Target Information
| Target General Information | Top | |||||
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| Target ID |
T14200
(Former ID: TTDI00034)
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| Target Name |
ATP-binding cassette transporter G5 (ABCG5)
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| Synonyms |
Sterolin1; ATPbinding cassette subfamily G member 5; ABCG5
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| Gene Name |
ABCG5
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| Target Type |
Literature-reported target
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| Function |
Transporter that appears to play an indispensable role in the selective transportof the dietary cholesterol in and out of the enterocytes and in the selective sterol excretion by the liver into bile.
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| BioChemical Class |
ABC transporter
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| UniProt ID | ||||||
| Sequence |
MGDLSSLTPGGSMGLQVNRGSQSSLEGAPATAPEPHSLGILHASYSVSHRVRPWWDITSC
RQQWTRQILKDVSLYVESGQIMCILGSSGSGKTTLLDAMSGRLGRAGTFLGEVYVNGRAL RREQFQDCFSYVLQSDTLLSSLTVRETLHYTALLAIRRGNPGSFQKKVEAVMAELSLSHV ADRLIGNYSLGGISTGERRRVSIAAQLLQDPKVMLFDEPTTGLDCMTANQIVVLLVELAR RNRIVVLTIHQPRSELFQLFDKIAILSFGELIFCGTPAEMLDFFNDCGYPCPEHSNPFDF YMDLTSVDTQSKEREIETSKRVQMIESAYKKSAICHKTLKNIERMKHLKTLPMVPFKTKD SPGVFSKLGVLLRRVTRNLVRNKLAVITRLLQNLIMGLFLLFFVLRVRSNVLKGAIQDRV GLLYQFVGATPYTGMLNAVNLFPVLRAVSDQESQDGLYQKWQMMLAYALHVLPFSVVATM IFSSVCYWTLGLHPEVARFGYFSAALLAPHLIGEFLTLVLLGIVQNPNIVNSVVALLSIA GVLVGSGFLRNIQEMPIPFKIISYFTFQKYCSEILVVNEFYGLNFTCGSSNVSVTTNPMC AFTQGIQFIEKTCPGATSRFTMNFLILYSFIPALVILGIVVFKIRDHLISR Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | PDB | ||||
| HIT2.0 ID | T90K33 | |||||
| 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: Cholesterol | Ligand Info | |||||
| Structure Description | The structure of human ABCG5/ABCG8 purified from mammalian cells | PDB:7R8A | ||||
| Method | Electron microscopy | Resolution | 2.90 Å | Mutation | No | [2] |
| PDB Sequence |
PHSLGILHAS
44 YSRQILKDVS73 LYVESGQIMC83 ILGSSGSGKT93 TLLDAMSGRG107 TFLGEVYVNG 117 RALRREQFQD127 CFSYVLQSDT137 LLSSLTVRET147 LHYTALLAIR157 RGNPGSFQKK 167 VEAVMAELSL177 SHVADRLIGN187 YSLGGISTGE197 RRRVSIAAQL207 LQDPKVMLFD 217 EPTTGLDCMT227 ANQIVVLLVE237 LARRNRIVVL247 TIHQPRSELF257 QLFDKIAILS 267 FGELIFCGTP277 AEMLDFFNDC287 GYPCPEHSNP297 FDFYMDLTSV307 DTQSKEREIE 317 TSKRVQMIES327 AYKKSAICHK337 TLKNIERMKH347 LKTLPMVPFK357 TKDSPGVFSK 367 LGVLLRRVTR377 NLVRNKLAVI387 TRLLQNLIMG397 LFLLFFVLRV407 RSNVLKGAIQ 417 DRVGLLYQFV427 GATPYTGMLN437 AVNLFPVLRA447 VSDQESQDGL457 YQKWQMMLAY 467 ALHVLPFSVV477 ATMIFSSVCY487 WTLGLHPEVA497 RFGYFSAALL507 APHLIGEFLT 517 LVLLGIVQNP527 NIVNSVVALL537 SIAGVLVGSG547 FLRNIQEMPI557 PFKIISYFTF 567 QKYCSEILVV577 NEFYGLNFTC587 GNPMCAFTQG605 IQFIEKTCPG615 ATSRFTMNFL 625 ILYSFIPALV635 ILGIVVFKIR645 DHLI
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| Click to View More Binding Site Information of This Target and Ligand Pair | ||||||
| Ligand Name: Ergosterol | Ligand Info | |||||
| Structure Description | The structure of human ABCG5/ABCG8 purified from yeast | PDB:7R89 | ||||
| Method | Electron microscopy | Resolution | 2.60 Å | Mutation | No | [2] |
| PDB Sequence |
PHSLGILHAS
44 YSRQILKDVS73 LYVESGQIMC83 ILGSSGSGKT93 TLLDAMSGRG107 TFLGEVYVNG 117 RALRREQFQD127 CFSYVLQSDT137 LLSSLTVRET147 LHYTALLAIR157 RGNPGSFQKK 167 VEAVMAELSL177 SHVADRLIGN187 YSLGGISTGE197 RRRVSIAAQL207 LQDPKVMLFD 217 EPTTGLDCMT227 ANQIVVLLVE237 LARRNRIVVL247 TIHQPRSELF257 QLFDKIAILS 267 FGELIFCGTP277 AEMLDFFNDC287 GYPCPEHSNP297 FDFYMDLTSV307 DTQSKEREIE 317 TSKRVQMIES327 AYKKSAICHK337 TLKNIERMKH347 LKTLPMVPFK357 TKDSPGVFSK 367 LGVLLRRVTR377 NLVRNKLAVI387 TRLLQNLIMG397 LFLLFFVLRV407 RSNVLKGAIQ 417 DRVGLLYQFV427 GATPYTGMLN437 AVNLFPVLRA447 VSDQESQDGL457 YQKWQMMLAY 467 ALHVLPFSVV477 ATMIFSSVCY487 WTLGLHPEVA497 RFGYFSAALL507 APHLIGEFLT 517 LVLLGIVQNP527 NIVNSVVALL537 SIAGVLVGSG547 FLRNIQEMPI557 PFKIISYFTF 567 QKYCSEILVV577 NEFYGLNFTC587 GNPMCAFTQG605 IQFIEKTCPG615 ATSRFTMNFL 625 ILYSFIPALV635 ILGIVVFKIR645 DHLI
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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 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 Pathway Affiliation
Biological Network Descriptors
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There is no similarity protein (E value < 0.005) for this target
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| KEGG Pathway | Pathway ID | Affiliated Target | Pathway Map |
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| ABC transporters | hsa02010 | Affiliated Target |
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| Class: Environmental Information Processing => Membrane transport | Pathway Hierarchy | ||
| Fat digestion and absorption | hsa04975 | Affiliated Target |
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| Class: Organismal Systems => Digestive system | Pathway Hierarchy | ||
| Bile secretion | hsa04976 | Affiliated Target |
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| Class: Organismal Systems => Digestive system | Pathway Hierarchy | ||
| Cholesterol metabolism | hsa04979 | Affiliated Target |
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| Class: Organismal Systems => Digestive system | Pathway Hierarchy | ||
| Degree | 3 | Degree centrality | 3.22E-04 | Betweenness centrality | 2.10E-09 |
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| Closeness centrality | 1.86E-01 | Radiality | 1.31E+01 | Clustering coefficient | 6.67E-01 |
| Neighborhood connectivity | 1.17E+01 | Topological coefficient | 5.30E-01 | Eccentricity | 12 |
| Download | Click to Download the Full PPI Network of This Target | ||||
| References | Top | |||||
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| REF 1 | ABCG5/ABCG8 in cholesterol excretion and atherosclerosis. Clin Chim Acta. 2014 Jan 20;428:82-8. | |||||
| REF 2 | Molecular basis of cholesterol efflux via ABCG subfamily transporters. Proc Natl Acad Sci U S A. 2021 Aug 24;118(34):e2110483118. | |||||
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