Details of the Target

General Information of Target

Target ID LDTP12871
Target Name Gamma-secretase subunit PEN-2 (PSENEN)
Gene Name PSENEN
Gene ID 55851
Synonyms
PEN2; Gamma-secretase subunit PEN-2; Presenilin enhancer protein 2
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MGVQAGLFGMLGFLGVALGGSPALRWYRTSCHLTKAVPGNPLGYLSFLAKDAQGLALIHA
RWDAHRRLQSCSWEDEPELTAAYGALCAHETAWGSFIHTPGPELQRALATLQSQWEACRA
LEESPAGARKKRAAGQSGVPGGGHQREKRGWTMPGTLWCGVGDSAGNSSELGVFQGPDLC
CREHDRCPQNISPLQYNYGIRNYRFHTISHCDCDTRFQQCLQNQHDSISDIVGVAFFNVL
EIPCFVLEEQEACVAWYWWGGCRMYGTVPLARLQPRTFYNASWSSRATSPTPSSRSPAPP
KPRQKQHLRKGPPHQKGSKRPSKANTTALQDPMVSPRLDVAPTGLQGPQGGLKPQGARWV
CRSFRRHLDQCEHQIGPREIEFQLLNSAQEPLFHCNCTRRLARFLRLHSPPEVTNMLWEL
LGTTCFKLAPPLDCVEGKNCSRDPRAIRVSARHLRRLQQRRHQLQDKGTDERQPWPSEPL
RGPMSFYNQCLQLTQAARRPDRQQKSWSQ
Target Bioclass
Other
Family
PEN-2 family
Subcellular location
Endoplasmic reticulum membrane
Function
Essential subunit of the gamma-secretase complex, an endoprotease complex that catalyzes the intramembrane cleavage of integral membrane proteins such as Notch receptors and APP (amyloid-beta precursor protein). The gamma-secretase complex plays a role in Notch and Wnt signaling cascades and regulation of downstream processes via its role in processing key regulatory proteins, and by regulating cytosolic CTNNB1 levels (Probable). PSENEN modulates both endoproteolysis of presenilin and gamma-secretase activity.
Uniprot ID
Q9NZ42
Ensemble ID
ENST00000222266.2
HGNC ID
HGNC:30100
ChEMBL ID
CHEMBL2374

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 3 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
STPyne
 Probe Info  		K11(10.00)  LDD0277  [1]
IA-alkyne
 Probe Info  		C15(2.14)  LDD2182  [2]
IPM
 Probe Info  		N.A.  LDD2156  [3]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0625  F8 Ramos C15(0.79)  LDD2187  [2]
 LDCM0572  Fragment10 Ramos C15(2.96)  LDD2189  [2]
 LDCM0573  Fragment11 Ramos C15(7.22)  LDD2190  [2]
 LDCM0574  Fragment12 Ramos C15(6.53)  LDD2191  [2]
 LDCM0575  Fragment13 Ramos C15(1.13)  LDD2192  [2]
 LDCM0579  Fragment20 Ramos C15(8.72)  LDD2194  [2]
 LDCM0580  Fragment21 Ramos C15(1.00)  LDD2195  [2]
 LDCM0582  Fragment23 Ramos C15(1.07)  LDD2196  [2]
 LDCM0578  Fragment27 Ramos C15(0.77)  LDD2197  [2]
 LDCM0586  Fragment28 Ramos C15(0.74)  LDD2198  [2]
 LDCM0588  Fragment30 Ramos C15(1.92)  LDD2199  [2]
 LDCM0589  Fragment31 Ramos C15(1.52)  LDD2200  [2]
 LDCM0590  Fragment32 Ramos C15(3.41)  LDD2201  [2]
 LDCM0468  Fragment33 Ramos C15(1.10)  LDD2202  [2]
 LDCM0596  Fragment38 Ramos C15(10.42)  LDD2203  [2]
 LDCM0566  Fragment4 Ramos C15(3.38)  LDD2184  [2]
 LDCM0610  Fragment52 Ramos C15(1.29)  LDD2204  [2]
 LDCM0614  Fragment56 Ramos C15(1.01)  LDD2205  [2]
 LDCM0569  Fragment7 Ramos C15(2.71)  LDD2186  [2]
 LDCM0022  KB02 Ramos C15(2.14)  LDD2182  [2]
 LDCM0627  NUDT7-COV-1 HEK-293T C15(1.94); C15(1.61)  LDD2206  [4]
 LDCM0628  OTUB2-COV-1 HEK-293T C15(0.63)  LDD2207  [4]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Presenilin-1 (PSEN1) Peptidase A22A family P49768
Tyrosine-protein kinase Fyn (FYN) Tyr protein kinase family P06241
Transporter and channel
Click To Hide/Show 4 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Amyloid-beta precursor protein (APP) APP family P05067
Ileal sodium/bile acid cotransporter (SLC10A2) Bile acid:sodium symporter (BASS) family Q12908
Sodium-dependent organic anion transporter (SLC10A6) Bile acid:sodium symporter (BASS) family Q3KNW5
Transmembrane emp24 domain-containing protein 10 (TMED10) EMP24/GP25L family P49755
Other
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Ferritin light chain (FTL) Ferritin family P02792
Nicastrin (NCSTN) Nicastrin family Q92542
Cytohesin-1 (CYTH1) . Q15438

The Drug(s) Related To This Target

Investigative
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
E-2012 Small molecular drug DB05171

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 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
3 Benchmarking Cleavable Biotin Tags for Peptide-Centric Chemoproteomics. J Proteome Res. 2022 May 6;21(5):1349-1358. doi: 10.1021/acs.jproteome.2c00174. Epub 2022 Apr 25.
Mass spectrometry data entry: PXD031019
4 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.