Details of the Target

General Information of Target

Target ID LDTP03819
Target Name Serine/threonine-protein phosphatase PP1-gamma catalytic subunit (PPP1CC)
Gene Name PPP1CC
Gene ID 5501
Synonyms
Serine/threonine-protein phosphatase PP1-gamma catalytic subunit; PP-1G; EC 3.1.3.16; Protein phosphatase 1C catalytic subunit
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MADLDKLNIDSIIQRLLEVRGSKPGKNVQLQENEIRGLCLKSREIFLSQPILLELEAPLK
ICGDIHGQYYDLLRLFEYGGFPPESNYLFLGDYVDRGKQSLETICLLLAYKIKYPENFFL
LRGNHECASINRIYGFYDECKRRYNIKLWKTFTDCFNCLPIAAIVDEKIFCCHGGLSPDL
QSMEQIRRIMRPTDVPDQGLLCDLLWSDPDKDVLGWGENDRGVSFTFGAEVVAKFLHKHD
LDLICRAHQVVEDGYEFFAKRQLVTLFSAPNYCGEFDNAGAMMSVDETLMCSFQILKPAE
KKKPNATRPVTPPRGMITKQAKK
Target Bioclass
Enzyme
Family
PPP phosphatase family, PP-1 subfamily
Subcellular location
Cytoplasm
Function
Protein phosphatase that associates with over 200 regulatory proteins to form highly specific holoenzymes which dephosphorylate hundreds of biological targets. Protein phosphatase 1 (PP1) is essential for cell division, and participates in the regulation of glycogen metabolism, muscle contractility and protein synthesis. Dephosphorylates RPS6KB1. Involved in regulation of ionic conductances and long-term synaptic plasticity. May play an important role in dephosphorylating substrates such as the postsynaptic density-associated Ca(2+)/calmodulin dependent protein kinase II. Component of the PTW/PP1 phosphatase complex, which plays a role in the control of chromatin structure and cell cycle progression during the transition from mitosis into interphase. In balance with CSNK1D and CSNK1E, determines the circadian period length, through the regulation of the speed and rhythmicity of PER1 and PER2 phosphorylation. May dephosphorylate CSNK1D and CSNK1E. Dephosphorylates the 'Ser-418' residue of FOXP3 in regulatory T-cells (Treg) from patients with rheumatoid arthritis, thereby inactivating FOXP3 and rendering Treg cells functionally defective.
Uniprot ID
P36873
Ensemble ID
ENST00000335007.10
HGNC ID
HGNC:9283
ChEMBL ID
CHEMBL4438

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
CCK81 SNV: p.Y78H DBIA    Probe Info 
HCT116 SNV: p.R191Q .
IGROV1 SNV: p.D95N DBIA    Probe Info 
LNCaP clone FGC SNV: p.N131S .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 21 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
YN-4
 Probe Info  		100.00  LDD0445  [1]
BTD
 Probe Info  		C127(2.82)  LDD1699  [2]
IPM
 Probe Info  		C127(0.00); C171(0.00); C172(0.00); C140(0.00)  LDD0241  [3]
Probe 1
 Probe Info  		Y255(49.87)  LDD3495  [4]
m-APA
 Probe Info  		11.59  LDD0403  [5]
DBIA
 Probe Info  		C73(1.48)  LDD3310  [6]
AHL-Pu-1
 Probe Info  		C127(2.29)  LDD0169  [7]
HHS-475
 Probe Info  		Y70(0.59); Y137(0.68); Y255(0.89); Y134(1.07)  LDD0264  [8]
HHS-465
 Probe Info  		Y134(10.00); Y137(10.00)  LDD2237  [9]
ATP probe
 Probe Info  		K141(0.00); K238(0.00); K23(0.00); K26(0.00)  LDD0199  [10]
4-Iodoacetamidophenylacetylene
 Probe Info  		N.A.  LDD0038  [11]
IA-alkyne
 Probe Info  		C171(0.00); C140(0.00); C155(0.00); C127(0.00)  LDD0032  [12]
IPIAA_H
 Probe Info  		C245(0.00); C105(0.00); C171(0.00); C202(0.00)  LDD0030  [13]
IPIAA_L
 Probe Info  		C62(0.00); C202(0.00); C245(0.00); C127(0.00)  LDD0031  [13]
Lodoacetamide azide
 Probe Info  		N.A.  LDD0037  [11]
NHS
 Probe Info  		K147(0.00); K26(0.00); K260(0.00)  LDD0010  [14]
PF-06672131
 Probe Info  		N.A.  LDD0152  [15]
W1
 Probe Info  		C127(0.00); C202(0.00); C245(0.00); C140(0.00)  LDD0236  [3]
AOyne
 Probe Info  		4.80  LDD0443  [16]
NAIA_5
 Probe Info  		C62(0.00); C245(0.00); C105(0.00); C127(0.00)  LDD2223  [17]
TER-AC
 Probe Info  		N.A.  LDD0426  [18]
PAL-AfBPP Probe
Click To Hide/Show 6 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
FFF probe14
 Probe Info  		15.37  LDD0477  [19]
FFF probe2
 Probe Info  		6.80  LDD0463  [19]
FFF probe3
 Probe Info  		7.50  LDD0464  [19]
VE-P
 Probe Info  		N.A.  LDD0396  [20]
DA-2
 Probe Info  		N.A.  LDD0070  [21]
STS-1
 Probe Info  		N.A.  LDD0068  [22]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0524  2-Cyano-N-(2-morpholin-4-yl-ethyl)-acetamide MDA-MB-231 C62(1.29)  LDD2117  [2]
 LDCM0025  4SU-RNA DM93 C62(2.32); C171(10.47)  LDD0170  [7]
 LDCM0026  4SU-RNA+native RNA HEK-293T C127(2.29)  LDD0169  [7]
 LDCM0156  Aniline NCI-H1299 11.59  LDD0403  [5]
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C62(1.69)  LDD1702  [2]
 LDCM0625  F8 Ramos C140(0.77); C127(1.75); C62(0.95); 1.47  LDD2187  [23]
 LDCM0572  Fragment10 Ramos C140(0.56); C127(0.64); C62(0.64)  LDD2189  [23]
 LDCM0573  Fragment11 Ramos C140(0.77); C127(3.01); C62(1.96); C245(1.18)  LDD2190  [23]
 LDCM0574  Fragment12 Ramos C140(0.56); C127(0.68); C62(0.74)  LDD2191  [23]
 LDCM0575  Fragment13 Ramos C140(0.87); C127(1.04); C62(1.02)  LDD2192  [23]
 LDCM0576  Fragment14 Ramos C140(0.82); C127(0.74); C62(1.17); C245(0.67)  LDD2193  [23]
 LDCM0579  Fragment20 Ramos C140(0.53); C127(0.69); C62(0.67)  LDD2194  [23]
 LDCM0580  Fragment21 Ramos C140(0.86); C127(0.90); C62(0.99)  LDD2195  [23]
 LDCM0582  Fragment23 Ramos C140(1.03); C127(0.80); C62(1.13)  LDD2196  [23]
 LDCM0578  Fragment27 Ramos C140(0.76); C127(1.11); C62(1.00)  LDD2197  [23]
 LDCM0586  Fragment28 Ramos C140(0.64); C127(0.62); C62(0.93); C245(1.02)  LDD2198  [23]
 LDCM0588  Fragment30 Ramos C140(1.05); C127(1.14); C62(0.91)  LDD2199  [23]
 LDCM0589  Fragment31 Ramos C140(1.19); C127(1.03); C62(1.21)  LDD2200  [23]
 LDCM0590  Fragment32 Ramos C140(0.51); C127(0.82); C62(0.56)  LDD2201  [23]
 LDCM0468  Fragment33 Ramos C140(0.81); C127(1.11); C62(0.83)  LDD2202  [23]
 LDCM0596  Fragment38 Ramos C140(0.89); C127(1.38); C62(0.97)  LDD2203  [23]
 LDCM0566  Fragment4 Ramos C140(0.72); C127(0.83); C62(1.06); C245(0.32)  LDD2184  [23]
 LDCM0610  Fragment52 Ramos C140(0.89); C127(1.26); C62(1.06)  LDD2204  [23]
 LDCM0614  Fragment56 Ramos C140(1.11); C127(1.50); C62(0.86)  LDD2205  [23]
 LDCM0569  Fragment7 Ramos C140(0.59); C127(0.70); C62(1.30); C245(0.21)  LDD2186  [23]
 LDCM0571  Fragment9 Ramos C140(0.55); C127(0.60); C62(0.55)  LDD2188  [23]
 LDCM0116  HHS-0101 DM93 Y70(0.59); Y137(0.68); Y255(0.89); Y134(1.07)  LDD0264  [8]
 LDCM0117  HHS-0201 DM93 Y70(0.38); Y137(0.53); Y134(0.75); Y255(3.02)  LDD0265  [8]
 LDCM0118  HHS-0301 DM93 Y137(0.61); Y134(0.92); Y255(1.24)  LDD0266  [8]
 LDCM0119  HHS-0401 DM93 Y137(0.85); Y134(1.28); Y255(1.51)  LDD0267  [8]
 LDCM0120  HHS-0701 DM93 Y137(0.89); Y134(1.54); Y255(1.96)  LDD0268  [8]
 LDCM0022  KB02 Ramos C140(0.56); C127(0.83); C62(0.81); C245(0.16)  LDD2182  [23]
 LDCM0023  KB03 MDA-MB-231 C62(2.58)  LDD1701  [2]
 LDCM0024  KB05 COLO792 C73(1.48)  LDD3310  [6]
 LDCM0509  N-(4-bromo-3,5-dimethylphenyl)-2-nitroacetamide MDA-MB-231 C127(1.34)  LDD2102  [2]
 LDCM0497  Nucleophilic fragment 11b MDA-MB-231 C127(1.37)  LDD2090  [2]
 LDCM0506  Nucleophilic fragment 16a MDA-MB-231 C62(1.29)  LDD2099  [2]
 LDCM0512  Nucleophilic fragment 19a MDA-MB-231 C62(1.05)  LDD2105  [2]
 LDCM0521  Nucleophilic fragment 23b MDA-MB-231 C62(0.68)  LDD2114  [2]
 LDCM0522  Nucleophilic fragment 24a MDA-MB-231 C62(0.88)  LDD2115  [2]
 LDCM0526  Nucleophilic fragment 26a MDA-MB-231 C62(1.03)  LDD2119  [2]
 LDCM0532  Nucleophilic fragment 29a MDA-MB-231 C62(0.96)  LDD2125  [2]
 LDCM0541  Nucleophilic fragment 36 MDA-MB-231 C62(0.73)  LDD2134  [2]
 LDCM0211  Nucleophilic fragment 3b MDA-MB-231 C127(1.40)  LDD1700  [2]
 LDCM0552  Nucleophilic fragment 6a MDA-MB-231 C62(1.37)  LDD2146  [2]
 LDCM0559  Nucleophilic fragment 9b MDA-MB-231 C127(1.90)  LDD2153  [2]
 LDCM0627  NUDT7-COV-1 HEK-293T C127(0.92)  LDD2206  [24]
 LDCM0628  OTUB2-COV-1 HEK-293T C127(0.82)  LDD2207  [24]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 10 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
UDP-N-acetylglucosamine--peptide N-acetylglucosaminyltransferase 110 kDa subunit (OGT) Glycosyltransferase 41 family O15294
Serine/threonine-protein kinase Nek2 (NEK2) NEK Ser/Thr protein kinase family P51955
Serine/threonine-protein kinase LMTK1 (AATK) Tyr protein kinase family Q6ZMQ8
Serine/threonine-protein kinase LMTK2 (LMTK2) Tyr protein kinase family Q8IWU2
Protein phosphatase inhibitor 2 (PPP1R2) Protein phosphatase inhibitor 2 family P41236
Protein phosphatase inhibitor 2 family member B (PPP1R2B) Protein phosphatase inhibitor 2 family Q6NXS1
Protein phosphatase inhibitor 2 family member C (PPP1R2C) Protein phosphatase inhibitor 2 family O14990
Unconventional prefoldin RPB5 interactor 1 (URI1) RNA polymerase II subunit 5-mediating protein family O94763
Breast cancer type 1 susceptibility protein (BRCA1) . P38398
E3 ubiquitin-protein ligase PPP1R11 (PPP1R11) . O60927
Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Cellular tumor antigen p53 (TP53) P53 family P04637
Transcription factor
Click To Hide/Show 4 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Cysteine/serine-rich nuclear protein 1 (CSRNP1) AXUD1 family Q96S65
Cysteine/serine-rich nuclear protein 2 (CSRNP2) AXUD1 family Q9H175
Zinc finger protein 629 (ZNF629) Krueppel C2H2-type zinc-finger protein family Q9UEG4
Estrogen receptor (ESR1) Nuclear hormone receptor family P03372
Other
Click To Hide/Show 15 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
A-kinase anchor protein 4 (AKAP4) AKAP110 family Q5JQC9
Apoptosis-stimulating of p53 protein 2 (TP53BP2) ASPP family Q13625
Dynein light chain Tctex-type 4 (DYNLT4) Dynein light chain Tctex-type family Q5JR98
Protein phosphatase 1 regulatory subunit 15B (PPP1R15B) PPP1R15 family Q5SWA1
Ran-binding protein 9 (RANBP9) RANBP9/10 family Q96S59
Ribosomal RNA processing protein 1 homolog B (RRP1B) RRP1 family Q14684
Protein phosphatase 1 regulatory subunit 7 (PPP1R7) SDS22 family Q15435
CD2 antigen cytoplasmic tail-binding protein 2 (CD2BP2) . O95400
Neurabin-2 (PPP1R9B) . Q96SB3
Nutritionally-regulated adipose and cardiac enriched protein homolog (NRAC) . Q8N912
Protein phosphatase 1 regulatory subunit 16A (PPP1R16A) . Q96I34
Protein phosphatase 1 regulatory subunit 3B (PPP1R3B) . Q86XI6
Protein phosphatase 1 regulatory subunit 3C (PPP1R3C) . Q9UQK1
Stabilizer of axonemal microtubules 4 (SAXO4) . Q7Z5V6
Zinc finger FYVE domain-containing protein 9 (ZFYVE9) . O95405

The Drug(s) Related To This Target

Investigative
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
910-deepithio-910-didehydroacanthifolicin Small molecular drug DB02169
Calyculin A Small molecular drug DB02860
Motuporin . DB04738

References

1 Ynamide Electrophile for the Profiling of Ligandable Carboxyl Residues in Live Cells and the Development of New Covalent Inhibitors. J Med Chem. 2022 Aug 11;65(15):10408-10418. doi: 10.1021/acs.jmedchem.2c00272. Epub 2022 Jul 26.
2 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
3 Oxidant-Induced Bioconjugation for Protein Labeling in Live Cells. ACS Chem Biol. 2023 Jan 20;18(1):112-122. doi: 10.1021/acschembio.2c00740. Epub 2022 Dec 21.
4 An Azo Coupling-Based Chemoproteomic Approach to Systematically Profile the Tyrosine Reactivity in the Human Proteome. Anal Chem. 2021 Jul 27;93(29):10334-10342. doi: 10.1021/acs.analchem.1c01935. Epub 2021 Jul 12.
5 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.
6 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840
7 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
8 Discovery of a Cell-Active SuTEx Ligand of Prostaglandin Reductase 2. Chembiochem. 2021 Jun 15;22(12):2134-2139. doi: 10.1002/cbic.202000879. Epub 2021 Apr 29.
9 Global targeting of functional tyrosines using sulfur-triazole exchange chemistry. Nat Chem Biol. 2020 Feb;16(2):150-159. doi: 10.1038/s41589-019-0404-5. Epub 2019 Nov 25.
10 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.
11 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
12 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
13 SP3-Enabled Rapid and High Coverage Chemoproteomic Identification of Cell-State-Dependent Redox-Sensitive Cysteines. Mol Cell Proteomics. 2022 Apr;21(4):100218. doi: 10.1016/j.mcpro.2022.100218. Epub 2022 Feb 25.
Mass spectrometry data entry: PXD029500 , PXD031647
14 A modification-centric assessment tool for the performance of chemoproteomic probes. Nat Chem Biol. 2022 Aug;18(8):904-912. doi: 10.1038/s41589-022-01074-8. Epub 2022 Jul 21.
Mass spectrometry data entry: PXD027758 , PXD027755 , PXD027760 , PXD027762 , PXD027756 , PXD027591 , PXD007149 , PXD030064 , PXD032392 , PXD027789 , PXD027767 , PXD027764
15 Site-Specific Activity-Based Protein Profiling Using Phosphonate Handles. Mol Cell Proteomics. 2023 Jan;22(1):100455. doi: 10.1016/j.mcpro.2022.100455. Epub 2022 Nov 24.
Mass spectrometry data entry: PXD036569
16 Chemoproteomic profiling of targets of lipid-derived electrophiles by bioorthogonal aminooxy probe. Redox Biol. 2017 Aug;12:712-718. doi: 10.1016/j.redox.2017.04.001. Epub 2017 Apr 5.
17 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
18 Differently Tagged Probes for Protein Profiling of Mitochondria. Chembiochem. 2019 May 2;20(9):1155-1160. doi: 10.1002/cbic.201800735. Epub 2019 Mar 26.
19 Ligand and Target Discovery by Fragment-Based Screening in Human Cells. Cell. 2017 Jan 26;168(3):527-541.e29. doi: 10.1016/j.cell.2016.12.029. Epub 2017 Jan 19.
20 Pharmacological Targeting of Vacuolar H(+)-ATPase via Subunit V1G Combats Multidrug-Resistant Cancer. Cell Chem Biol. 2020 Nov 19;27(11):1359-1370.e8. doi: 10.1016/j.chembiol.2020.06.011. Epub 2020 Jul 9.
21 Cell-based proteome profiling of potential dasatinib targets by use of affinity-based probes. J Am Chem Soc. 2012 Feb 15;134(6):3001-14. doi: 10.1021/ja208518u. Epub 2012 Feb 1.
22 Proteome profiling reveals potential cellular targets of staurosporine using a clickable cell-permeable probe. Chem Commun (Camb). 2011 Oct 28;47(40):11306-8. doi: 10.1039/c1cc14824a. Epub 2011 Sep 16.
23 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
24 Rapid Covalent-Probe Discovery by Electrophile-Fragment Screening. J Am Chem Soc. 2019 Jun 5;141(22):8951-8968. doi: 10.1021/jacs.9b02822. Epub 2019 May 22.