Target Information
| Target General Information | Top | |||||
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| Target ID |
T20534
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| Target Name |
Pseudomonas Transcriptional activator protein LasR (Pseudo LasR)
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| Gene Name |
Pseudo LasR
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| Target Type |
Preclinical target
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[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Glanders [ICD-11: 1B92] | |||||
| Function |
Transcriptional activator of elastase structural gene (LasB). Binds to the PAI autoinducer.
Click to Show/Hide
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| UniProt ID | ||||||
| Sequence |
MALVDGFLELERSSGKLEWSAILQKMASDLGFSKILFGLLPKDSQDYENAFIVGNYPAAW
REHYDRAGYARVDPTVSHCTQSVLPIFWEPSIYQTRKQHEFFEEASAAGLVYGLTMPLHG ARGELGALSLSVEAENRAEANRFMESVLPTLWMLKDYALQSGAGLAFEHPVSKPVVLTSR EKEVLQWCAIGKTSWEISVICNCSEANVNFHMGNIRRKFGVTSRRVAAIMAVNLGLITL Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | PDB | ||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Preclinical Drug(s) | [+] 2 Preclinical Drugs | + | ||||
| 1 | 3-Oxo-C12-(2-amino-cyclohexanone) | Drug Info | Preclinical | Pseudomonas infection | [1] | |
| 2 | C30 | Drug Info | Preclinical | Pseudomonas infection | [1] | |
| Mode of Action | [+] 2 Modes of Action | + | ||||
| Agonist | [+] 1 Agonist drugs | + | ||||
| 1 | 3-Oxo-C12-(2-amino-cyclohexanone) | Drug Info | [1] | |||
| Inhibitor | [+] 1 Inhibitor drugs | + | ||||
| 1 | C30 | Drug Info | [1] | |||
| Drug Binding Sites of Target | Top | |||||
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| Ligand Name: PAI-1 | Ligand Info | |||||
| Structure Description | LasR-OC12 HSL complex | PDB:3IX3 | ||||
| Method | X-ray diffraction | Resolution | 1.40 Å | Mutation | No | [2] |
| PDB Sequence |
FLELERSSGK
16 LEWSAILQKM26 ASDLGFSKIL36 FGLLPKDSQD46 YENAFIVGNY56 PAAWREHYDR 66 AGYARVDPTV76 SHCTQSVLPI86 FWEPSIYQTR96 KQHEFFEEAS106 AAGLVYGLTM 116 PLHGARGELG126 ALSLSVEAEN136 RAEANRFMES146 VLPTLWMLKD156 YALQSGAGLA 166 FEH
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LEU36
3.828
GLY38
3.960
LEU39
4.141
LEU40
4.083
TYR47
4.026
ALA50
3.689
ILE52
3.951
TYR56
2.733
TRP60
3.045
ARG61
3.897
TYR64
3.413
ALA70
4.771
ASP73
2.793
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| Click to View More Binding Site Information of This Target and Ligand Pair | ||||||
| Ligand Name: 4-(3-bromophenoxy)-N-[(3S)-2-oxothiolan-3-yl]butanamide | Ligand Info | |||||
| Structure Description | LasR LBD:mBTL complex | PDB:6MWL | ||||
| Method | X-ray diffraction | Resolution | 1.50 Å | Mutation | No | [3] |
| PDB Sequence |
GFLELERSSG
9 KLEWSAILQK19 MASDLGFSKI29 LFGLLPKDSQ39 DYENAFIVGN49 YPAAWREHYD 59 RAGYARVDPT69 VSHCTQSVLP79 IFWEPSIYQT89 RKQHEFFEEA99 SAAGLVYGLT 109 MPLHGARGEL119 GALSLSVEAE129 NRAEANRFME139 SVLPTLWMLK149 DYALQSGAGL 159 AF
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LEU30
4.608
GLY32
3.709
LEU33
3.702
LEU34
3.965
TYR41
4.021
ALA44
4.075
ILE46
3.962
TYR50
2.708
TRP54
2.973
TYR58
3.881
ASP67
2.924
THR69
3.210
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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 | LasR-OC12 HSL complex | |||||
| REF 3 | An Autoinducer Analogue Reveals an Alternative Mode of Ligand Binding for the LasR Quorum-Sensing Receptor. ACS Chem Biol. 2019 Mar 15;14(3):378-389. | |||||
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