Details of the Drug Transporter (DTP)

General Information of Drug Transporter (DTP) (ID: DTI58LU)

DTP Name Sulfonylurea receptor 1 (ABCC8)
Gene Name ABCC8
UniProt ID
Q09428 (ABCC8_HUMAN)
VARIDT ID
DTD0061
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Synonyms ATP-binding cassette sub-family C member 8; ABCC8; ABC36; HRINS; SUR; SUR1; HHF1; TNDM2; SUR1delta2
DTP Family ATP-Binding Cassette (ABC) Superfamily
Drug Conjugate Transporter (DCT) Family (ABCC)
Sequence
MPLAFCGSENHSAAYRVDQGVLNNGCFVDALNVVPHVFLLFITFPILFIGWGSQSSKVHI
HHSTWLHFPGHNLRWILTFMLLFVLVCEIAEGILSDGVTESHHLHLYMPAGMAFMAAVTS
VVYYHNIETSNFPKLLIALLVYWTLAFITKTIKFVKFLDHAIGFSQLRFCLTGLLVILYG
MLLLVEVNVIRVRRYIFFKTPREVKPPEDLQDLGVRFLQPFVNLLSKGTYWWMNAFIKTA
HKKPIDLRAIGKLPIAMRALTNYQRLCEAFDAQVRKDIQGTQGARAIWQALSHAFGRRLV
LSSTFRILADLLGFAGPLCIFGIVDHLGKENDVFQPKTQFLGVYFVSSQEFLANAYVLAV
LLFLALLLQRTFLQASYYVAIETGINLRGAIQTKIYNKIMHLSTSNLSMGEMTAGQICNL
VAIDTNQLMWFFFLCPNLWAMPVQIIVGVILLYYILGVSALIGAAVIILLAPVQYFVATK
LSQAQRSTLEYSNERLKQTNEMLRGIKLLKLYAWENIFRTRVETTRRKEMTSLRAFAIYT
SISIFMNTAIPIAAVLITFVGHVSFFKEADFSPSVAFASLSLFHILVTPLFLLSSVVRST
VKALVSVQKLSEFLSSAEIREEQCAPHEPTPQGPASKYQAVPLRVVNRKRPAREDCRGLT
GPLQSLVPSADGDADNCCVQIMGGYFTWTPDGIPTLSNITIRIPRGQLTMIVGQVGCGKS
SLLLAALGEMQKVSGAVFWSSLPDSEIGEDPSPERETATDLDIRKRGPVAYASQKPWLLN
ATVEENIIFESPFNKQRYKMVIEACSLQPDIDILPHGDQTQIGERGINLSGGQRQRISVA
RALYQHANVVFLDDPFSALDIHLSDHLMQAGILELLRDDKRTVVLVTHKLQYLPHADWII
AMKDGTIQREGTLKDFQRSECQLFEHWKTLMNRQDQELEKETVTERKATEPPQGLSRAMS
SRDGLLQDEEEEEEEAAESEEDDNLSSMLHQRAEIPWRACAKYLSSAGILLLSLLVFSQL
LKHMVLVAIDYWLAKWTDSALTLTPAARNCSLSQECTLDQTVYAMVFTVLCSLGIVLCLV
TSVTVEWTGLKVAKRLHRSLLNRIILAPMRFFETTPLGSILNRFSSDCNTIDQHIPSTLE
CLSRSTLLCVSALAVISYVTPVFLVALLPLAIVCYFIQKYFRVASRDLQQLDDTTQLPLL
SHFAETVEGLTTIRAFRYEARFQQKLLEYTDSNNIASLFLTAANRWLEVRMEYIGACVVL
IAAVTSISNSLHRELSAGLVGLGLTYALMVSNYLNWMVRNLADMELQLGAVKRIHGLLKT
EAESYEGLLAPSLIPKNWPDQGKIQIQNLSVRYDSSLKPVLKHVNALIAPGQKIGICGRT
GSGKSSFSLAFFRMVDTFEGHIIIDGIDIAKLPLHTLRSRLSIILQDPVLFSGTIRFNLD
PERKCSDSTLWEALEIAQLKLVVKALPGGLDAIITEGGENFSQGQRQLFCLARAFVRKTS
IFIMDEATASIDMATENILQKVVMTAFADRTVVTIAHRVHTILSADLVIVLKRGAILEFD
KPEKLLSRKDSVFASFVRADK
Function This transporter is subunit of the beta-cell ATP-sensitive potassium channel (KATP) and it regulator of ATP-sensitive K+ channels and insulin release.
TCDB ID
3.A.1.208.4
Gene ID
6833
KEGG Pathway
ABC transporters (hsa02010 )
Insulin secretion (hsa04911 )
Type II diabetes mellitus (hsa04930 )
Reactome Pathway
Regulation of insulin secretion (R-HSA-422356 )
Defective ABCC8 can cause hypo- and hyper-glycemias (R-HSA-5683177 )
ATP sensitive Potassium channels (R-HSA-1296025 )

Molecular Interaction Atlas (MIA) of This DTP

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DTP
1 Approved Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Tolbutamide DM02AWV Advanced cancer 2A00-2F9Z Approved [10]
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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 7.13E-01 -2.09E-03 -7.73E-03
Adrenocortical carcinoma 2D11.Z Kidney 1.63E-03 -3.30E-01 -6.43E-01
Alopecia ED70 Skin from scalp 5.63E-01 2.06E-02 8.16E-02
Alzheimer's disease 8A20 Entorhinal cortex 5.65E-03 -7.02E-02 -3.19E-01
Ankylosing spondylitis FA92.0 Pheripheral blood 2.86E-01 -4.48E-02 -4.30E-01
Aortic stenosis BB70 Calcified aortic valve 7.76E-01 -2.00E-01 -2.68E-01
Apnea 7A40 Hyperplastic tonsil 5.81E-01 -2.36E-01 -9.12E-01
Arthropathy FA00-FA5Z Peripheral blood 4.27E-01 5.83E-03 4.03E-02
Asthma CA23 Nasal and bronchial airway 1.56E-01 -3.96E-02 -9.37E-02
Atopic dermatitis EA80 Skin 3.44E-02 -1.16E-01 -1.04E+00
Autism 6A02 Whole blood 5.78E-01 4.02E-02 1.86E-01
Autoimmune uveitis 9A96 Peripheral monocyte 1.89E-01 -4.95E-02 -3.03E-01
Autosomal dominant monocytopenia 4B04 Whole blood 2.73E-01 7.35E-02 5.17E-01
Bacterial infection of gingival 1C1H Gingival tissue 7.38E-01 1.43E-02 4.91E-02
Batten disease 5C56.1 Whole blood 8.19E-01 1.84E-02 1.23E-01
Behcet's disease 4A62 Peripheral blood 9.35E-02 1.20E-01 5.49E-01
Bipolar disorder 6A60-6A6Z Prefrontal cortex 7.45E-01 -2.57E-02 -2.16E-01
Bladder cancer 2C94 Bladder tissue 1.68E-05 4.15E-01 3.29E+00
Breast cancer 2C60-2C6Z Breast tissue 3.38E-06 6.01E-02 1.54E-01
Cardioembolic stroke 8B11.20 Whole blood 6.36E-01 -6.90E-03 -3.96E-02
Cervical cancer 2C77 Cervical tissue 3.19E-01 8.06E-02 2.85E-01
Childhood onset rheumatic disease FA20.Z Peripheral blood 9.33E-01 8.92E-02 3.13E-01
Chronic hepatitis C 1E51.1 Whole blood 1.06E-01 1.35E-01 8.25E-01
Chronic obstructive pulmonary disease CA22 Lung tissue 2.48E-02 1.04E-01 3.79E-01
Chronic obstructive pulmonary disease CA22 Small airway epithelium 6.55E-02 1.00E-01 4.41E-01
Chronic rhinosinusitis CA0A Sinus mucosa tissue 2.44E-01 5.28E-02 5.48E-01
Colon cancer 2B90 Colon tissue 4.03E-26 -2.14E-01 -1.12E+00
Coronary artery disease BA80-BA8Z Peripheral blood 2.27E-01 9.61E-02 1.99E+00
Diffuse large B-cell lymphoma 2A81 Tonsil tissue 6.31E-01 3.29E-03 1.75E-02
Endometriosis GA10 Endometrium tissue 2.16E-01 -7.59E-02 -1.55E-01
Familial hypercholesterolemia 5C80.00 Peripheral blood 2.82E-01 -1.15E-01 -4.49E-01
Familial hypercholesterolemia 5C80.00 Whole blood 4.62E-03 -3.65E-01 -1.32E+00
Gastric cancer 2B72 Gastric tissue 1.14E-01 -4.64E-01 -1.75E+00
Glioblastopma 2A00.00 Nervous tissue 2.48E-102 -7.70E-01 -2.12E+00
Glioma 2A00.0Y-2A00.0Z White matter tissue 5.41E-03 -5.45E-01 -1.54E+00
Head and neck cancer 2D42 Head and neck tissue 6.40E-01 -2.60E-02 -9.78E-02
HIV-associated neurocognitive impairment 8A2Y-8A2Z White matter tissue 9.72E-01 -2.12E-03 -7.04E-03
Huntington's disease 8A01.10 Whole blood 1.12E-01 1.09E-01 5.32E-01
Idiopathic pulmonary fibrosis CB03.4 Lung tissue 1.70E-01 -1.45E-01 -2.14E-01
Immunodeficiency 4A00-4A20 Peripheral blood 1.21E-01 7.06E-02 6.03E-01
Influenza 1.00E+30 Whole blood 1.29E-01 1.27E-01 6.93E-01
Interstitial cystitis GC00.3 Bladder tissue 5.95E-01 -3.47E-02 -5.96E-01
Intracranial aneurysm 8B01.0 Intracranial artery 5.18E-02 -2.00E-01 -8.38E-01
Irritable bowel syndrome DD91.0 Rectal colon tissue 6.15E-01 -3.48E-02 -1.88E-01
Ischemic stroke 8B11 Peripheral blood 7.69E-03 1.17E-01 1.05E+00
Juvenile idiopathic arthritis FA24 Peripheral blood 1.79E-01 5.99E-02 1.64E-01
Lateral sclerosis 8B60.4 Cervical spinal cord 1.36E-01 2.65E-01 7.05E-01
Lateral sclerosis 8B60.4 Skin 5.29E-01 1.38E-01 5.81E-01
Liver cancer 2C12.0 Liver tissue 7.50E-02 -1.83E-01 -5.53E-01
Liver failure DB99.7-DB99.8 Liver tissue 1.14E-01 7.08E-02 5.22E-01
Lung cancer 2C25 Lung tissue 1.86E-01 -1.06E-01 -3.87E-01
Lupus erythematosus 4A40 Whole blood 2.28E-01 -5.85E-02 -1.47E-01
Major depressive disorder 6A70-6A7Z Whole blood 6.84E-01 2.87E-02 1.15E-01
Major depressive disorder 6A70-6A7Z Hippocampus 4.11E-01 -1.59E-02 -1.32E-01
Melanoma 2C30 Skin 1.36E-02 -1.93E-01 -4.57E-01
Multiple myeloma 2A83.1 Bone marrow 2.80E-04 -4.61E-01 -2.58E+00
Multiple myeloma 2A83.1 Peripheral blood 4.13E-01 -1.54E-02 -5.93E-02
Multiple sclerosis 8A40 Plasmacytoid dendritic cells 7.63E-01 4.63E-02 1.67E-01
Myelodysplastic syndrome 2A36-2A3Z Bone marrow 3.08E-01 -2.09E-02 -8.70E-02
Myelofibrosis 2A20.2 Whole blood 6.63E-01 -6.36E-02 -4.69E-01
Myocardial infarction BA41-BA50 Peripheral blood 4.59E-03 1.45E-01 4.50E-01
Myopathy 8C70.6 Muscle tissue 1.31E-01 -1.12E-01 -6.72E-01
Neonatal sepsis KA60 Whole blood 1.46E-04 -1.48E-01 -5.46E-01
Neuroectodermal tumour 2A00.11 Brain stem tissue 3.61E-05 -5.26E-01 -2.70E+00
Non-alcoholic fatty liver disease DB92 Liver tissue 4.51E-01 -7.82E-02 -4.02E-01
Obesity related type 2 diabetes 5A11 Omental adipose tissue 4.83E-01 5.37E-03 3.15E-02
Olive pollen allergy CA08.00 Peripheral blood 5.93E-02 2.05E-01 1.17E+00
Oral cancer 2B6E Oral tissue 1.01E-11 -6.34E-01 -2.52E+00
Osteoarthritis FA00-FA0Z Synovial tissue 7.54E-01 2.37E-02 9.72E-02
Osteoporosis FB83.1 Bone marrow 2.98E-03 3.82E-01 2.58E+00
Ovarian cancer 2C73 Ovarian tissue 7.18E-01 -1.00E-02 -2.73E-02
Pancreatic cancer 2C10 Pancreas 4.46E-01 -1.83E-01 -1.97E-01
Parkinson's disease 8A00.0 Substantia nigra tissue 5.96E-02 -1.31E-01 -5.19E-01
Pediatric respiratory syncytial virus infection CA40.11 Peripheral blood 3.43E-02 -1.12E-01 -9.21E-01
Pituitary cancer 2D12 Pituitary tissue 5.37E-06 -6.45E-01 -1.87E+00
Pituitary gonadotrope tumour 2D12 Pituitary tissue 2.84E-05 -7.61E-01 -2.36E+00
Polycystic ovary syndrome 5A80.1 Vastus lateralis muscle 8.03E-01 2.43E-02 8.73E-02
Polycythemia vera 2A20.4 Whole blood 3.54E-01 1.45E-02 1.00E-01
Pompe disease 5C51.3 Biceps muscle 1.77E-02 5.55E-01 3.99E+00
Preterm birth KA21.4Z Myometrium 6.54E-01 2.63E-02 3.72E-01
Prostate cancer 2C82 Prostate 2.46E-01 9.26E-03 3.07E-02
Psoriasis EA90 Skin 6.68E-03 -1.26E-01 -3.85E-01
Rectal cancer 2B92 Rectal colon tissue 2.16E-03 -3.17E-01 -2.25E+00
Renal cancer 2C90-2C91 Kidney 3.89E-01 -1.87E-01 -6.28E-01
Retinoblastoma 2D02.2 Uvea 5.68E-11 -1.07E+00 -4.52E+00
Rheumatoid arthritis FA20 Synovial tissue 3.56E-01 1.20E-01 3.90E-01
Rhinovirus infection CA42.1 Nasal epithelium tissue 5.60E-01 4.66E-02 3.66E-01
Schizophrenia 6A20 Prefrontal cortex 1.96E-01 -1.94E-02 -2.94E-02
Schizophrenia 6A20 Superior temporal cortex 4.09E-01 -1.74E-02 -1.88E-01
Scleroderma 4A42.Z Whole blood 6.60E-02 8.01E-02 7.05E-01
Seizure 8A60-8A6Z Whole blood 6.86E-01 1.92E-02 1.26E-01
Sensitive skin EK0Z Skin 7.43E-01 -3.27E-02 -2.04E-01
Sepsis with septic shock 1G41 Whole blood 1.00E-01 1.94E-02 7.36E-02
Shwachman-Diamond syndrome 3A70.0 Bone marrow 3.48E-02 3.08E-01 1.18E+00
Sickle cell disease 3A51.0-3A51.3 Peripheral blood 1.65E-01 9.94E-02 5.39E-01
Simpson golabi behmel syndrome LD2C Adipose tissue 3.13E-01 -1.10E-01 -1.49E+00
Sjogren's syndrome 4A43.2 Salivary gland tissue 1.79E-01 -2.11E-01 -7.72E-01
Skin cancer 2C30-2C3Z Skin 1.13E-11 -2.38E-01 -6.36E-01
Thrombocythemia 3B63 Whole blood 9.16E-01 -4.93E-02 -3.72E-01
Thrombocytopenia 3B64 Whole blood 7.74E-01 -1.60E-02 -5.73E-02
Thyroid cancer 2D10 Thyroid 1.44E-03 -1.73E-01 -4.34E-01
Tibial muscular dystrophy 8C75 Muscle tissue 5.43E-06 -3.64E-01 -2.66E+00
Tuberous sclerosis complex LD2D.2 Perituberal tissue 2.74E-01 -9.58E-03 -1.73E-01
Type 2 diabetes 5A11 Liver tissue 5.25E-01 1.22E-04 5.80E-04
Ureter cancer 2C92 Urothelium 1.99E-01 1.19E-02 8.22E-02
Uterine cancer 2C78 Endometrium tissue 3.32E-17 -4.80E-01 -7.16E-01
Vitiligo ED63.0 Skin 4.47E-04 -3.42E-01 -2.84E+00
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⏷ Show the Full List of Expression Under 107 Diseases

The Drug Therapeutic Target (DTT) Role of This DTP

DTP DTT Name ATP-binding cassette transporter C8 (ABCC8) DTT Info
DTP DTT Type Successful
6 Approved Drug(s) Targeting This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Acetohexamide DMR6N7H Diabetic complication 5A2Y Approved [1]
Glibenclamide DM8JXPZ Diabetic complication 5A2Y Approved [2]
Gliclazide DMN6QO5 Diabetic complication 5A2Y Approved [3]
Glimepiride DM5FSJA Diabetic complication 5A2Y Approved [4]
Repaglinide DM5SXUV Diabetic complication 5A2Y Approved [5]
Tolbutamide DM02AWV Advanced cancer 2A00-2F9Z Approved [6]
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⏷ Show the Full List of 6 Approved Drug(s)
1 Clinical Trial Drug(s) Targeting This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
NN-414 DMRJEXM Type-1 diabetes 5A10 Phase 1 [7]
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2 Investigative Drug(s) Targeting This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
HBR-985 DMKDBFL Discovery agent N.A. Investigative [8]
NS-11757 DM98VMZ Atrial fibrillation BC81.3 Investigative [9]
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References

1 Diabetes and insulin secretion: the ATP-sensitive K+ channel (K ATP) connection.Diabetes.2005 Nov;54(11):3065-72.
2 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
3 Structural basis for the interference between nicorandil and sulfonylurea action. Diabetes. 2001 Oct;50(10):2253-9.
4 Mechanism of disopyramide-induced hypoglycaemia in a patient with Type 2 diabetes. Diabet Med. 2009 Jan;26(1):76-8.
5 Metformin/Repaglinide (PrandiMet) for type 2 diabetes. Med Lett Drugs Ther. 2009 Jun 1;51(1313):41-3.
6 Expression of an activating mutation in the gene encoding the KATP channel subunit Kir6.2 in mouse pancreatic beta cells recapitulates neonatal diabetes. J Clin Invest. 2009 Jan;119(1):80-90.
7 Attenuation of hyperinsulinemia by NN414, a SUR1/Kir6.2 selective K-adenosine triphosphate channel opener, improves glucose tolerance and lipid profile in obese Zucker rats.Metabolism.2004 Apr;53(4):441-7.
8 Cardioselective K(ATP) channel blockers derived from a new series of m-anisamidoethylbenzenesulfonylthioureas. J Med Chem. 2001 Mar 29;44(7):1085-98.
9 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2944).
10 ABCC8 and ABCC9: ABC transporters that regulate K+ channels. Pflugers Arch. 2007 Feb;453(5):703-18.