Target Information
| Target General Information | Top | |||||
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| Target ID |
T89573
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| Target Name |
Staphylococcus Sortase A (Stap-coc srtA)
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| Synonyms |
Surface protein sorting A
Click to Show/Hide
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| Gene Name |
Stap-coc srtA
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| Target Type |
Preclinical target
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[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Staphylococcal/streptococcal disease [ICD-11: 1B5Y] | |||||
| Function |
Transpeptidase that anchors surface proteins to the cell wall. Recognizes and modifies its substrate by proteolytic cleavage of a C-terminal sorting signal. Following cleavage, a covalent intermediate is formed via a thioester bond between the sortase and its substrate, which is then transferred and covalently attached to the cell wall. This sortase recognizes a Leu-Pro-x-Thr-Gly (LPXTG) motif, which is cleaved by the sortase between the threonine and glycine residues. Utilizes lipid II as the peptidoglycan substrate for the sorting reaction. Responsible for the display of important virulence factors. Important for interactions with the host and host colonization during infection.
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| UniProt ID | ||||||
| EC Number |
EC 3.4.22.70
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| Sequence |
MKKWTNRLMTIAGVVLILVAAYLFAKPHIDNYLHDKDKDEKIEQYDKNVKEQASKDKKQQ
AKPQIPKDKSKVAGYIEIPDADIKEPVYPGPATPEQLNRGVSFAEENESLDDQNISIAGH TFIDRPNYQFTNLKAAKKGSMVYFKVGNETRKYKMTSIRDVKPTDVGVLDEQKGKDKQLT LITCDDYNEKTGVWEKRKIFVATEVK Click to Show/Hide
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| Drugs and Modes of Action | Top | |||||
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| Preclinical Drug(s) | [+] 1 Preclinical Drugs | + | ||||
| 1 | PMID25197057-Compound6e | Drug Info | Preclinical | Staphylococcus infection | [1] | |
| Mode of Action | [+] 1 Modes of Action | + | ||||
| Inhibitor | [+] 1 Inhibitor drugs | + | ||||
| 1 | PMID25197057-Compound6e | Drug Info | [1] | |||
| Drug Binding Sites of Target | Top | |||||
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| Ligand Name: 3-Hydroxy-6-(hydroxymethyl)-2-(thiophen-3-ylmethyl)pyran-4-one | Ligand Info | |||||
| Structure Description | Solution structure of sortase A from S. aureus in complex with 2-(aminomethyl)-3-hydroxy-4H-pyran-4-one based prodrug | PDB:6R1V | ||||
| Method | Solution NMR | Resolution | N.A. | Mutation | No | [2] |
| PDB Sequence |
MQAKPQIPKD
10 KSKVAGYIEI20 PDADIKEPVY30 PGPATPEQLN40 RGVSFAEENE50 SLDDQNISIA 60 GHTFIDRPNY70 QFTNLKAAKK80 GSMVYFKVGN90 ETRKYKMTSI100 RDVKPTDVEV 110 LDEQKGKDKQ120 LTLITCDDYN130 EKTGVWEKRK140 IFVATEVK
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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 Similarity Proteins
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There is no similarity protein (E value < 0.005) for this target
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| References | Top | |||||
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| REF 1 | Different drugs for bad bugs: antivirulence strategies in the age of antibiotic resistance. Nat Rev Drug Discov. 2017 Jul;16(7):457-471. | |||||
| REF 2 | Targeting Bacterial Sortase A with Covalent Inhibitors: 27 New Starting Points for Structure-Based Hit-to-Lead Optimization. ACS Infect Dis. 2020 Feb 14;6(2):186-194. | |||||
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