Download TRANSPORTERS AS TARGETS

TRANSPORTERS AS TARGETS
OPTI-TARGET™: ASSAYS FOR TRANSPORTERS AS THERAPEUTIC, TOXICITY, AND DELIVERY TARGETS
Transporter Physiological role
Gene
Major tissue distribution
ASBT
Bile acid uptake
SLC10A2
Ileum, kidney, biliary tract (apical)
asc-1
Amino acid transport
SLC7A10
Brain, heart, placenta, skeletal muscle and kidney
SLC1A5
Lung, skeletal muscle, large intestine, kidney, testis, adipose
tissue, tumor cells
ASCT2
Amino acid transport
Examples of interacting xenobiotics
Available
species
Elobixia, LUM001, SHP626, A4250
Human
BMS-466442
Human
Cancer
GPNA, ketamine
Human
Troglitazone, rifampicin, benzbromarone, bosentan,
cyclosporine A
Human, rat,
dog
Related disease/ADR
Hypertriglycerimaemia, constipation,
cholestatic liver diseases, nash, primary bile
acid malabsorption
Learning and memory impairment,
schizophrenia
BSEP
Bile acid efflux
ABCB11
Liver
PFIC II, drug induced cholestasis and
hepatitis
CNT1
Nucleoside uptake
SLC28A1
Liver, kidney, small intestine, tumor cells
Cancer
Gemcitabine, cytarabine, azacitidine, zalcitabine,
floxuridine
Human, rat
Cancer
Ribavirin, cladribine, didanosine, fludarabine, clofarabine,
floxuridine, acacitidine, cladribine
Human, rat
Cancer
Gemcitabine, azacitidine, mercaptopurine, fludarabine,
clofarabine, cladribine, floxuridine
Human, rat
Altropane, vanoexerine, difluoropine, iometopane, DBL583, GBR-12783, RTI-229, 11C-PE2I
Human
Riluzole, l-trans-PDC, HIP-A, MPDC,TFB-TBOA, UCPH101
Human
Dihydrokainic acid, SYM-2081, WAY-213613,l-trans-PDC
Human
CNT2
Nucleoside uptake
SLC28A2
CNT3
Nucleoside uptake
SLC28A3
Kidney (apical membrane), liver, heart, brain, placenta, pancreas,
skeletal muscle, colon, rectum, small intestine, lymphocytes,
tumor cells
Pancreas, trachea, bone marrow, and mammary gland, intestine,
brain, heart, prostrate, liver, tumor cells
Parkinson disease, tourette syndrome, ADHD,
addiction, major affective disorders
Alzheimer's disease, huntington's
disease, epilepsy, cerebellar ataxia type 7,
schizophrenia, excitotoxicity
Amyotrophic lateral sclerosis, alzheimer's
disease, huntington's disease, epilepsy,
ischemia, schizophrenia, excitotoxicity
DAT
Neurotransmission
SLC6A3
Brain (dopaminergic neurons), gut
EAAT1
Neurotransmission
SLC1A3
Brain (astrocytes, bergmann glia), heart, skeletal muscle, placenta
EAAT2
Neurotransmission
SLC1A2
Brain (astrocytes, bergmann glia, neurons), liver, pancreas
ENT1
Nucleoside transport
SLC29A1
Heart, brain, mammary gland, erythrocytes and placenta, tumor
cells
Cancer
Gemcitabine, 5-FU, zalcitabine, cytarabine,
Human
fludarabine,cladribine, azacitidine, pentostatin, decitabine
ENT2
Nucleoside transport
SLC29A2
Skeletal muscle, liver, lung, placenta, brain, heart, kidney, ovarian
tissues
Cancer
Zidovudine, zalcitabine, cytarabine, fludarabine, 5-FU,
azacitidine, pentostatin, decitabine, cladribine
Human, rat
ENT4/PMAT
Nucleoside transport
and extrasynaptic
reuptake
SLC29A4
Heart, brain, skeletal muscle
Depression, schizophrenia, bipolar disorder
Trazodone, decynium-22
Human
GAT1
Neurotransmission
SLC6A1
Central and peripheral neurons (GABAergic neurons)
Epilepsy, schizophrenia, ADHD
Tiagabine, nipecotic acid, deramciclane, hyperforin,
riluzole, SKF-89976A, NNC-711, SNAP-5114, CI-966
Human
Epilepsy
Tiagabine, β-Alanine, nipecotic acid, riluzole, NNC052090, SKF 89976A
Human
Epilepsy
Tiagabine, β-Alanine, nipecotic acid, riluzole, SKF
89976A
Human
Schizophrenia
Bitopertin, PF-04958242
Human
Depression, orthostatic intolerance, anorexia
nervosa, cardiovascular disorders, ADHD
Atomoxetine, reboxetine, desipramine,edivoxetine,
viloxazine, maprotiline, nisoxetine, 123I-MIBG, 11C-HED
Human
GAT2
GAT3
Neurotransmission
Neurotransmission
SLC6A13
SLC6A11
GLYT1
Neurotransmission
SLC6A9
NET
Neurotransmission
SLC6A2
OATP1B1
OATP1B3
Hepatic uptake of
bilirubin and a variety
of anionic drugs
Hepatic uptake of
bilirubin and a variety
of anionic drugs
Statin-induced myopathy, hyperbilirubinemia,
rotor syndrome
Cyclosporine A, rifampicin, gemfibrozil, ritonavir/lopinavir
Human
SLCO1B3
Liver (hepatocytes)
Unconjugated hyperbilirubinemia, rotor
syndrome
Cyclosporine A, rifampicin, ritonavir/lopinavir
Human
Cytotoxicity of cisplatin, oxaliplatin and
picoplatin
Cisplatin, oxaliplatin, picoplatin
Human, rat
Prostate cancer, coronary heart disease,
obsessive compulsive disorder, depression
Oxaliplatin, picoplatin, tetrabenazine, trazodone
Human, rat
Rheumatoid arthritis, crohn's disease
Verapamil, quinidine, propafenone, clofilum
Human
Primary systemic carnitine deficiency,
crohn's disease
Verapamil, quinidine, valproate, cephaloridine, pyrilamine
Human
Hereditary folate malabsorption, cancer
Methotrxate, pemetrexed, bromosulfophthalein
Human
Human
OCT3
Cation uptake;
SLC22A3
extrasynaptic reuptake
OCTN1
Ergothioneine uptake
SLC22A4
OCTN2
Carnitine uptake
SLC22A5
PEPT1
Peptide uptake
Brain, retina, liver, spleen, kidney, pancreas, uterus, stomach,
lung, placenta, intestine
Brain (non adrenergic neuronal somata, axons, dendrites),
peripheral nervous system, adrenal gland (chromaffin cells),
placenta
Liver (hepatocytes)
Cation uptake
Vitamin transport
Brain (gabaergic neurons)
SLCO1B1
OCT2
PCFT
Brain (meninges, ependyma, choroid plexus), retina, liver, kidney
SLC22A2
SLC46A1
Kidney, small intestine, lung, placenta, thymus, brain (neurons,
blood-brain barrier), inner ear
Heart, skeletal muscle, brain (neurons, glial cells, plexus
choroideus), small intestine, liver, lung, kidney, urinary bladder,
mammary gland, skin blood vessels
Kidney, intestine, spleen, heart, skeletal muscle, brain, mammary
gland, thymus, prostate, airways, testis, eye, fetal liver, sperm,
immune cells
Skeletal muscle, kidney, prostate, lung, pancreas, heart, small
intestine, adrenal gland, thyroid gland, liver, etc.
Small intestine, choroid plexus, kidney (proximal tubule), liver
(sinusoidal), placenta
SLC15A1
Small intestine, kidney, pancreas, bile duct, liver
Inflammatory bowel disease
Glycylsarcosine, bestatin, y-ALA, cephalexin, valacyclovir,
cyclacillin, losartan
Lead exposure
Cefaclor, glycylsarcosine, bestatin, cephalexin,
valacyclovir, losartan
Human
Methotrxate, pemetrexed, tomudex,
edatrexate, bromosulfophthalein
Human
PEPT2
Peptide uptake
SLC15A2
Apical surface of epithelial cells from kidney and choroid plexus;
neurons, astrocytes (neonates), lung, mammary gland, spleen,
enteric nervous system
RFC
Vitamin transport
SLC19A1
Ubiquitous
Cancer
SERT
Neurotransmission
SCL6A4
Brain, peripheral nervous system, placenta, epithelium cells,
platelets
Anxiety, depression, autism gastrointestinal
disorders, premature ejaculation, obesity,
schizophrenia OCD
SGLT2
Glucose transport
SLC5A2
Kidney, brain, liver, heart muscle, thyroid, salivary glands
Type ii diabetes, familial renal glucosuria
SNAT1
Amino acid transport
SLC38A1
Brain, retina, heart, placenta, adrenal gland
Suicidal behavior, cancer
MeAIB
Human
SNAT2
Amino acid transport
SLC38A2
Ubiquitous
Schizophrenia, cancer
MeAIB
Human
Ubiquitous
Thiamine-responsive megaloblastic anemia
syndrome
Fedratinib, amprolium, pyrithiamine, oxythiamine
Human
Fedratinib, amprolium, pyrithiamine, oxythiamine
Human
THTR1
Vitamin transport
SLC19A2
Sertraline, fluvoxamine, fluoxetine, citalopram,
zimelidine, dapoxetine, paroxetine, escitalopram,
123I-ADAM
Canagliflozin, dapagliflozin, empagliflozin, tofogliflozin,
ipragliflizin, remogliflozin, sotagliflozin, ertugliflozin
Human
Human
THTR2
Vitamin transport
SLC19A3
Ubiquitous
Biotin-responsive basal ganglia disease,
wernicke's encephalopathy
URAT1
Uric acid reneal
tubular reabsorption
SLC22A12
Kidney
Renal hypo-uricemia, gout
Lesinurad, RDEA3170, KUX-1151, benzbromarone
Human
xCT
Amino acid transport
SLC7A11
and neurotransmission
Macrophages, brain, retinal pigment cells, liver, kidney, tumor
cells
Cancer, epilepsy, neurodegenerative diseases
Sulfasalazine, erastin, BAY-94-9392, BMAA
Human
Transporter Services and Solutions for DDI, DMPK,
Safety, Pharmacology, and Beyond
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