Details of the Target

General Information of Target

Target ID LDTP05246
Target Name Cyclin-dependent kinase 16 (CDK16)
Gene Name CDK16
Gene ID 5127
Synonyms
PCTAIRE1; PCTK1; Cyclin-dependent kinase 16; EC 2.7.11.22; Cell division protein kinase 16; PCTAIRE-motif protein kinase 1; Serine/threonine-protein kinase PCTAIRE-1
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MDRMKKIKRQLSMTLRGGRGIDKTNGAPEQIGLDESGGGGGSDPGEAPTRAAPGELRSAR
GPLSSAPEIVHEDLKMGSDGESDQASATSSDEVQSPVRVRMRNHPPRKISTEDINKRLSL
PADIRLPEGYLEKLTLNSPIFDKPLSRRLRRVSLSEIGFGKLETYIKLDKLGEGTYATVY
KGKSKLTDNLVALKEIRLEHEEGAPCTAIREVSLLKDLKHANIVTLHDIIHTEKSLTLVF
EYLDKDLKQYLDDCGNIINMHNVKLFLFQLLRGLAYCHRQKVLHRDLKPQNLLINERGEL
KLADFGLARAKSIPTKTYSNEVVTLWYRPPDILLGSTDYSTQIDMWGVGCIFYEMATGRP
LFPGSTVEEQLHFIFRILGTPTEETWPGILSNEEFKTYNYPKYRAEALLSHAPRLDSDGA
DLLTKLLQFEGRNRISAEDAMKHPFFLSLGERIHKLPDTTSIFALKEIQLQKEASLRSSS
MPDSGRPAFRVVDTEF
Target Bioclass
Enzyme
Family
Protein kinase superfamily, CMGC Ser/Thr protein kinase family, CDC2/CDKX subfamily
Subcellular location
Cytoplasm
Function
Protein kinase that plays a role in vesicle-mediated transport processes and exocytosis. Regulates GH1 release by brain neurons. Phosphorylates NSF, and thereby regulates NSF oligomerization. Required for normal spermatogenesis. Regulates neuron differentiation and dendrite development. Plays a role in the regulation of insulin secretion in response to changes in blood glucose levels. Can phosphorylate CCNY at 'Ser-336' (in vitro).
Uniprot ID
Q00536
Ensemble ID
ENST00000276052.10
HGNC ID
HGNC:8749
ChEMBL ID
CHEMBL4597

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
TE8 SNV: p.A51V .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 10 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
STPyne
 Probe Info  		K143(5.72); K194(8.12); K311(10.00)  LDD0277  [1]
m-APA
 Probe Info  		11.63  LDD0403  [2]
BTD
 Probe Info  		C277(1.54); C206(0.79)  LDD2140  [3]
AHL-Pu-1
 Probe Info  		C206(3.04)  LDD0169  [4]
Acrolein
 Probe Info  		N.A.  LDD0221  [5]
ATP probe
 Probe Info  		K288(0.00); K194(0.00)  LDD0199  [6]
4-Iodoacetamidophenylacetylene
 Probe Info  		N.A.  LDD0038  [7]
IA-alkyne
 Probe Info  		N.A.  LDD0036  [7]
Crotonaldehyde
 Probe Info  		N.A.  LDD0219  [5]
Methacrolein
 Probe Info  		N.A.  LDD0218  [5]
PAL-AfBPP Probe
Click To Hide/Show 3 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C056
 Probe Info  		26.35  LDD1753  [8]
C391
 Probe Info  		41.36  LDD2050  [8]
STS-1
 Probe Info  		N.A.  LDD0136  [9]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0026  4SU-RNA+native RNA HEK-293T C206(3.04)  LDD0169  [4]
 LDCM0156  Aniline NCI-H1299 11.63  LDD0403  [2]
 LDCM0108  Chloroacetamide HeLa N.A.  LDD0222  [5]
 LDCM0625  F8 Ramos C206(1.32)  LDD2187  [10]
 LDCM0572  Fragment10 Ramos C206(7.77)  LDD2189  [10]
 LDCM0573  Fragment11 Ramos C206(1.09)  LDD2190  [10]
 LDCM0575  Fragment13 Ramos C206(1.04)  LDD2192  [10]
 LDCM0576  Fragment14 Ramos C206(1.82)  LDD2193  [10]
 LDCM0579  Fragment20 Ramos C206(1.87)  LDD2194  [10]
 LDCM0580  Fragment21 Ramos C206(1.57)  LDD2195  [10]
 LDCM0582  Fragment23 Ramos C206(0.54)  LDD2196  [10]
 LDCM0578  Fragment27 Ramos C206(0.80)  LDD2197  [10]
 LDCM0586  Fragment28 Ramos C206(0.68)  LDD2198  [10]
 LDCM0588  Fragment30 Ramos C206(1.24)  LDD2199  [10]
 LDCM0589  Fragment31 Ramos C206(0.63)  LDD2200  [10]
 LDCM0468  Fragment33 Ramos C206(2.60)  LDD2202  [10]
 LDCM0596  Fragment38 Ramos C206(1.21)  LDD2203  [10]
 LDCM0566  Fragment4 Ramos C206(3.25)  LDD2184  [10]
 LDCM0610  Fragment52 Ramos C206(1.42)  LDD2204  [10]
 LDCM0614  Fragment56 Ramos C206(0.69)  LDD2205  [10]
 LDCM0107  IAA HeLa N.A.  LDD0221  [5]
 LDCM0023  KB03 Ramos C206(3.41)  LDD2183  [10]
 LDCM0024  KB05 Ramos C206(2.73)  LDD2185  [10]
 LDCM0109  NEM HeLa N.A.  LDD0223  [5]
 LDCM0546  Nucleophilic fragment 40 MDA-MB-231 C277(1.54); C206(0.79)  LDD2140  [3]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Transcription factor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Zinc finger and BTB domain-containing protein 14 (ZBTB14) Krueppel C2H2-type zinc-finger protein family O43829
Other
Click To Hide/Show 4 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
G1/S-specific cyclin-D3 (CCND3) Cyclin family P30281
Cyclin-Y-like protein 1 (CCNYL1) Cyclin family Q8N7R7
Protein transport protein Sec23A (SEC23A) SEC23/SEC24 family Q15436
Amyloid protein-binding protein 2 (APPBP2) . Q92624

The Drug(s) Related To This Target

Approved
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Fostamatinib Small molecular drug DB12010
Investigative
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
(2z3e)-23'-biindole-2'3(1h1'h)-dione 3-{O-[(3r)-34-dihydroxybutyl]Oxime} . DB07766

References

1 A Paal-Knorr agent for chemoproteomic profiling of targets of isoketals in cells. Chem Sci. 2021 Oct 15;12(43):14557-14563. doi: 10.1039/d1sc02230j. eCollection 2021 Nov 10.
Mass spectrometry data entry: PXD028270
2 Quantitative and Site-Specific Chemoproteomic Profiling of Targets of Acrolein. Chem Res Toxicol. 2019 Mar 18;32(3):467-473. doi: 10.1021/acs.chemrestox.8b00343. Epub 2019 Jan 15.
3 Nucleophilic covalent ligand discovery for the cysteine redoxome. Nat Chem Biol. 2023 Nov;19(11):1309-1319. doi: 10.1038/s41589-023-01330-5. Epub 2023 May 29.
Mass spectrometry data entry: PXD039908 , PXD029761
4 Chemoproteomic capture of RNA binding activity in living cells. Nat Commun. 2023 Oct 7;14(1):6282. doi: 10.1038/s41467-023-41844-z.
Mass spectrometry data entry: PXD044625
5 ACR-Based Probe for the Quantitative Profiling of Histidine Reactivity in the Human Proteome. J Am Chem Soc. 2023 Mar 8;145(9):5252-5260. doi: 10.1021/jacs.2c12653. Epub 2023 Feb 27.
6 Targeted Proteomic Approaches for Proteome-Wide Characterizations of the AMP-Binding Capacities of Kinases. J Proteome Res. 2022 Aug 5;21(8):2063-2070. doi: 10.1021/acs.jproteome.2c00225. Epub 2022 Jul 12.
7 Enhancing Cysteine Chemoproteomic Coverage through Systematic Assessment of Click Chemistry Product Fragmentation. Anal Chem. 2022 Mar 8;94(9):3800-3810. doi: 10.1021/acs.analchem.1c04402. Epub 2022 Feb 23.
Mass spectrometry data entry: PXD028853
8 Large-scale chemoproteomics expedites ligand discovery and predicts ligand behavior in cells. Science. 2024 Apr 26;384(6694):eadk5864. doi: 10.1126/science.adk5864. Epub 2024 Apr 26.
Mass spectrometry data entry: PXD041587
9 Design and synthesis of minimalist terminal alkyne-containing diazirine photo-crosslinkers and their incorporation into kinase inhibitors for cell- and tissue-based proteome profiling. Angew Chem Int Ed Engl. 2013 Aug 12;52(33):8551-6. doi: 10.1002/anie.201300683. Epub 2013 Jun 10.
10 Site-specific quantitative cysteine profiling with data-independent acquisition-based mass spectrometry. Methods Enzymol. 2023;679:295-322. doi: 10.1016/bs.mie.2022.07.037. Epub 2022 Sep 7.
Mass spectrometry data entry: PXD027578