Target Information

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Target General Information
Drugs and Modes of Action
Drug Binding Sites of Target
Different Human System Profiles of Target
Chemical Structure based Activity Landscape of Target
Target Regulators
Target Profiles in Patients
Target Affiliated Biological Pathways
References
Drug Binding Sites of Target  Top
Ligand Name: Preverex Ligand Info
Structure Description Cryo-EM structure of human glucose transporter GLUT4 bound to cytochalasin B in lipid nanodiscs PDB:7WSM
Method Electron microscopy Resolution 3.25 Å Mutation No [3]
PDB Sequence
TGTLVLAVFS
30
AVLGSLQFGY
40
NIGVINAPQK
50
VIEQSYNETW
60
LGRQGPEGPS
70

SIPPGTLTTL
80
WALSVAIFSV
90
GGMISSFLIG
100
IISQWLGRKR
110
AMLVNNVLAV
120

LGGSLMGLAN
130
AAASYEMLIL
140
GRFLIGAYSG
150
LTSGLVPMYV
160
GEIAPTHLRG
170

ALGTLNQLAI
180
VIGILIAQVL
190
GLESLLGTAS
200
LWPLLLGLTV
210
LPALLQLVLL
220

PFCPESPRYL
230
YIIQNLEGPA
240
RKSLKRLTGW
250
ADVSGVLAEL
260
KDEKRKLERE
270

RPLSLLQLLG
280
SRTHRQPLII
290
AVVLQLSQQL
300
SGINAVFYYS
310
TSIFETAGVG
320

QPAYATIGAG
330
VVNTVFTLVS
340
VLLVERAGRR
350
TLHLLGLAGM
360
CGCAILMTVA
370

LLLLERVPAM
380
SYVSIVAIFG
390
FVAFFEIGPG
400
PIPWFIVAEL
410
FSQGPRPAAM
420

AVAGFSNWTS
430
NFIIGMGFQY
440
VAEAMGPYVF
450
LLFAVLLLGF
460
FIFTFLRVPE
470

TRGRTFDQIS
480
AAFH
Residue
Distance (Å)
PHE38
3.916
ILE42
4.281
SER153
3.533
PRO157
4.017
ASN176
3.833
GLN177
3.569
ILE180
3.691
ILE184
4.100
GLN298
2.479
GLN299
3.127
ILE303
3.910
Residue
Distance (Å)
ASN304
3.999
PHE307
3.308
PHE395
3.944
GLU396
4.016
GLY400
3.582
PRO401
4.195
TRP404
2.966
GLY424
3.760
ASN427
3.631
TRP428
3.522
ASN431
4.083
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
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 Pathway Affiliation of target is determined by the life-essential pathways provided on KEGG database. The target-affiliated pathways were defined based on the following two criteria (a) the pathways of the studied target should be life-essential for both healthy individuals and patients, and (b) the studied target should occupy an upstream position in the pathways and therefore had the ability to regulate biological function.
Targets involved in a fewer pathways have greater likelihood to be successfully developed, while those associated with more human pathways increase the chance of undesirable interferences with other human processes (Pharmacol Rev, 58: 259-279, 2006).
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
Human Pathway Affiliation
Biological Network Descriptors
Protein Name Pfam ID Percentage of Identity (%) E value
Solute carrier family 22 member 7 (SLC22A7)
PF07690
26.934 (94/349) 6.37E-05
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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KEGG Pathway Pathway ID Affiliated Target Pathway Map
FoxO signaling pathway hsa04068 Affiliated Target
  Class: Environmental Information Processing => Signal transduction Pathway Hierarchy
AMPK signaling pathway hsa04152 Affiliated Target
  Class: Environmental Information Processing => Signal transduction Pathway Hierarchy
Insulin signaling pathway hsa04910 Affiliated Target
  Class: Organismal Systems => Endocrine system Pathway Hierarchy
Adipocytokine signaling pathway hsa04920 Affiliated Target
  Class: Organismal Systems => Endocrine system Pathway Hierarchy
Degree 12 Degree centrality 1.29E-03 Betweenness centrality 1.09E-03
Closeness centrality 2.31E-01 Radiality 1.41E+01 Clustering coefficient 1.36E-01
Neighborhood connectivity 2.67E+01 Topological coefficient 1.10E-01 Eccentricity 11
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