Details of the Target

General Information of Target

Target ID LDTP04097
Target Name Cyclin-dependent kinase inhibitor 1B (CDKN1B)
Gene Name CDKN1B
Gene ID 1027
Synonyms
KIP1; p27; Cyclin-dependent kinase inhibitor 1B; Cyclin-dependent kinase inhibitor p27; p27Kip1
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MSNVRVSNGSPSLERMDARQAEHPKPSACRNLFGPVDHEELTRDLEKHCRDMEEASQRKW
NFDFQNHKPLEGKYEWQEVEKGSLPEFYYRPPRPPKGACKVPAQESQDVSGSRPAAPLIG
APANSEDTHLVDPKTDPSDSQTGLAEQCAGIRKRPATDDSSTQNKRANRTEENVSDGSPN
AGSVEQTPKKPGLRRRQT
Target Type
Literature-reported
Target Bioclass
Other
Family
CDI family
Subcellular location
Nucleus
Function
Important regulator of cell cycle progression. Inhibits the kinase activity of CDK2 bound to cyclin A, but has little inhibitory activity on CDK2 bound to SPDYA. Involved in G1 arrest. Potent inhibitor of cyclin E- and cyclin A-CDK2 complexes. Forms a complex with cyclin type D-CDK4 complexes and is involved in the assembly, stability, and modulation of CCND1-CDK4 complex activation. Acts either as an inhibitor or an activator of cyclin type D-CDK4 complexes depending on its phosphorylation state and/or stoichometry.
TTD ID
T14006
Uniprot ID
P46527
DrugMap ID
TTLGFVW
Ensemble ID
ENST00000228872.9
HGNC ID
HGNC:1785
ChEMBL ID
CHEMBL3758070

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 8 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
4-Iodoacetamidophenylacetylene
 Probe Info  		N.A.  LDD0038  [1]
IA-alkyne
 Probe Info  		N.A.  LDD0162  [2]
Lodoacetamide azide
 Probe Info  		N.A.  LDD0037  [1]
IPM
 Probe Info  		N.A.  LDD0025  [3]
NAIA_5
 Probe Info  		N.A.  LDD2224  [4]
TFBX
 Probe Info  		N.A.  LDD0027  [3]
DBIA
 Probe Info  		C29(0.06)  LDD2236  [5]
Methacrolein
 Probe Info  		N.A.  LDD0218  [6]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0634  CY-0357 Hep-G2 C148(0.50)  LDD2228  [4]
 LDCM0131  RA190 MM1.R C148(1.09)  LDD0304  [7]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 13 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Cullin-1 (CUL1) Cullin family Q13616
DNA replication licensing factor MCM7 (MCM7) MCM family P33993
COP9 signalosome complex subunit 5 (COPS5) Peptidase M67A family Q92905
Ribosomal protein S6 kinase alpha-1 (RPS6KA1) AGC Ser/Thr protein kinase family Q15418
Cyclin-dependent kinase 1 (CDK1) CMGC Ser/Thr protein kinase family P06493
Cyclin-dependent kinase 2 (CDK2) CMGC Ser/Thr protein kinase family P24941
Cyclin-dependent kinase 4 (CDK4) CMGC Ser/Thr protein kinase family P11802
Cyclin-dependent kinase 5 (CDK5) CMGC Ser/Thr protein kinase family Q00535
Inhibitor of nuclear factor kappa-B kinase subunit alpha (CHUK) Ser/Thr protein kinase family O15111
Tyrosine-protein kinase Lyn (LYN) Tyr protein kinase family P07948
Transforming protein RhoA (RHOA) Rho family P61586
TNF receptor-associated factor 2 (TRAF2) TNF receptor-associated factor family Q12933
S-phase kinase-associated protein 2 (SKP2) . Q13309
Transporter and channel
Click To Hide/Show 4 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
G2/mitotic-specific cyclin-B1 (CCNB1) Cyclin family P14635
G1/S-specific cyclin-D1 (CCND1) Cyclin family P24385
Importin subunit alpha-4 (KPNA3) Importin alpha family O00505
Importin subunit alpha-6 (KPNA5) Importin alpha family O15131
Transcription factor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
THAP domain-containing protein 1 (THAP1) THAP1 family Q9NVV9
Other
Click To Hide/Show 8 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Cyclin-A1 (CCNA1) Cyclin family P78396
Cyclin-A2 (CCNA2) Cyclin family P20248
G1/S-specific cyclin-D2 (CCND2) Cyclin family P30279
G1/S-specific cyclin-D3 (CCND3) Cyclin family P30281
G1/S-specific cyclin-E1 (CCNE1) Cyclin family P24864
G1/S-specific cyclin-E2 (CCNE2) Cyclin family O96020
Speedy protein A (SPDYA) Speedy/Ringo family Q5MJ70
Stathmin (STMN1) Stathmin family P16949

References

1 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
2 SP3-FAIMS Chemoproteomics for High-Coverage Profiling of the Human Cysteinome*. Chembiochem. 2021 May 14;22(10):1841-1851. doi: 10.1002/cbic.202000870. Epub 2021 Feb 18.
Mass spectrometry data entry: PXD023056 , PXD023059 , PXD023058 , PXD023057 , PXD023060
3 Chemoproteomic Profiling by Cysteine Fluoroalkylation Reveals Myrocin G as an Inhibitor of the Nonhomologous End Joining DNA Repair Pathway. J Am Chem Soc. 2021 Dec 8;143(48):20332-20342. doi: 10.1021/jacs.1c09724. Epub 2021 Nov 24.
Mass spectrometry data entry: PXD029255
4 N-Acryloylindole-alkyne (NAIA) enables imaging and profiling new ligandable cysteines and oxidized thiols by chemoproteomics. Nat Commun. 2023 Jun 15;14(1):3564. doi: 10.1038/s41467-023-39268-w.
Mass spectrometry data entry: PXD041264
5 Global profiling of phosphorylation-dependent changes in cysteine reactivity. Nat Methods. 2022 Mar;19(3):341-352. doi: 10.1038/s41592-022-01398-2. Epub 2022 Feb 28.
Mass spectrometry data entry: PXD026730
6 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.
7 Physical and Functional Analysis of the Putative Rpn13 Inhibitor RA190. Cell Chem Biol. 2020 Nov 19;27(11):1371-1382.e6. doi: 10.1016/j.chembiol.2020.08.007. Epub 2020 Aug 27.