Details of the Target
General Information of Target
| Target ID | LDTP03111 | |||||
|---|---|---|---|---|---|---|
| Target Name | Phosphatidylcholine translocator ABCB4 (ABCB4) | |||||
| Gene Name | ABCB4 | |||||
| Gene ID | 5244 | |||||
| Synonyms |
MDR3; PGY3; Phosphatidylcholine translocator ABCB4; EC 7.6.2.1; ATP-binding cassette sub-family B member 4; Multidrug resistance protein 3; P-glycoprotein 3 |
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| 3D Structure | ||||||
| Sequence |
MDLEAAKNGTAWRPTSAEGDFELGISSKQKRKKTKTVKMIGVLTLFRYSDWQDKLFMSLG
TIMAIAHGSGLPLMMIVFGEMTDKFVDTAGNFSFPVNFSLSLLNPGKILEEEMTRYAYYY SGLGAGVLVAAYIQVSFWTLAAGRQIRKIRQKFFHAILRQEIGWFDINDTTELNTRLTDD ISKISEGIGDKVGMFFQAVATFFAGFIVGFIRGWKLTLVIMAISPILGLSAAVWAKILSA FSDKELAAYAKAGAVAEEALGAIRTVIAFGGQNKELERYQKHLENAKEIGIKKAISANIS MGIAFLLIYASYALAFWYGSTLVISKEYTIGNAMTVFFSILIGAFSVGQAAPCIDAFANA RGAAYVIFDIIDNNPKIDSFSERGHKPDSIKGNLEFNDVHFSYPSRANVKILKGLNLKVQ SGQTVALVGSSGCGKSTTVQLIQRLYDPDEGTINIDGQDIRNFNVNYLREIIGVVSQEPV LFSTTIAENICYGRGNVTMDEIKKAVKEANAYEFIMKLPQKFDTLVGERGAQLSGGQKQR IAIARALVRNPKILLLDEATSALDTESEAEVQAALDKAREGRTTIVIAHRLSTVRNADVI AGFEDGVIVEQGSHSELMKKEGVYFKLVNMQTSGSQIQSEEFELNDEKAATRMAPNGWKS RLFRHSTQKNLKNSQMCQKSLDVETDGLEANVPPVSFLKVLKLNKTEWPYFVVGTVCAIA NGGLQPAFSVIFSEIIAIFGPGDDAVKQQKCNIFSLIFLFLGIISFFTFFLQGFTFGKAG EILTRRLRSMAFKAMLRQDMSWFDDHKNSTGALSTRLATDAAQVQGATGTRLALIAQNIA NLGTGIIISFIYGWQLTLLLLAVVPIIAVSGIVEMKLLAGNAKRDKKELEAAGKIATEAI ENIRTVVSLTQERKFESMYVEKLYGPYRNSVQKAHIYGITFSISQAFMYFSYAGCFRFGA YLIVNGHMRFRDVILVFSAIVFGAVALGHASSFAPDYAKAKLSAAHLFMLFERQPLIDSY SEEGLKPDKFEGNITFNEVVFNYPTRANVPVLQGLSLEVKKGQTLALVGSSGCGKSTVVQ LLERFYDPLAGTVFVDFGFQLLDGQEAKKLNVQWLRAQLGIVSQEPILFDCSIAENIAYG DNSRVVSQDEIVSAAKAANIHPFIETLPHKYETRVGDKGTQLSGGQKQRIAIARALIRQP QILLLDEATSALDTESEKVVQEALDKAREGRTCIVIAHRLSTIQNADLIVVFQNGRVKEH GTHQQLLAQKGIYFSMVSVQAGTQNL |
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| Target Type |
Clinical trial
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| Target Bioclass |
Enzyme
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| Family |
ABC transporter superfamily, ABCB family, Multidrug resistance exporter (TC 3.A.1.201) subfamily
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| Subcellular location |
Cell membrane
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| Function |
[Isoform 1]: Energy-dependent phospholipid efflux translocator that acts as a positive regulator of biliary lipid secretion. Functions as a floppase that translocates specifically phosphatidylcholine (PC) from the inner to the outer leaflet of the canalicular membrane bilayer into the canaliculi of hepatocytes. Translocation of PC makes the biliary phospholipids available for extraction into the canaliculi lumen by bile salt mixed micelles and therefore protects the biliary tree from the detergent activity of bile salts . Plays a role in the recruitment of phosphatidylcholine (PC), phosphatidylethanolamine (PE) and sphingomyelin (SM) molecules to nonraft membranes and to further enrichment of SM and cholesterol in raft membranes in hepatocytes. Required for proper phospholipid bile formation. Indirectly involved in cholesterol efflux activity from hepatocytes into the canalicular lumen in the presence of bile salts in an ATP-dependent manner. Promotes biliary phospholipid secretion as canaliculi-containing vesicles from the canalicular plasma membrane. In cooperation with ATP8B1, functions to protect hepatocytes from the deleterious detergent activity of bile salts. Does not confer multidrug resistance.
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| TTD ID | ||||||
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| Ensemble ID | ||||||
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| ChEMBL ID | ||||||
Probe(s) Labeling This Target
ABPP Probe
| Probe name | Structure | Binding Site(Ratio) | Interaction ID | Ref | |
|---|---|---|---|---|---|
|
DBIA Probe Info |
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C1074(0.93) | LDD3314 | [1] | |
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IA-alkyne Probe Info |
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N.A. | LDD0165 | [2] | |
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IPM Probe Info |
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N.A. | LDD0025 | [3] | |
Competitor(s) Related to This Target
The Interaction Atlas With This Target
The Drug(s) Related To This Target
Approved
| Drug Name | Drug Type | External ID | |||
|---|---|---|---|---|---|
| Etravirine | Small molecular drug | DB06414 | |||
| Silodosin | Small molecular drug | DB06207 | |||
Phase 2
| Drug Name | Drug Type | External ID | |||
|---|---|---|---|---|---|
| Encequidar | Small molecular drug | D9UGX7 | |||
Discontinued
| Drug Name | Drug Type | External ID | |||
|---|---|---|---|---|---|
| Dexniguldipine | Small molecular drug | D0B1MJ | |||
| Dofequidar Fumarate | Small molecular drug | D0H0EM | |||
| Laniquidar | Small molecular drug | D0A5MI | |||
| Ly335979 | Small molecular drug | D06DCL | |||
References