Details of the Drug Transporter (DTP)

General Information of Drug Transporter (DTP) (ID: DT1UMXN)

DTP Name Niemann-Pick C1-like protein 1 (SLC65A2)
Gene Name SLC65A2
UniProt ID
Q9UHC9 (NPCL1_HUMAN)
VARIDT ID
DTD0439
3D Structure
Download
2D Sequence (FASTA)
Download
3D Structure (PDB)
Download
Synonyms LDLCQ7; NPC1-like intracellular cholesterol transporter 1; NPC11L1; NPC1L1; SLC65A2
DTP Family Resistance-Nodulation-Cell Division (RND) Superfamily
Eukaryotic (Putative) Sterol Transporter (EST) Family
Sequence
MAEAGLRGWLLWALLLRLAQSEPYTTIHQPGYCAFYDECGKNPELSGSLMTLSNVSCLSN
TPARKITGDHLILLQKICPRLYTGPNTQACCSAKQLVSLEASLSITKALLTRCPACSDNF
VNLHCHNTCSPNQSLFINVTRVAQLGAGQLPAVVAYEAFYQHSFAEQSYDSCSRVRVPAA
ATLAVGTMCGVYGSALCNAQRWLNFQGDTGNGLAPLDITFHLLEPGQAVGSGIQPLNEGV
ARCNESQGDDVATCSCQDCAASCPAIARPQALDSTFYLGQMPGSLVLIIILCSVFAVVTI
LLVGFRVAPARDKSKMVDPKKGTSLSDKLSFSTHTLLGQFFQGWGTWVASWPLTILVLSV
IPVVALAAGLVFTELTTDPVELWSAPNSQARSEKAFHDQHFGPFFRTNQVILTAPNRSSY
RYDSLLLGPKNFSGILDLDLLLELLELQERLRHLQVWSPEAQRNISLQDICYAPLNPDNT
SLYDCCINSLLQYFQNNRTLLLLTANQTLMGQTSQVDWKDHFLYCANAPLTFKDGTALAL
SCMADYGAPVFPFLAIGGYKGKDYSEAEALIMTFSLNNYPAGDPRLAQAKLWEEAFLEEM
RAFQRRMAGMFQVTFMAERSLEDEINRTTAEDLPIFATSYIVIFLYISLALGSYSSWSRV
MVDSKATLGLGGVAVVLGAVMAAMGFFSYLGIRSSLVILQVVPFLVLSVGADNIFIFVLE
YQRLPRRPGEPREVHIGRALGRVAPSMLLCSLSEAICFFLGALTPMPAVRTFALTSGLAV
ILDFLLQMSAFVALLSLDSKRQEASRLDVCCCVKPQELPPPGQGEGLLLGFFQKAYAPFL
LHWITRGVVLLLFLALFGVSLYSMCHISVGLDQELALPKDSYLLDYFLFLNRYFEVGAPV
YFVTTLGYNFSSEAGMNAICSSAGCNNFSFTQKIQYATEFPEQSYLAIPASSWVDDFIDW
LTPSSCCRLYISGPNKDKFCPSTVNSLNCLKNCMSITMGSVRPSVEQFHKYLPWFLNDRP
NIKCPKGGLAAYSTSVNLTSDGQVLDTVAILSPRLEYSGTISAHCNLYLLDSTSRFMAYH
KPLKNSQDYTEALRAARELAANITADLRKVPGTDPAFEVFPYTITNVFYEQYLTILPEGL
FMLSLCLVPTFAVSCLLLGLDLRSGLLNLLSIVMILVDTVGFMALWGISYNAVSLINLVS
AVGMSVEFVSHITRSFAISTKPTWLERAKEATISMGSAVFAGVAMTNLPGILVLGLAKAQ
LIQIFFFRLNLLITLLGLLHGLVFLPVILSYVGPDVNPALALEQKRAEEAVAAVMVASCP
NHPSRVSTADNIYVNHSFEGSIKGAGAISNFLPNNGRQF
Function
This transporter is critical for the uptake of cholesterol across the plasma membrane of the intestinal enterocyte. Is the direct molecular target of ezetimibe, a drug that inhibits cholesterol absorption. Lack of activity leads to multiple lipid transport defects. The protein may have a function in the transport of multiple lipids and their homeostasis, and may play a critical role in regulating lipid metabolism. Acts as a negative regulator of NPC2 and down-regulates its expression and secretion by inhibiting its maturation and accelerating its degradation.
Endogenous Substrate(s) Lipids
TCDB ID
2.A.6.6.6
Gene ID
29881
KEGG Pathway
Fat digestion and absorption (hsa04975 )
Reactome Pathway
Intestinal lipid absorption (R-HSA-8963678 )

Molecular Interaction Atlas (MIA) of This DTP

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DTP
1 Investigative Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cholesterol DMR3J6S Discovery agent N.A. Investigative [3]
------------------------------------------------------------------------------------

Molecular Expression Atlas (MEA) of This DTP

Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This DTP
Disease Name ICD 11 Studied Tissue p-value Fold-Change Z-score
Acute myelocytic leukaemia 2B33.1 Bone marrow 2.83E-02 2.01E-02 1.11E-01
Adrenocortical carcinoma 2D11.Z Kidney 3.55E-01 -2.47E-02 -8.79E-02
Alopecia ED70 Skin from scalp 1.30E-02 2.08E-01 7.80E-01
Alzheimer's disease 8A20 Entorhinal cortex 1.95E-01 -3.72E-02 -2.07E-01
Ankylosing spondylitis FA92.0 Pheripheral blood 5.79E-01 -6.21E-02 -4.73E-01
Aortic stenosis BB70 Calcified aortic valve 6.57E-01 9.93E-02 2.44E-01
Apnea 7A40 Hyperplastic tonsil 7.03E-02 -2.56E-01 -1.25E+00
Arthropathy FA00-FA5Z Peripheral blood 4.17E-01 6.54E-02 5.90E-01
Asthma CA23 Nasal and bronchial airway 7.69E-01 -3.33E-02 -1.46E-01
Atopic dermatitis EA80 Skin 3.32E-01 -4.22E-03 -3.75E-02
Autism 6A02 Whole blood 1.61E-01 -7.72E-02 -4.05E-01
Autoimmune uveitis 9A96 Peripheral monocyte 7.91E-01 7.98E-02 4.10E-01
Autosomal dominant monocytopenia 4B04 Whole blood 9.84E-01 1.22E-02 7.12E-02
Bacterial infection of gingival 1C1H Gingival tissue 7.14E-01 2.55E-02 1.00E-01
Batten disease 5C56.1 Whole blood 1.45E-01 1.21E-01 1.27E+00
Behcet's disease 4A62 Peripheral blood 7.68E-01 -5.97E-02 -2.80E-01
Bipolar disorder 6A60-6A6Z Prefrontal cortex 3.93E-01 2.14E-02 1.41E-01
Bladder cancer 2C94 Bladder tissue 8.69E-08 6.95E-01 6.38E+00
Breast cancer 2C60-2C6Z Breast tissue 4.81E-12 -1.18E-01 -4.47E-01
Cardioembolic stroke 8B11.20 Whole blood 2.29E-01 7.69E-02 5.49E-01
Cervical cancer 2C77 Cervical tissue 9.20E-01 9.37E-02 2.53E-01
Childhood onset rheumatic disease FA20.Z Peripheral blood 6.25E-01 1.08E-03 3.58E-03
Chronic hepatitis C 1E51.1 Whole blood 1.13E-01 1.19E-01 8.23E-01
Chronic obstructive pulmonary disease CA22 Lung tissue 4.71E-01 -6.41E-03 -4.01E-02
Chronic obstructive pulmonary disease CA22 Small airway epithelium 1.65E-04 1.24E-01 7.36E-01
Chronic rhinosinusitis CA0A Sinus mucosa tissue 5.12E-01 -1.05E-01 -7.14E-01
Colon cancer 2B90 Colon tissue 6.05E-02 -1.12E-02 -4.79E-02
Coronary artery disease BA80-BA8Z Peripheral blood 6.82E-02 -2.07E-01 -1.43E+00
Diffuse large B-cell lymphoma 2A81 Tonsil tissue 3.19E-01 -3.13E-02 -1.73E-01
Endometriosis GA10 Endometrium tissue 2.65E-02 1.56E-01 4.32E-01
Familial hypercholesterolemia 5C80.00 Peripheral blood 7.61E-01 -4.43E-02 -2.47E-01
Familial hypercholesterolemia 5C80.00 Whole blood 1.75E-01 -4.92E-02 -2.72E-01
Gastric cancer 2B72 Gastric tissue 5.22E-01 8.67E-03 3.03E-02
Glioblastopma 2A00.00 Nervous tissue 4.45E-57 -2.84E-01 -1.06E+00
Glioma 2A00.0Y-2A00.0Z White matter tissue 6.35E-02 -2.33E-01 -1.09E+00
Head and neck cancer 2D42 Head and neck tissue 3.81E-02 4.56E-02 2.46E-01
HIV-associated neurocognitive impairment 8A2Y-8A2Z White matter tissue 5.66E-01 -6.09E-02 -2.45E-01
Huntington's disease 8A01.10 Whole blood 9.68E-02 1.82E-01 1.16E+00
Idiopathic pulmonary fibrosis CB03.4 Lung tissue 3.98E-01 -6.86E-02 -4.16E-01
Immunodeficiency 4A00-4A20 Peripheral blood 3.43E-02 8.66E-02 7.63E-01
Influenza 1.00E+30 Whole blood 1.12E-01 7.94E-02 1.05E+00
Interstitial cystitis GC00.3 Bladder tissue 1.01E-01 1.84E-01 1.46E+00
Intracranial aneurysm 8B01.0 Intracranial artery 4.59E-01 -2.19E-01 -9.09E-01
Irritable bowel syndrome DD91.0 Rectal colon tissue 1.02E-01 6.33E-02 3.54E-01
Ischemic stroke 8B11 Peripheral blood 2.33E-02 1.24E-01 8.54E-01
Juvenile idiopathic arthritis FA24 Peripheral blood 2.42E-03 1.30E-01 4.97E-01
Lateral sclerosis 8B60.4 Cervical spinal cord 4.19E-01 1.19E-01 4.71E-01
Lateral sclerosis 8B60.4 Skin 8.88E-01 2.90E-02 2.32E-01
Liver cancer 2C12.0 Liver tissue 2.99E-05 -4.78E-01 -8.72E-01
Liver failure DB99.7-DB99.8 Liver tissue 4.88E-02 -3.01E-01 -1.41E+00
Lung cancer 2C25 Lung tissue 1.43E-03 -4.55E-02 -2.03E-01
Lupus erythematosus 4A40 Whole blood 6.05E-02 -6.32E-02 -1.81E-01
Major depressive disorder 6A70-6A7Z Whole blood 4.61E-01 1.66E-02 6.08E-02
Major depressive disorder 6A70-6A7Z Hippocampus 9.91E-01 -4.20E-02 -3.08E-01
Melanoma 2C30 Skin 1.89E-01 -1.99E-01 -4.03E-01
Multiple myeloma 2A83.1 Bone marrow 2.10E-04 -2.72E-01 -2.19E+00
Multiple myeloma 2A83.1 Peripheral blood 4.26E-01 -1.39E-01 -7.91E-01
Multiple sclerosis 8A40 Plasmacytoid dendritic cells 8.85E-01 -2.75E-02 -1.33E-01
Myelodysplastic syndrome 2A36-2A3Z Bone marrow 5.55E-01 -6.07E-02 -4.45E-01
Myelofibrosis 2A20.2 Whole blood 3.56E-01 -5.43E-02 -3.99E-01
Myocardial infarction BA41-BA50 Peripheral blood 1.16E-02 1.57E-01 6.21E-01
Myopathy 8C70.6 Muscle tissue 6.30E-04 -2.96E-01 -2.40E+00
Neonatal sepsis KA60 Whole blood 4.66E-02 1.19E-01 5.17E-01
Neuroectodermal tumour 2A00.11 Brain stem tissue 8.42E-03 -3.89E-01 -1.01E+00
Non-alcoholic fatty liver disease DB92 Liver tissue 3.71E-01 -9.41E-02 -4.19E-01
Obesity related type 2 diabetes 5A11 Omental adipose tissue 4.51E-02 1.48E-01 1.10E+00
Olive pollen allergy CA08.00 Peripheral blood 2.86E-02 2.71E-01 1.55E+00
Oral cancer 2B6E Oral tissue 5.32E-09 -5.48E-01 -1.89E+00
Osteoarthritis FA00-FA0Z Synovial tissue 7.27E-02 -2.83E-02 -1.31E-01
Osteoporosis FB83.1 Bone marrow 9.76E-02 1.10E-01 5.96E-01
Ovarian cancer 2C73 Ovarian tissue 4.54E-01 -5.82E-02 -1.92E-01
Pancreatic cancer 2C10 Pancreas 3.66E-02 -2.21E-01 -6.67E-01
Parkinson's disease 8A00.0 Substantia nigra tissue 5.43E-01 1.43E-01 6.19E-01
Pediatric respiratory syncytial virus infection CA40.11 Peripheral blood 6.60E-01 -2.89E-02 -2.22E-01
Pituitary cancer 2D12 Pituitary tissue 1.80E-01 1.62E-01 6.03E-01
Pituitary gonadotrope tumour 2D12 Pituitary tissue 1.87E-01 2.55E-01 1.18E+00
Polycystic ovary syndrome 5A80.1 Vastus lateralis muscle 6.99E-01 4.42E-02 3.36E-01
Polycythemia vera 2A20.4 Whole blood 3.19E-01 1.87E-02 1.23E-01
Pompe disease 5C51.3 Biceps muscle 3.08E-01 -7.15E-02 -5.35E-01
Preterm birth KA21.4Z Myometrium 6.70E-01 -1.40E-02 -9.43E-02
Prostate cancer 2C82 Prostate 3.53E-01 -1.43E-01 -4.96E-01
Psoriasis EA90 Skin 1.81E-01 -3.36E-02 -1.26E-01
Rectal cancer 2B92 Rectal colon tissue 6.56E-01 -1.96E-02 -1.95E-01
Renal cancer 2C90-2C91 Kidney 1.56E-01 -3.06E-01 -8.17E-01
Retinoblastoma 2D02.2 Uvea 7.33E-06 -2.95E-01 -3.09E+00
Rheumatoid arthritis FA20 Synovial tissue 1.28E-01 -2.64E-01 -7.29E-01
Rhinovirus infection CA42.1 Nasal epithelium tissue 6.93E-01 4.14E-02 2.19E-01
Schizophrenia 6A20 Prefrontal cortex 2.31E-01 5.14E-02 1.96E-01
Schizophrenia 6A20 Superior temporal cortex 1.56E-01 -6.62E-02 -4.38E-01
Scleroderma 4A42.Z Whole blood 6.43E-02 5.84E-02 7.56E-01
Seizure 8A60-8A6Z Whole blood 9.18E-01 -1.79E-02 -8.44E-02
Sensitive skin EK0Z Skin 6.46E-01 -9.35E-02 -4.23E-01
Sepsis with septic shock 1G41 Whole blood 2.72E-04 6.30E-02 3.20E-01
Shwachman-Diamond syndrome 3A70.0 Bone marrow 3.89E-01 1.99E-01 5.19E-01
Sickle cell disease 3A51.0-3A51.3 Peripheral blood 6.35E-03 2.28E-01 1.08E+00
Simpson golabi behmel syndrome LD2C Adipose tissue 3.26E-01 -8.64E-02 -7.01E-01
Sjogren's syndrome 4A43.2 Salivary gland tissue 8.79E-01 -2.16E-02 -1.06E-01
Skin cancer 2C30-2C3Z Skin 8.87E-05 -9.35E-02 -3.23E-01
Thrombocythemia 3B63 Whole blood 5.04E-01 3.16E-02 2.36E-01
Thrombocytopenia 3B64 Whole blood 5.49E-01 9.92E-02 4.47E-01
Thyroid cancer 2D10 Thyroid 4.40E-03 6.13E-02 3.26E-01
Tibial muscular dystrophy 8C75 Muscle tissue 1.06E-04 -3.27E-01 -2.07E+00
Tuberous sclerosis complex LD2D.2 Perituberal tissue 5.21E-02 1.50E-01 1.83E+00
Type 2 diabetes 5A11 Liver tissue 9.73E-01 -3.45E-02 -2.37E-01
Ureter cancer 2C92 Urothelium 8.40E-01 1.02E-03 5.90E-03
Uterine cancer 2C78 Endometrium tissue 4.52E-07 1.47E-01 5.01E-01
Vitiligo ED63.0 Skin 3.91E-01 3.15E-02 3.92E-01
------------------------------------------------------------------------------------
⏷ Show the Full List of Expression Under 107 Diseases

The Drug Therapeutic Target (DTT) Role of This DTP

DTP DTT Name Niemann-Pick C1-like protein 1 (NPC1L1) DTT Info
DTP DTT Type Successful
1 Approved Drug(s) Targeting This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Ezetimibe DM7A8TW Atherosclerosis BD40 Approved [1]
------------------------------------------------------------------------------------
1 Investigative Drug(s) Targeting This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Ezetimibe-glucuronide DM5V3S7 Discovery agent N.A. Investigative [2]
------------------------------------------------------------------------------------

References

1 Update on patented cholesterol absorption inhibitors. Expert Opin Ther Pat. 2009 Aug;19(8):1083-107.
2 Spiroimidazolidinone NPC1L1 inhibitors. 1: Discovery by 3D-similarity-based virtual screening. Bioorg Med Chem Lett. 2009 Jun 1;19(11):2965-8.
3 Niemann-Pick C1 Like 1 protein is critical for intestinal cholesterol absorption. Science. 2004 Feb 20;303(5661):1201-4.