General Information of Target

Target ID LDTP00818
Target Name Hypocretin neuropeptide precursor (HCRT)
Gene Name HCRT
Gene ID 3060
Synonyms
OX; PPORX; PPOX; Hypocretin neuropeptide precursor; Hypocretin; Hcrt; Orexin precursor; Prepro-orexin; Preprohypocretin) [Cleaved into: Orexin-A; Hypocretin-1; Hcrt1; Orexin-B; Hypocretin-2; Hcrt2)]
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MNLPSTKVSWAAVTLLLLLLLLPPALLSSGAAAQPLPDCCRQKTCSCRLYELLHGAGNHA
AGILTLGKRRSGPPGLQGRLQRLLQASGNHAAGILTMGRRAGAEPAPRPCLGRRCSAPAA
ASVAPGGQSGI
Target Type
Literature-reported
Target Bioclass
Other
Family
Orexin family
Subcellular location
Rough endoplasmic reticulum
Function
Neuropeptides that play a significant role in the regulation of food intake and sleep-wakefulness, possibly by coordinating the complex behavioral and physiologic responses of these complementary homeostatic functions. A broader role in the homeostatic regulation of energy metabolism, autonomic function, hormonal balance and the regulation of body fluids, is also suggested.; [Orexin-A]: Binds to orexin receptors HCRTR1/OX1R and HCRTR2/OX2R with a high affinity. Stimulates food intake. Modulates pituitary luteinizing hormone secretion in an ovarian steroid-dependent manner.; [Orexin-B]: Binds to orexin receptor HCRTR2/OX2R only. Stimulates food intake. Modulates pituitary luteinizing hormone secretion in an ovarian steroid-dependent manner.
TTD ID
T60744
Uniprot ID
O43612
DrugMap ID
TTU5HJP
Ensemble ID
ENST00000293330.1
HGNC ID
HGNC:4847

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info 
C410(1.62); C183(2.80)  LDD3312  [1]
PAL-AfBPP Probe
Click To Hide/Show 2 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
STS-1
 Probe Info 
N.A.  LDD0137  [2]
STS-2
 Probe Info 
N.A.  LDD0139  [2]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 22RV1 C26(1.45); C258(1.55)  LDD2243  [1]
 LDCM0023  KB03 22RV1 C26(1.17); C258(1.69)  LDD2660  [1]
 LDCM0024  KB05 HMCB C410(1.62); C183(2.80)  LDD3312  [1]

The Interaction Atlas With This Target

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
Pidolic Acid Small molecular drug DB03088
Investigative
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Pyroglutamic Acid Small molecular drug D0U7QA

References

1 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
2 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.