Target Information
| Target General Information | Top | |||||
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| Target ID |
T05806
(Former ID: TTDR00853)
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| Target Name |
Valacyclovir hydrolase (BPHL)
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| Synonyms |
VACVase; MCNAA; DJ40E16.6.1; Breast epithelial mucin-associated antigen; Bph-rp; Biphenyl hydrolase-like protein (Serine hydrolase) (Breast epithelial mucin-associated antigen, MCNAA, Bph-rp), variant 1; Biphenyl hydrolase-like protein; BPHL
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| Gene Name |
BPHL
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| Target Type |
Literature-reported target
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[1] | ||||
| Function |
Serine hydrolase that catalyzes the hydrolytic activation of amino acid ester prodrugs of nucleoside analogs such as valacyclovir and valganciclovir. Activates valacyclovir to acyclovir. May play a role in detoxification processes. It is a specific alpha-amino acid ester hydrolase that prefers small, hydrophobic, and aromatic side chains and does not have a stringent requirement for the leaving group other than preferring aprimary alcohol.
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| BioChemical Class |
Carboxylic ester hydrolase
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| UniProt ID | ||||||
| EC Number |
EC 3.1.-.-
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| Sequence |
MVAVLGGRGVLRLRLLLSALKPGIHVPRAGPAAAFGTSVTSAKVAVNGVQLHYQQTGEGD
HAVLLLPGMLGSGETDFGPQLKNLNKKLFTVVAWDPRGYGHSRPPDRDFPADFFERDAKD AVDLMKALKFKKVSLLGWSDGGITALIAAAKYPSYIHKMVIWGANAYVTDEDSMIYEGIR DVSKWSERTRKPLEALYGYDYFARTCEKWVDGIRQFKHLPDGNICRHLLPRVQCPALIVH GEKDPLVPRFHADFIHKHVKGSRLHLMPEGKHNLHLRFADEFNKLAEDFLQ Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | PDB | ||||
| 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: L-tyrosinamide | Ligand Info | |||||
| Structure Description | Crystal structure of valacyclovir hydrolase complexed with a product analogue | PDB:2OCI | ||||
| Method | X-ray diffraction | Resolution | 1.90 Å | Mutation | No | [2] |
| PDB Sequence |
SVTSAKVAVN
30 GVQLHYQQTG40 EGDHAVLLLP50 GMLGSGETDF60 GPQLKNLNKK70 LFTVVAWDPR 80 GYGHSRPPDR90 DFPADFFERD100 AKDAVDLMKA110 LKFKKVSLLG120 WSDGGITALI 130 AAAKYPSYIH140 KMVIWGANAY150 VTDEDSMIYE160 GIRDVSKWSE170 RTRKPLEALY 180 GYDYFARTCE190 KWVDGIRQFK200 HLPDGNICRH210 LLPRVQCPAL220 IVHGEKDPLV 230 PRFHADFIHK240 HVKGSRLHLM250 PEGKHNLHLR260 FADEFNKLAE270 DFLQ |
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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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| Protein Name | Pfam ID | Percentage of Identity (%) | E value |
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| Epoxide hydrolase 3 (EPHX3) | 29.565 (34/115) | 8.99E-06 |
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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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| References | Top | |||||
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| REF 1 | The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. | |||||
| REF 2 | Molecular basis of prodrug activation by human valacyclovirase, an alpha-amino acid ester hydrolase. J Biol Chem. 2008 Apr 4;283(14):9318-27. | |||||
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