTEIN KINASE PLK1
polypeptide(L) P53350 SERINE/THREONINE-PROTEIN KINASE PLK1
polypeptide(L) 2V5Q DESIGN ANKYRIN REPEAT PROTEIN

2YAC
Nms-P937, a 4,5-Dihydro-1H-Pyrazolo[4,3-H]Quinazoline Derivative as Potent and Selective Polo-Like Kinase 1 Inhibitor.

Entity type Code Description
polypeptide(L) P53350 SERINE/THREONINE-PROTEIN KINASE PLK1
Ligand 937 1-(2-HYDROXYETHYL)-8-[[5-(4-METHYLPIPERAZIN-1-YL)-2-(TRIFLUOROMETHOXY)PHENYL]AMINO]-4,5-DIHYDROPYRIMIDO[5,4-G]INDAZOLE-3-CARBOXAMIDE
Ligand TLA L(+)-TARTARIC ACID

3BZI
Molecular and structural basis of polo-like kinase 1 substrate recognition: Implications in centrosomal localization.

Entity type Code Description
polypeptide(L) P53350 Serine/threonine-protein kinase PLK1
polypeptide(L) P30307 9 mer peptide from M-phase inducer phosphatase 3

3C5L
Structural and functional analyses of minimal phosphopeptides targeting the polo-box domain of polo-like kinase 1.

Entity type Code Description
polypeptide(L) P53350 Serine/threonine-protein kinase PLK1
polypeptide(L) 3C5L Peptide

3FC2
BI 6727, A Polo-like Kinase Inhibitor with Improved Pharmacokinetic Profile and Broad Antitumor Activity.

Entity type Code Description
polypeptide(L) P53350 Serine/threonine-protein kinase PLK1
Ligand IBI N-{TRANS-4-[4-(CYCLOPROPYLMETHYL)PIPERAZIN-1-YL]CYCLOHEXYL}-4-{[(7R)-7-ETHYL-5-METHYL-8-(1-METHYLETHYL)-6-OXO-5,6,7,8-TETRAHYDROPTERIDIN-2-YL]AMINO}-3-METHOXYBENZAMIDE
Ligand PEG DI(HYDROXYETHYL)ETHER

3FVH
Structural and functional analyses of minimal phosphopeptides targeting the polo-box domain of polo-like kinase 1

Entity type Code Description
polypeptide(L) P53350 Serine/threonine-protein kinase PLK1
polypeptide(L) 3FVH Acetyl-Leu-His-Ser-phosphoThr-Ala-NH2 peptide

3HIH
Structural and functional analyses of minimal phosphopeptides targeting the polo-box domain of polo-like kinase 1.

Entity type Code Description
polypeptide(L) P53350 Serine/threonine-protein kinase PLK1

3HIK
Structural and functional analyses of minimal phosphopeptides targeting the polo-box domain of polo-like kinase 1.

Entity type Code Description
polypeptide(L) P53350 Serine/threonine-protein kinase PLK1
polypeptide(L) None Pentamer phosphopeptide

3KB7
Identification of 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivatives as a new class of orally and selective Polo-like kinase 1 inhibitors

Entity type Code Description
polypeptide(L) P53350 Serine/threonine-protein kinase PLK1
Ligand 071 8-{[2-METHOXY-5-(4-METHYLPIPERAZIN-1-YL)PHENYL]AMINO}-1-METHYL-4,5-DIHYDRO-1H-PYRAZOLO[4,3-H]QUINAZOLINE-3-CARBOXAMIDE
Ligand TLA L(+)-TARTARIC ACID

3P2W
From crystal packing to molecular recognition: prediction and discovery of a binding site on the surface of polo-like kinase 1

Entity type Code Description
polypeptide(L) P53350 Serine/threonine-protein kinase PLK1

3P2Z
From crystal packing to molecular recognition: prediction and discovery of a binding site on the surface of polo-like kinase 1

Entity type Code Description
polypeptide(L) P53350 Serine/threonine-protein kinase PLK1
polypeptide(L) 3P2Z phosphopeptide

3P34
From crystal packing to molecular recognition: prediction and discovery of a binding site on the surface of polo-like kinase 1

Entity type Code Description
polypeptide(L) P53350 Serine/threonine-protein kinase PLK1
polypeptide(L) 3P34 phosphopeptide

3P35
From crystal packing to molecular recognition: prediction and discovery of a binding site on the surface of polo-like kinase 1

Entity type Code Description
polypeptide(L) P53350 Serine/threonine-protein kinase PLK1
polypeptide(L) 3P35 phosphopeptide

3P36
From crystal packing to molecular recognition: prediction and discovery of a binding site on the surface of polo-like kinase 1

Entity type Code Description
polypeptide(L) P53350 Serine/threonine-protein kinase PLK1
polypeptide(L) 3P36 phosphopeptide

3P37
From crystal packing to molecular recognition: prediction and discovery of a binding site on the surface of polo-like kinase 1

Entity type Code Description
polypeptide(L) P53350 Serine/threonine-protein kinase PLK1
polypeptide(L) 3P37 phosphopeptide

3Q1I
From crystal packing to molecular recognition: prediction and discovery of a binding site on the surface of polo-like kinase 1

Entity type Code Description
polypeptide(L) P53350 Serine/threonine-protein kinase PLK1
polypeptide(L) O14776 peptide from Transcription elongation regulator 1
Ligand 1PE PENTAETHYLENE GLYCOL
Ligand PEG DI(HYDROXYETHYL)ETHER
Ligand PG0 2-(2-METHOXYETHOXY)ETHANOL

3RQ7
Serendipitous alkylation of a Plk1 ligand uncovers a new binding channel.

Entity type Code Description
polypeptide(L) P53350 Serine/threonine-protein kinase PLK1
polypeptide(L) 3RQ7 C6H5(CH2)8-derivatized peptide inhibitor

3THB
Discovery of a Potent and Orally Bioavailable Benzolactam-Derived Inhibitor of Polo-Like Kinase 1 (MLN0905).

Entity type Code Description
polypeptide(L) P53350 Serine/threonine-protein kinase PLK1
Ligand 3TA 9-CHLORO-2-({5-[3-(DIMETHYLAMINO)PROPYL]-2-METHYLPYRIDIN-3-YL}AMINO)-5,7-DIHYDRO-6H-PYRIMIDO[5,4-D][1]BENZAZEPINE-6-THIONE

4A4L
5-(2-Amino-Pyrimidin-4-Yl)-1H-Pyrrole and 2-(2-Amino-Pyrimidin-4-Yl)-1,5,6,7-Tetrahydro-Pyrrolo[3,2-C]Pyridin-4-One Derivatives as New Classes of Selective and Orally Available Polo-Like Kinase 1 Inhibitors.

Entity type Code Description
polypeptide(L) P53350 SERINE/THREONINE-PROTEIN KINASE PLK1
Ligand TLA L(+)-TARTARIC ACID
Ligand 939 1-METHYL-5-(2-{[5-(4-METHYLPIPERAZIN-1-YL)-2-(TRIFLUOROMETHOXY)PHENYL]AMINO}PYRIMIDIN-4-YL)-1H-PYRROLE-3-CARBOXAMIDE

4A4O
5-(2-Amino-Pyrimidin-4-Yl)-1H-Pyrrole and 2-(2-Amino-Pyrimidin-4-Yl)-1,5,6,7-Tetrahydro-Pyrrolo[3,2-C]Pyridin-4-One Derivatives as New Classes of Selective and Orally Available Polo-Like Kinase 1 Inhibitors.

Entity type Code Description
polypeptide(L) P53350 SERINE/THREONINE-PROTEIN KINASE PLK1
Ligand TLA L(+)-TARTARIC ACID
Ligand 664 1-METHYL-2-(2-{[5-(4-METHYLPIPERAZIN-1-YL)-2-(TRIFLUOROMETHOXY)PHENYL]AMINO}PYRIMIDIN-4-YL)-1,5,6,7-TETRAHYDRO-4H-PYRROLO[3,2-C]PYRIDIN-4-ONE

4DFW
Oxime-based Post Solid-phase Peptide Diversification: Identification of High Affinity Polo-like Kinase 1 (Plk1) Polo-box Domain Binding Peptides

Entity type Code Description
polypeptide(L) P53350 Serine/threonine-protein kinase PLK1
polypeptide(L) 4DFW Peptide

4E67
Using ligand-mapping simulations to design a ligand selectively targeting a cryptic surface pocket of polo-like kinase 1.

Entity type Code Description
polypeptide(L) P53350 Serine/threonine-protein kinase PLK1
polypeptide(L) 4E67 hydrocinnamoyl-derivatized PLHSpTA peptide

4E9C
High-throughput interrogation of ligand binding mode using a fluorescence-based assay.

Entity type Code Description
polypeptide(L) P53350 Serine/threonine-protein kinase PLK1
polypeptide(L) 4E9C LDPPLHSpTA phosphopeptide
Ligand PG0 2-(2-METHOXYETHOXY)ETHANOL

4E9D
High-throughput interrogation of ligand binding mode using a fluorescence-based assay.

Entity type Code Description
polypeptide(L) P53350 Serine/threonine-protein kinase PLK1
polypeptide(L) 4E9D 3-(1-benzothiophen-2-yl)propanoyl-derivatized DPPLHSpTA peptide

4H5X
Thymoquinone Blocks pSer/pThr Recognition by Plk1 Polo-Box Domain As a Phosphate Mimic

Entity type Code Description
polypeptide(L) P53350 Serine/threonine-protein kinase PLK1

4H71
Thymoquinone Blocks pSer/pThr Recognition by Plk1 Polo-Box Domain As a Phosphate Mimic

Entity type Code Description
polypeptide(L) P53350 Serine/threonine-protein kinase PLK1
Ligand PXE 2-METHYL-5-(1-METHYLETHYL)CYCLOHEXA-2,5-DIENE-1,4-DIONE 1-OXIME

4HAB
Development of cyclic peptomer inhibitors targeting the polo-box domain of polo-like kinase 1.

Entity type Code Description
polypeptide(L) P53350 Serine/threonine-protein kinase PLK1
polypeptide(L) 4HAB PL-49
Ligand CXS 3-CYCLOHEXYL-1-PROPYLSULFONIC ACID

4HCO
Thymoquinone Blocks pSer/pThr Recognition by Plk1 Polo-Box Domain As a Phosphate Mimic

Entity type Code Description
polypeptide(L) P53350 Serine/threonine-protein kinase PLK1
Ligand IMW 2-METHYL-5-(1-METHYLETHYL)CYCLOHEXA-2,5-DIENE-1,4-DIONE

4HY2
Development of cyclic peptomer inhibitors targeting the polo-box domain of polo-like kinase 1.

Entity type Code Description
polypeptide(L) P53350 Serine/threonine-protein kinase PLK1
polypeptide(L) 4HY2 PL-42

4J52
Discovery of TAK-960: An orally available small molecule inhibitor of polo-like kinase 1 (PLK1).

Entity type Code Description
polypeptide(L) P53350 Serine/threonine-protein kinase PLK1
Ligand 1J3 4-{[(7R)-9-CYCLOPENTYL-7-ETHENYL-7-FLUORO-5-METHYL-6-OXO-6,7,8,9-TETRAHYDRO-5H-PYRIMIDO[4,5-B][1,4]DIAZEPIN-2-YL]AMINO}-3-METHOXY-N-(4-METHYLPIPERAZIN-1-YL)BENZAMIDE

4J53
Discovery of TAK-960: An orally available small molecule inhibitor of polo-like kinase 1 (PLK1).

Entity type Code Description
polypeptide(L) P53350 Serine/threonine-protein kinase PLK1
Ligand 1J4 4-[(9-CYCLOPENTYL-7,7-DIFLUORO-5-METHYL-6-OXO-6,7,8,9-TETRAHYDRO-5H-PYRIMIDO[4,5-B][1,4]DIAZEPIN-2-YL)AMINO]-2-FLUORO-5-METHOXY-N-(1-METHYLPIPERIDIN-4-YL)BENZAMIDE

4MLU
Peptide-Based Inhibitors of Plk1 Polo-box Domain Containing Mono-anionic Phosphothreonine Esters and Their Pivaloyloxymethyl Prodrugs.

Entity type Code Description
polypeptide(L) P53350 Serine/threonine-protein kinase PLK1
polypeptide(L) 4MLU Phosphothreonine ester-containing peptide