Target Information
| Target General Information | Top | |||||
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| Target ID |
T72195
(Former ID: TTDI02019)
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| Target Name |
Annexin A5 (ANXA5)
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| Synonyms |
Vascular anticoagulantalpha; Vascular anticoagulant-alpha; VACalpha; VAC-alpha; Thromboplastin inhibitor; Placental anticoagulant protein I; Placental anticoagulant protein 4; PP4; PAPI; PAP-I; Lipocortin V; Endonexin II; ENX2; Calphobindin I; CBPI; CBP-I; Annexin5; Annexin-5; Annexin V; Anchorin CII; ANX5
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| Gene Name |
ANXA5
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| Target Type |
Clinical trial target
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[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Injury [ICD-11: NA00-ND5Z] | |||||
| Function |
This protein is an anticoagulant protein that acts as an indirect inhibitor of the thromboplastin-specific complex, which is involved in the blood coagulation cascade.
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| BioChemical Class |
Annexin protein
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| UniProt ID | ||||||
| Sequence |
MAQVLRGTVTDFPGFDERADAETLRKAMKGLGTDEESILTLLTSRSNAQRQEISAAFKTL
FGRDLLDDLKSELTGKFEKLIVALMKPSRLYDAYELKHALKGAGTNEKVLTEIIASRTPE ELRAIKQVYEEEYGSSLEDDVVGDTSGYYQRMLVVLLQANRDPDAGIDEAQVEQDAQALF QAGELKWGTDEEKFITIFGTRSVSHLRKVFDKYMTISGFQIEETIDRETSGNLEQLLLAV VKSIRSIPAYLAETLYYAMKGAGTDDHTLIRVMVSRSEIDLFNIRKEFRKNFATSLYSMI KGDTSGDYKKALLLLCGEDD Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | PDB | ||||
| HIT2.0 ID | T40IPP | |||||
| Drugs and Modes of Action | Top | |||||
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| Clinical Trial Drug(s) | [+] 1 Clinical Trial Drugs | + | ||||
| 1 | Diannexin | Drug Info | Phase 2 | Myocardial reperfusion injury | [2] | |
| Mode of Action | [+] 1 Modes of Action | + | ||||
| Modulator | [+] 1 Modulator drugs | + | ||||
| 1 | Diannexin | Drug Info | [1] | |||
| Cell-based Target Expression Variations | Top | |||||
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| Cell-based Target Expression Variations | ||||||
| Drug Binding Sites of Target | Top | |||||
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| Ligand Name: K201 free base | Ligand Info | |||||
| Structure Description | CRYSTAL STRUCTURE OF RECOMBINANT HUMAN PLACENTAL ANNEXIN V COMPLEXED WITH K-201 AS A CALCIUM CHANNEL ACTIVITY INHIBITOR | PDB:1HAK | ||||
| Method | X-ray diffraction | Resolution | 3.00 Å | Mutation | No | [3] |
| PDB Sequence |
QVLRGTVTDF
12 PGFDERADAE22 TLRKAMKGLG32 TDEESILTLL42 TSRSNAQRQE52 ISAAFKTLFG 62 RDLLDDLKSE72 LTGKFEKLIV82 ALMKPSRLYD92 AYELKHALKG102 AGTNEKVLTE 112 IIASRTPEEL122 RAIKQVYEEE132 YGSSLEDDVV142 GDTSGYYQRM152 LVVLLQANRD 162 PDAGIDEAQV172 EQDAQALFQA182 GELKWGTDEE192 KFITIFGTRS202 VSHLRKVFDK 212 YMTISGFQIE222 ETIDRETSGN232 LEQLLLAVVK242 SIRSIPAYLA252 ETLYYAMKGA 262 GTDDHTLIRV272 MVSRSEIDLF282 NIRKEFRKNF292 ATSLYSMIKG302 DTSGDYKKAL 312 LLLCGEDD
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| Click to View More Binding Site Information of This Target with Different Ligands | ||||||
| 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 Tissue Distribution
of target is determined from a proteomics study that quantified more than 12,000 genes across 32 normal human tissues. Tissue Specificity (TS) score was used to define the enrichment of target across tissues.
The distribution of targets among different tissues or organs need to be taken into consideration when assessing the target druggability, as it is generally accepted that the wider the target distribution, the greater the concern over potential adverse effects
(Nat Rev Drug Discov, 20: 64-81, 2021).
Human Similarity Proteins
Human Tissue Distribution
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There is no similarity protein (E value < 0.005) for this target
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Note:
If a protein has TS (tissue specficity) scores at least in one tissue >= 2.5, this protein is called tissue-enriched (including tissue-enriched-but-not-specific and tissue-specific). In the plots, the vertical lines are at thresholds 2.5 and 4.
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| Target Regulators | Top | |||||
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| Target-interacting Proteins | ||||||
| Target Affiliated Biological Pathways | Top | |||||
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| WikiPathways | [+] 2 WikiPathways | + | ||||
| 1 | Prostaglandin Synthesis and Regulation | |||||
| 2 | Apoptosis-related network due to altered Notch3 in ovarian cancer | |||||
| References | Top | |||||
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| REF 1 | Expression and purification of recombinant human annexin V in Escherichia coli. Prep Biochem Biotechnol. 2000 Nov;30(4):305-12. | |||||
| REF 2 | ClinicalTrials.gov (NCT00615966) Phase 2 Study of the Safety of Diannexin in Kidney Transplant Recipients. U.S. National Institutes of Health. | |||||
| REF 3 | Crystal structure of annexin V with its ligand K-201 as a calcium channel activity inhibitor. J Mol Biol. 1997 Nov 21;274(1):16-20. | |||||
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