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
Target Profiles in Patients
Target Affiliated Biological Pathways
References
Drug Binding Sites of Target  Top
Ligand Name: Oleic acid Ligand Info
Structure Description Crystal Structure Analysis of GM2-activator protein complexed with phosphatidylcholine PDB:2AG4
Method X-ray diffraction Resolution 1.80 Å Mutation No [4]
PDB Sequence
HMSSFSWDNC
10
DEGKDPAVIR
20
SLTLEPDPIV
30
VPGNVTLSVV
40
GSTSVPLSSP
50

LKVDLVLEKE
60
VAGLWIKIPC
70
TDYIGSCTFE
80
HFCDVLDMLI
90
PTGEPCPEPL
100

RTYGLPCHCP
110
FKEGTYSLPK
120
SEFVVPDLEL
130
PSWLTTGNYR
140
IESVLSSSGK
150

RLGCIKIAAS
160
LKGI
Residue
Distance (Å)
LEU37
3.295
VAL39
3.760
PRO97
3.831
GLU98
3.722
Residue
Distance (Å)
PRO99
4.264
LEU100
4.067
LEU118
4.004
PHE123
4.120
Click to View More Binding Site Information of This Target and Ligand Pair
Ligand Name: Lauric acid Ligand Info
Structure Description Crystal Structure analysis of GM2-Activator protein complexed with phosphatidylcholine PDB:2AF9
Method X-ray diffraction Resolution 2.00 Å Mutation No [4]
PDB Sequence
MSSFSWDNCD
9
EGKDPAVIRS
19
LTLEPDPIVV
29
PGNVTLSVVG
39
STSVPLSSPL
49

KVDLVLEKEV
59
AGLWIKIPCT
69
DYIGSCTFEH
79
FCDVLDMLIP
89
TGEPCPEPLR
99

TYGLPCHCPF
109
KEGTYSLPKS
119
EFVVPDLELP
129
SWLTTGNYRI
139
ESVLSSSGKR
149

LGCIKIAASL
159
KGI
Residue
Distance (Å)
LEU45
3.872
LEU49
3.870
VAL51
3.461
LEU53
3.965
LEU55
4.279
LYS57
3.511
ILE66
4.456
PHE80
3.186
PHE109
3.072
LEU132
3.035
THR133
4.533
TYR137
3.146
Residue
Distance (Å)
ARG138
4.151
ILE139
3.326
GLU140
4.535
SER141
3.314
LEU143
4.991
ILE153
3.348
LYS154
4.842
ILE155
3.328
ALA156
3.948
ALA157
3.513
LEU159
3.568
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
There is no similarity protein (E value < 0.005) for this target
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.
 Download Picture         KEGG Link      
KEGG Pathway Pathway ID Affiliated Target Pathway Map
Lysosome hsa04142 Affiliated Target
  Class: Cellular Processes => Transport and catabolism Pathway Hierarchy
Degree 2 Degree centrality 2.15E-04 Betweenness centrality 0.00E+00
Closeness centrality 1.08E-01 Radiality 9.72E+00 Clustering coefficient 1.00E+00
Neighborhood connectivity 5.00E+00 Topological coefficient 1.00E+00 Eccentricity 15
Download Click to Download the Full PPI Network of This Target

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