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 Regulators
Target Profiles in Patients
Target Affiliated Biological Pathways
References
Drug Binding Sites of Target  Top
Ligand Name: Cholesterol Ligand Info
Structure Description Solution structure of double super helix model PDB:3K2S
Method Solution scattering Resolution N.A. Mutation No [17]
PDB Sequence
DEPPQSPWDR
10
VKDLATVYVD
20
VLKDSGRDYV
30
SQFEGSALGK
40
QLNLKLLDNW
50

DSVTSTFSKL
60
REQLGPVTQE
70
FWDNLEKETE
80
GLRQEMSKDL
90
EEVKAKVQPY
100

LDDFQKKWQE
110
EMELYRQKVE
120
PLRAELQEGA
130
RQKLHELQEK
140
LSPLGEEMRD
150

RARAHVDALR
160
THLAPYSDEL
170
RQRLAARLEA
180
LKENGGARLA
190
EYHAKATEHL
200

STLSEKAKPA
210
LEDLRQGLLP
220
VLESFKVSFL
230
SALEEYTKKL
240
NTQ
Residue
Distance (Å)
THR202
4.101
LEU203
3.305
LYS206
3.488
ALA207
4.588
Residue
Distance (Å)
ALA210
3.519
ASP213
3.414
LEU214
3.576
Ligand Name: 1,2-Dimyristoyl-sn-glycero-3-phosphocholine Ligand Info
Structure Description MT1-MMP HPX Domain with Blade 2 Loop Bound to Nanodiscs PDB:6CM1
Method Solution NMR Resolution N.A. Mutation No [18]
PDB Sequence
STFSKLREQL
64
GPVTQEFWDN
74
LEKETEGLRQ
84
EMSKDLEEVK
94
AKVQPYLDDF
104

QKKWQEEMEL
114
YRQKVEPYLD
124
DFQKKWQEEM
134
ELYRQKVEPL
144
RAELQEGARQ
154

KLHELQEKLS
164
PLGEEMRDRA
174
RAHVDALRTH
184
LAPYSDELRQ
194
RLAARLEALK
204

ENGGARLAEY
214
HAKATEHLST
224
LSEKAKPALE
234
DLRQGLLPVL
244
ESFKVSFLSA
254

LEEYTKKLNT
264
Q
Residue
Distance (Å)
SER55
1.666
PHE57
2.257
SER58
2.230
ARG61
1.642
THR68
3.307
GLN69
4.754
TRP72
2.084
ASP73
4.931
LEU75
2.169
GLU76
2.068
LYS77
3.913
THR79
2.406
GLU80
2.069
ARG83
1.616
GLN84
4.543
MET86
2.259
LEU90
2.296
LYS94
1.716
GLN98
4.130
LEU101
4.290
ASP102
2.871
GLN105
2.554
TRP108
2.091
GLN109
2.101
MET112
2.179
GLU113
2.624
TYR115
2.419
ARG116
2.103
VAL119
3.261
GLU120
2.604
LEU123
2.497
ASP124
3.562
PHE126
2.717
GLN127
2.622
TRP130
2.228
GLN131
4.036
MET134
2.313
TYR137
2.004
ARG138
2.220
GLN139
4.700
VAL141
2.517
GLU142
3.682
ARG145
1.783
ALA146
4.388
LEU148
2.346
GLN149
2.869
ALA152
2.282
ARG153
2.414
LYS155
2.594
LEU156
2.157
HIS157
4.932
LEU159
2.221
GLN160
2.325
GLU161
4.457
LEU163
2.489
SER164
2.360
LEU166
2.255
GLY167
2.197
GLU168
4.083
MET170
2.118
ARG171
2.704
ASP172
4.327
ARG173
3.628
Residue
Distance (Å)
ALA174
2.453
ARG175
2.252
HIS177
2.499
VAL178
2.278
ASP179
4.840
LEU181
2.418
ARG182
2.175
THR183
4.979
LEU185
2.149
ALA186
2.284
TYR188
2.892
SER189
2.385
ASP190
4.712
LEU192
2.723
ARG193
1.874
GLN194
2.246
LEU196
2.484
ALA197
2.726
ARG199
4.912
LEU200
2.081
GLU201
4.790
LEU203
2.288
LYS204
2.044
GLU205
4.396
ASN206
4.730
GLY207
2.420
GLY208
2.193
ALA209
4.795
ARG210
2.219
LEU211
2.289
TYR214
2.480
HIS215
2.259
ALA218
2.678
THR219
3.890
LEU222
2.203
SER223
2.020
THR224
4.299
LEU225
2.226
SER226
2.061
GLU227
2.415
LYS228
2.626
ALA229
2.344
LYS230
3.473
ALA232
2.561
LEU233
2.154
LEU236
2.238
ARG237
2.353
LEU240
2.024
LEU241
3.085
VAL243
2.494
LEU244
2.094
PHE247
2.279
LYS248
1.920
SER250
2.153
PHE251
2.269
LEU252
2.919
ALA254
2.475
LEU255
2.212
TYR258
1.703
LYS261
3.864
LEU262
2.575
GLN265
2.521
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
Laminin subunit alpha-2 (LAMA2)
PF00052 ; 
PF00053 ; 
PF00054 ; 
PF06008 ; 
PF06009 ; 
PF00055
More >>
 25.000 (37/148) 8.88E-04
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      
 Download Picture         KEGG Link      
 Download Picture         KEGG Link      
 Download Picture         KEGG Link      
KEGG Pathway Pathway ID Affiliated Target Pathway Map
PPAR signaling pathway hsa03320 Affiliated Target
  Class: Organismal Systems => Endocrine system Pathway Hierarchy
Fat digestion and absorption hsa04975 Affiliated Target
  Class: Organismal Systems => Digestive system Pathway Hierarchy
Vitamin digestion and absorption hsa04977 Affiliated Target
  Class: Organismal Systems => Digestive system Pathway Hierarchy
Cholesterol metabolism hsa04979 Affiliated Target
  Class: Organismal Systems => Digestive system Pathway Hierarchy
Degree 34 Degree centrality 3.65E-03 Betweenness centrality 3.47E-03
Closeness centrality 2.15E-01 Radiality 1.38E+01 Clustering coefficient 1.23E-01
Neighborhood connectivity 1.07E+01 Topological coefficient 6.17E-02 Eccentricity 11
Download Click to Download the Full PPI Network of This Target

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