Target Information
| Target General Information | Top | |||||
|---|---|---|---|---|---|---|
| Target ID |
T65429
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| Target Name |
G-protein coupled receptor 20 (GPR20)
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| Gene Name |
GPR20
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| Target Type |
Clinical trial target
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[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Gastrointestinal stromal tumour [ICD-11: 2B5B] | |||||
| Function |
Orphan receptor with constitutive G(i) signaling activity that activate cyclic AMP.
Click to Show/Hide
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| BioChemical Class |
G-protein coupled receptor 1 family
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| UniProt ID | ||||||
| Sequence |
MPSVSPAGPSAGAVPNATAVTTVRTNASGLEVPLFHLFARLDEELHGTFPGLWLALMAVH
GAIFLAGLVLNGLALYVFCCRTRAKTPSVIYTINLVVTDLLVGLSLPTRFAVYYGARGCL RCAFPHVLGYFLNMHCSILFLTCICVDRYLAIVRPEGSRRCRQPACARAVCAFVWLAAGA VTLSVLGVTGSRPCCRVFALTVLEFLLPLLVISVFTGRIMCALSRPGLLHQGRQRRVRAM QLLLTVLIIFLVCFTPFHARQVAVALWPDMPHHTSLVVYHVAVTLSSLNSCMDPIVYCFV TSGFQATVRGLFGQHGEREPSSGDVVSMHRSSKGSGRHHILSAGPHALTQALANGPEA Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Clinical Trial Drug(s) | [+] 1 Clinical Trial Drugs | + | ||||
| 1 | DS-6157 | Drug Info | Phase 1 | Gastrointestinal stromal tumour | [2] | |
| Mode of Action | [+] 1 Modes of Action | + | ||||
| Inhibitor | [+] 1 Inhibitor drugs | + | ||||
| 1 | DS-6157 | Drug Info | [1] | |||
| Cell-based Target Expression Variations | Top | |||||
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| Cell-based Target Expression Variations | ||||||
| Different Human System Profiles of Target | Top |
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Human Similarity Proteins
of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.
A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs
(Brief Bioinform, 21: 649-662, 2020).
Human Similarity Proteins
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| Protein Name | Pfam ID | Percentage of Identity (%) | E value |
|---|---|---|---|
| Mas-related G-protein coupled receptor member G (MRGPRG) | 26.316 (75/285) | 2.41E-04 | |
| References | Top | |||||
|---|---|---|---|---|---|---|
| REF 1 | Identification and Therapeutic Targeting of GPR20, Selectively Expressed in Gastrointestinal Stromal Tumors, with DS-6157a, a First-in-Class Antibody-Drug Conjugate. Cancer Discov. 2021 Jun;11(6):1508-1523. | |||||
| REF 2 | ClinicalTrials.gov (NCT04276415) DS-6157a in Participants With Advanced Gastrointestinal Stromal Tumor (GIST). U.S. National Institutes of Health. | |||||
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