Target Information
| Target General Information | Top | |||||
|---|---|---|---|---|---|---|
| Target ID |
T81569
|
|||||
| Target Name |
Zinc finger protein Helios (IKZF2)
|
|||||
| Synonyms |
Ikaros family zinc finger protein 2
Click to Show/Hide
|
|||||
| Gene Name |
IKZF2
|
|||||
| Target Type |
Clinical trial target
|
[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Solid tumour/cancer [ICD-11: 2A00-2F9Z] | |||||
| Function |
Associates with Ikaros at centromeric heterochromatin.
Click to Show/Hide
|
|||||
| UniProt ID | ||||||
| Sequence |
METEAIDGYITCDNELSPEREHSNMAIDLTSSTPNGQHASPSHMTSTNSVKLEMQSDEEC
DRKPLSREDEIRGHDEGSSLEEPLIESSEVADNRKVQELQGEGGIRLPNGKLKCDVCGMV CIGPNVLMVHKRSHTGERPFHCNQCGASFTQKGNLLRHIKLHSGEKPFKCPFCSYACRRR DALTGHLRTHSVGKPHKCNYCGRSYKQRSSLEEHKERCHNYLQNVSMEAAGQVMSHHVPP MEDCKEQEPIMDNNISLVPFERPAVIEKLTGNMGKRKSSTPQKFVGEKLMRFSYPDIHFD MNLTYEKEAELMQSHMMDQAINNAITYLGAEALHPLMQHPPSTIAEVAPVISSAYSQVYH PNRIERPISRETADSHENNMDGPISLIRPKSRPQEREASPSNSCLDSTDSESSHDDHQSY QGHPALNPKRKQSPAYMKEDVKALDTTKAPKGSLKDIYKVFNGEGEQIRAFKCEHCRVLF LDHVMYTIHMGCHGYRDPLECNICGYRSQDRYEFSSHIVRGEHTFH Click to Show/Hide
|
|||||
| 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 | DKY709 | Drug Info | Phase 1 | Solid tumour/cancer | [2] | |
| Mode of Action | [+] 1 Modes of Action | + | ||||
| Degrader | [+] 1 Degrader drugs | + | ||||
| 1 | DKY709 | Drug Info | [1] | |||
| Cell-based Target Expression Variations | Top | |||||
|---|---|---|---|---|---|---|
| Cell-based Target Expression Variations | ||||||
| Drug Binding Sites of Target | Top | |||||
|---|---|---|---|---|---|---|
| Ligand Name: 3-[3-[[1-[(3~{S})-2,6-bis(oxidanylidene)piperidin-3-yl]-2,5-bis(oxidanylidene)pyrrol-3-yl]amino]phenyl]-~{N}-(3-chloranyl-4-methyl-phenyl)propanamide | Ligand Info | |||||
| Structure Description | Crystal structure of DDB1-CRBN-ALV1 complex bound to Helios (IKZF2 ZF2) | PDB:7LPS | ||||
| Method | X-ray diffraction | Resolution | 3.78 Å | Mutation | No | [3] |
| PDB Sequence |
GERPFHCNQC
145 GASFTQKGNL155 LRHIKLHSG
|
|||||
|
|
||||||
| Click to View More Binding Site Information of This Target with Different Ligands | ||||||
| Different Human System Profiles of Target | Top |
|---|---|
|
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
|
|
| Protein Name | Pfam ID | Percentage of Identity (%) | E value |
|---|---|---|---|
| Zinc finger protein Pegasus (IKZF5) | 25.855 (121/468) | 5.24E-33 | |
| RE1-silencing transcription factor (REST) | 39.640 (44/111) | 4.93E-17 | |
| References | Top | |||||
|---|---|---|---|---|---|---|
| REF 1 | Targeted protein degraders crowd into the clinic. Nat Rev Drug Discov. 2021 Apr;20(4):247-250. | |||||
| REF 2 | ClinicalTrials.gov (NCT03891953) Study of Safety and Efficacy of DKY709 Alone or in Combination With PDR001 in Patients With Advanced Solid Tumors.. U.S. National Institutes of Health. | |||||
| REF 3 | Acute pharmacological degradation of Helios destabilizes regulatory T cells. Nat Chem Biol. 2021 Jun;17(6):711-717. | |||||
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.