Target Information
| Target General Information | Top | |||||
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| Target ID |
T58361
(Former ID: TTDR00964)
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| Target Name |
Transforming protein RhoB (RHOB)
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| Synonyms |
RhoB
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| Gene Name |
RHOB
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| Target Type |
Literature-reported target
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[1] | ||||
| Function |
Regulates a signal transduction pathway linking plasma membrane receptors to the assembly of focal adhesions and actin stress fibers.
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| UniProt ID | ||||||
| Sequence |
MAAIRKKLVVVGDGACGKTCLLIVFSKDEFPEVYVPTVFENYVADIEVDGKQVELALWDT
AGQEDYDRLRPLSYPDTDVILMCFSVDSPDSLENIPEKWVPEVKHFCPNVPIILVANKKD LRSDEHVRTELARMKQEPVRTDDGRAMAVRIQAYDYLECSAKTKEGVREVFETATRAALQ KRYGSQNGCINCCKVL Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | PDB | ||||
| HIT2.0 ID | T22N8Q | |||||
| 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: Guanosine-5'-Diphosphate | Ligand Info | |||||
| Structure Description | The crystal structure of RhoB in the GDP-bound state | PDB:2FV8 | ||||
| Method | X-ray diffraction | Resolution | 1.90 Å | Mutation | No | [2] |
| PDB Sequence |
YFQSMIRKKL
8 VVVGDGACGK18 TCLLIVFSKD28 EFPFENYVAD45 IEVDGKQVEL55 ALWDTAGQED 65 YDRLRPLSYP75 DTDVILMCFS85 VDSPDSLENI95 PEKWVPEVKH105 FCPNVPIILV 115 ANKKDLRSDE125 HVRTELARMK135 QEPVRTDDGR145 AMAVRIQAYD155 YLECSAKTKE 165 GVREVFETAT175 RAALQKRYGS185
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| Ligand Name: Guanosine-5'-Triphosphate | Ligand Info | |||||
| Structure Description | Crystal structure of Human RHOB Q63L in complex with GTP | PDB:6HXU | ||||
| Method | X-ray diffraction | Resolution | 1.19 Å | Mutation | Yes | [3] |
| PDB Sequence |
AAIRKKLVVV
11 GDGACGKTCL21 LIVFSKDEFP31 EVYVPTVFEN41 YVADIEVDGK51 QVELALWDTA 61 GLEDYDRLRP71 LSYPDTDVIL81 MCFSVDSPDS91 LENIPEKWVP101 EVKHFCPNVP 111 IILVANKKDL121 RSDEHVRTEL131 ARMKQEPVRT141 DDGRAMAVRI151 QAYDYLECSA 161 KTKEGVREVF171 ETATRAALQK181 RY
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GLY12
4.690
ASP13
3.816
GLY14
2.561
ALA15
2.210
CYS16
2.865
GLY17
2.334
LYS18
1.817
THR19
2.122
CYS20
1.989
LEU21
4.228
PHE30
2.363
PRO31
3.828
GLU32
4.905
TYR34
1.877
VAL35
4.402
PRO36
2.716
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| Click to View More Binding Site Information of This Target and Ligand Pair | ||||||
| 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).
Biological Network Descriptors
of target is determined based on a human protein-protein interactions (PPI) network consisting of 9,309 proteins and 52,713 PPIs, which were with a high confidence score of ≥ 0.95 collected from STRING database.
The network properties of targets based on protein-protein interactions (PPIs) have been widely adopted for the assessment of target’s druggability. Proteins with high node degree tend to have a high impact on network function through multiple interactions, while proteins with high betweenness centrality are regarded to be central for communication in interaction networks and regulate the flow of signaling information
(Front Pharmacol, 9, 1245, 2018;
Curr Opin Struct Biol. 44:134-142, 2017).
Human Similarity Proteins
Human Tissue Distribution
Biological Network Descriptors
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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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| Degree | 9 | Degree centrality | 9.67E-04 | Betweenness centrality | 7.49E-06 |
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| Closeness centrality | 1.99E-01 | Radiality | 1.34E+01 | Clustering coefficient | 2.78E-02 |
| Neighborhood connectivity | 1.08E+01 | Topological coefficient | 1.79E-01 | Eccentricity | 13 |
| Download | Click to Download the Full PPI Network of This Target | ||||
| References | Top | |||||
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| REF 1 | RhoB controls Akt trafficking and stage-specific survival of endothelial cells during vascular development. Genes Dev. 2003 Nov 1;17(21):2721-32. | |||||
| REF 2 | The crystal structure of RhoB in the GDP-bound state | |||||
| REF 3 | A Targeted Protein Degradation Cell-Based Screening for Nanobodies Selective toward the Cellular RHOB GTP-Bound Conformation. Cell Chem Biol. 2019 Nov 21;26(11):1544-1558.e6. | |||||
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