Details of the Target

General Information of Target

Target ID LDTP02834
Target Name Cyclic AMP-responsive element-binding protein 1 (CREB1)
Gene Name CREB1
Gene ID 1385
Synonyms
Cyclic AMP-responsive element-binding protein 1; CREB-1; cAMP-responsive element-binding protein 1
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MTMESGAENQQSGDAAVTEAENQQMTVQAQPQIATLAQVSMPAAHATSSAPTVTLVQLPN
GQTVQVHGVIQAAQPSVIQSPQVQTVQISTIAESEDSQESVDSVTDSQKRREILSRRPSY
RKILNDLSSDAPGVPRIEEEKSEEETSAPAITTVTVPTPIYQTSSGQYIAITQGGAIQLA
NNGTDGVQGLQTLTMTNAAATQPGTTILQYAQTTDGQQILVPSNQVVVQAASGDVQTYQI
RTAPTSTIAPGVVMASSPALPTQPAEEAARKREVRLMKNREAARECRRKKKEYVKCLENR
VAVLENQNKTLIEELKALKDLYCHKSD
Target Type
Literature-reported
Target Bioclass
Transcription factor
Family
BZIP family
Subcellular location
Nucleus
Function
Phosphorylation-dependent transcription factor that stimulates transcription upon binding to the DNA cAMP response element (CRE), a sequence present in many viral and cellular promoters. Transcription activation is enhanced by the TORC coactivators which act independently of Ser-119 phosphorylation. Involved in different cellular processes including the synchronization of circadian rhythmicity and the differentiation of adipose cells. Regulates the expression of apoptotic and inflammatory response factors in cardiomyocytes in response to ERFE-mediated activation of AKT signaling.
TTD ID
T92098
Uniprot ID
P16220
DrugMap ID
TTH4AN3
Ensemble ID
ENST00000353267.8
HGNC ID
HGNC:2345
ChEMBL ID
CHEMBL5587

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 15 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
m-APA
 Probe Info  		15.00  LDD0402  [1]
STPyne
 Probe Info  		K122(10.00); K319(3.19)  LDD0277  [2]
ONAyne
 Probe Info  		K319(10.00)  LDD0275  [2]
BTD
 Probe Info  		C300(0.60); C337(0.55)  LDD2091  [3]
AHL-Pu-1
 Probe Info  		C337(2.45)  LDD0169  [4]
IA-alkyne
 Probe Info  		C337(5.04)  LDD0372  [4]
DBIA
 Probe Info  		C337(5.18)  LDD0209  [5]
Acrolein
 Probe Info  		K333(0.00); H338(0.00)  LDD0226  [6]
IPM
 Probe Info  		N.A.  LDD0025  [7]
JW-RF-010
 Probe Info  		N.A.  LDD0026  [7]
NAIA_5
 Probe Info  		N.A.  LDD2224  [8]
TFBX
 Probe Info  		N.A.  LDD0148  [7]
Phosphinate-6
 Probe Info  		C296(0.00); C323(0.00)  LDD0018  [9]
1c-yne
 Probe Info  		N.A.  LDD0228  [10]
AOyne
 Probe Info  		15.00  LDD0443  [11]

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 C337(0.88)  LDD2117  [3]
 LDCM0026  4SU-RNA+native RNA HEK-293T C337(2.45)  LDD0169  [4]
 LDCM0156  Aniline NCI-H1299 11.68  LDD0403  [1]
 LDCM0498  BS-3668 MDA-MB-231 C300(0.60); C337(0.55)  LDD2091  [3]
 LDCM0632  CL-Sc Hep-G2 C323(0.66); C323(0.58)  LDD2227  [8]
 LDCM0023  KB03 Jurkat C337(5.18)  LDD0209  [5]
 LDCM0509  N-(4-bromo-3,5-dimethylphenyl)-2-nitroacetamide MDA-MB-231 C300(0.96)  LDD2102  [3]
 LDCM0109  NEM HeLa K333(0.00); H338(0.00)  LDD0226  [6]
 LDCM0506  Nucleophilic fragment 16a MDA-MB-231 C300(0.71)  LDD2099  [3]
 LDCM0507  Nucleophilic fragment 16b MDA-MB-231 C337(0.56)  LDD2100  [3]
 LDCM0511  Nucleophilic fragment 18b MDA-MB-231 C337(0.54)  LDD2104  [3]
 LDCM0514  Nucleophilic fragment 20a MDA-MB-231 C300(0.79); C337(0.97); C310(0.83)  LDD2107  [3]
 LDCM0526  Nucleophilic fragment 26a MDA-MB-231 C300(2.43); C337(1.05)  LDD2119  [3]
 LDCM0532  Nucleophilic fragment 29a MDA-MB-231 C300(0.62); C337(0.88)  LDD2125  [3]
 LDCM0534  Nucleophilic fragment 30a MDA-MB-231 C300(1.04); C337(0.91); C310(0.88)  LDD2127  [3]
 LDCM0543  Nucleophilic fragment 38 MDA-MB-231 C300(0.96); C337(1.46)  LDD2136  [3]
 LDCM0544  Nucleophilic fragment 39 MDA-MB-231 C300(0.83); C337(0.90); C310(0.59)  LDD2137  [3]
 LDCM0547  Nucleophilic fragment 41 MDA-MB-231 C337(0.58); C310(0.39)  LDD2141  [3]
 LDCM0554  Nucleophilic fragment 7a MDA-MB-231 C337(0.65)  LDD2148  [3]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 6 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Anterior gradient protein 2 homolog (AGR2) AGR family O95994
PAS domain-containing serine/threonine-protein kinase (PASK) CAMK Ser/Thr protein kinase family Q96RG2
Testis-specific serine/threonine-protein kinase 4 (TSSK4) CAMK Ser/Thr protein kinase family Q6SA08
CREB-binding protein (CREBBP) . Q92793
E3 ubiquitin-protein ligase RNF4 (RNF4) . P78317
Histone acetyltransferase p300 (EP300) . Q09472
Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Huntingtin (HTT) Huntingtin family P42858
Transcription factor
Click To Hide/Show 6 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Cyclic AMP-responsive element-binding protein 1 (CREB1) BZIP family P16220
Cyclic AMP-dependent transcription factor ATF-1 (ATF1) BZIP family P18846
Nuclear factor interleukin-3-regulated protein (NFIL3) BZIP family Q16649
Homeobox protein Meis1 (MEIS1) TALE/MEIS homeobox family O00470
Nuclear factor of activated T-cells, cytoplasmic 1 (NFATC1) . O95644
Nuclear factor of activated T-cells, cytoplasmic 2 (NFATC2) . Q13469
Other
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
CREB-regulated transcription coactivator 1 (CRTC1) TORC family Q6UUV9
CREB-regulated transcription coactivator 2 (CRTC2) TORC family Q53ET0

The Drug(s) Related To This Target

Approved
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Adenosine Phosphate Small molecular drug DB00131
Naloxone Small molecular drug DB01183

References

1 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.
2 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
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 Covalent Inhibition by a Natural Product-Inspired Latent Electrophile. J Am Chem Soc. 2023 May 24;145(20):11097-11109. doi: 10.1021/jacs.3c00598. Epub 2023 May 15.
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 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
8 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
9 DFT-Guided Discovery of Ethynyl-Triazolyl-Phosphinates as Modular Electrophiles for Chemoselective Cysteine Bioconjugation and Profiling. Angew Chem Int Ed Engl. 2022 Oct 10;61(41):e202205348. doi: 10.1002/anie.202205348. Epub 2022 Aug 22.
Mass spectrometry data entry: PXD033004
10 Tunable Amine-Reactive Electrophiles for Selective Profiling of Lysine. Angew Chem Int Ed Engl. 2022 Jan 26;61(5):e202112107. doi: 10.1002/anie.202112107. Epub 2021 Dec 16.
11 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.