General Information of Drug Transporter (DTP) (ID: DT9G7XN)

DTP Name Peptide transporter 1 (SLC15A1)
Gene Name SLC15A1
UniProt ID
P46059 (S15A1_HUMAN)
VARIDT ID
DTD0021
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Synonyms HPECT1; HPEPT1; Intestinal H(+)/peptide cotransporter; Oligopeptide transporter, small intestine isoform; PEPT1; SLC15A1; Solute carrier family 15 member 1
DTP Family Proton-Dependent Oligopeptide Transporter (POT/PTR) Family ;
Sequence
MGMSKSHSFFGYPLSIFFIVVNEFCERFSYYGMRAILILYFTNFISWDDNLSTAIYHTFV
ALCYLTPILGALIADSWLGKFKTIVSLSIVYTIGQAVTSVSSINDLTDHNHDGTPDSLPV
HVVLSLIGLALIALGTGGIKPCVSAFGGDQFEEGQEKQRNRFFSIFYLAINAGSLLSTII
TPMLRVQQCGIHSKQACYPLAFGVPAALMAVALIVFVLGSGMYKKFKPQGNIMGKVAKCI
GFAIKNRFRHRSKAFPKREHWLDWAKEKYDERLISQIKMVTRVMFLYIPLPMFWALFDQQ
GSRWTLQATTMSGKIGALEIQPDQMQTVNAILIVIMVPIFDAVLYPLIAKCGFNFTSLKK
MAVGMVLASMAFVVAAIVQVEIDKTLPVFPKGNEVQIKVLNIGNNTMNISLPGEMVTLGP
MSQTNAFMTFDVNKLTRINISSPGSPVTAVTDDFKQGQRHTLLVWAPNHYQVVKDGLNQK
PEKGENGIRFVNTFNELITITMSGKVYANISSYNASTYQFFPSGIKGFTISSTEIPPQCQ
PNFNTFYLEFGSAYTYIVQRKNDSCPEVKVFEDISANTVNMALQIPQYFLLTCGEVVFSV
TGLEFSYSQAPSNMKSVLQAGWLLTVAVGNIIVLIVAGAGQFSKQWAEYILFAALLLVVC
VIFAIMARFYTYINPAEIEAQFDEDEKKNRLEKSNPYFMSGANSQKQM
Function This tranporter mediates intake of oligopeptides of 2 to 4 amino acids with a preference for dipeptides and may constitute a major route for the absorption of protein digestion end-products.
Endogenous Substrate(s) H+
TCDB ID
2.A.17.4.9
Gene ID
6564
KEGG Pathway
Protein digestion and absorption (hsa04974 )
Reactome Pathway
Proton/oligopeptide cotransporters (R-HSA-427975 )

Molecular Interaction Atlas (MIA) of This DTP

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DTP
52 Approved Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Aminolevulinic acid hci DMS4BLQ Acne vulgaris ED80 Approved [4]
Amoxicillin DMUYNEI Acute otitis media AB00 Approved [5]
Ampicillin DMHWE7P Acute epiglottitis Approved [6]
Benazepril DMH1M9B Hypertension BA00-BA04 Approved [7]
Bestatin DM8L9D4 Acute myeloid leukaemia 2A60 Approved [8]
Captopril DM458UM Chronic heart failure BD1Z Approved [9]
Cefaclor DMJXDGC Bacterial infection 1A00-1C4Z Approved [10]
Cefadroxil DMMC345 Bacterial infection 1A00-1C4Z Approved [11]
Cefamandole DMNEXZF Bacteremia 1A73 Approved [12]
Cefazolin DMPDYFR Bacteremia 1A73 Approved [13]
Cefdinir DMJ7A0H Bacterial infection 1A00-1C4Z Approved [14]
Cefixime DMY60I8 Acute gonococcal cervicitis Approved [15]
Cefmetazole DM42W1B Bacterial infection 1A00-1C4Z Approved [12]
Cefoxitin DMY8NC4 Acute gonococcal cervicitis Approved [13]
Cefpodoxime DMJUNY5 Acute gonococcal cervicitis Approved [13]
Cefradine DMUNSWV Acute otitis media AB00 Approved [16]
Cefsulodin DMQXLF3 Pseudomonas infection 1B92 Approved [12]
Ceftibuten DMWV2AG Acute otitis media AB00 Approved [17]
Ceftriaxone DMCEW64 Acute gonococcal cervicitis Approved [12]
Cefuroxime axetil DM4CHN0 N. A. N. A. Approved [12]
Cephalexin DMD5JU8 Acute otitis media AB00 Approved [18]
Cephaloglycin DMYZITL Bacterial infection 1A00-1C4Z Approved [19]
Cyclacillin DMHSJB4 Bacterial infection 1A00-1C4Z Approved [20]
Dexamethasone DMMWZET Acute adrenal insufficiency Approved [21]
Dicloxacillin DM8EU0Z Bacterial infection 1A00-1C4Z Approved [20]
Enalapril DMNFUZR Congestive heart failure BD10 Approved [22]
Enalaprilat DMFYAM1 Congestive heart failure BD10 Approved [23]
Eprosartan DM07K2I Hypertension BA00-BA04 Approved [11]
Flucloxacillin DMNUWST Bacterial infection 1A00-1C4Z Approved [13]
Fosinopril DM9NJ52 Chronic heart failure BD1Z Approved [7]
Furosemide DMMQ8ZG Congestive heart failure BD10 Approved [21]
Irbesartan DMTP1DC Diabetic kidney disease GB61.Z Approved [11]
Lisdexamfetamine DM6W8V5 Attention deficit hyperactivity disorder 6A05.Z Approved [24]
Lisinopril DMUOK4C Chronic heart failure BD1Z Approved [21]
Losartan DM72JXH Diabetic kidney disease GB61.Z Approved [11]
Metoprolol DMOJ0V6 Acute coronary syndrome BA41 Approved [21]
Midodrine DME2PY5 Orthostatic hypotension BA21 Approved [20]
Moexipril DM26E4B Hypertension BA00-BA04 Approved [7]
Oseltamivir DMGO72P Influenza 1E30-1E32 Approved [25]
Perindopril DMOPZDT Hypertension BA00-BA04 Approved [7]
Piperacillin DMTBKF3 Acute gonococcal cervicitis Approved [13]
Ramipril DM2R68E Acute heart failure BD10-BD13 Approved [7]
Ribavirin DMEYLH9 Hepatitis C virus infection 1E51.1 Approved [26]
Spirapril DM5XLTY Hypertension BA00-BA04 Approved [7]
Sulfasalazine DMICA9H Irritable bowel syndrome DD91.0 Approved [21]
Sulpiride DMF54ZG Schizophrenia 6A20 Approved [27]
Temocapril DM1A79H N. A. N. A. Approved [28]
Temocaprilate DMNX2QI N. A. N. A. Approved [23]
Trandolapril DM4L6EU Chronic heart failure BD1Z Approved [7]
Valaciclovir DMHKS94 Genital herpes 1A94 Approved [29]
Valganciclovir DMS2IUH Virus infection 1A24-1D9Z Approved [30]
Valsartan DMREUQ6 Chronic heart failure BD1Z Approved [11]
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⏷ Show the Full List of 52 Approved Drug(s)
1 Clinical Trial Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Benzylpenicillin DMS9503 Actinomycosis Phase 3 [31]
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2 Discontinued Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cephaloridine DM4Y95F Gram-positive bacterial infection 1B74-1G40 Withdrawn from market [12]
Ceronapril DMFBNI6 Major depressive disorder 6A70.3 Discontinued in Phase 2 [19]
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2 Preclinical Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Metampicillin DMQW5MH N. A. N. A. Preclinical [20]
QSP DMASVOD N. A. N. A. Preclinical [32]
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2 Investigative Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
carnosine DMFYCB4 Discovery agent N.A. Investigative [33]
NAAG DMFGOW0 Discovery agent N.A. Investigative [34]
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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 7.54E-01 -1.25E-02 -8.78E-02
Adrenocortical carcinoma 2D11.Z Kidney 9.62E-01 1.33E-02 9.34E-02
Alopecia ED70 Skin from scalp 6.41E-03 -1.19E-01 -3.25E-01
Alzheimer's disease 8A20 Entorhinal cortex 4.57E-01 2.15E-02 1.72E-01
Ankylosing spondylitis FA92.0 Pheripheral blood 4.91E-01 -4.60E-02 -4.22E-01
Aortic stenosis BB70 Calcified aortic valve 7.50E-01 8.49E-02 1.64E-01
Apnea 7A40 Hyperplastic tonsil 7.98E-03 -4.79E-01 -1.92E+00
Arthropathy FA00-FA5Z Peripheral blood 5.85E-01 5.23E-03 5.13E-02
Asthma CA23 Nasal and bronchial airway 3.70E-03 3.25E-01 6.33E-01
Atopic dermatitis EA80 Skin 1.01E-02 -1.27E-01 -5.15E-01
Autism 6A02 Whole blood 1.71E-01 -6.13E-02 -2.67E-01
Autoimmune uveitis 9A96 Peripheral monocyte 2.65E-01 2.48E-01 9.96E-01
Autosomal dominant monocytopenia 4B04 Whole blood 7.66E-01 7.58E-02 5.54E-01
Bacterial infection of gingival 1C1H Gingival tissue 2.55E-10 -3.14E-01 -8.42E-01
Batten disease 5C56.1 Whole blood 6.05E-01 -7.58E-03 -7.96E-02
Behcet's disease 4A62 Peripheral blood 4.94E-01 8.49E-02 6.54E-01
Bipolar disorder 6A60-6A6Z Prefrontal cortex 5.18E-01 -3.24E-02 -2.35E-01
Bladder cancer 2C94 Bladder tissue 1.43E-04 6.43E-01 2.61E+00
Breast cancer 2C60-2C6Z Breast tissue 6.30E-01 -4.57E-02 -1.74E-01
Cardioembolic stroke 8B11.20 Whole blood 1.45E-03 -1.88E-01 -7.59E-01
Cervical cancer 2C77 Cervical tissue 2.84E-04 -7.15E-01 -1.37E+00
Childhood onset rheumatic disease FA20.Z Peripheral blood 4.31E-02 9.52E-02 6.09E-01
Chronic hepatitis C 1E51.1 Whole blood 4.46E-01 1.91E-02 1.16E-01
Chronic obstructive pulmonary disease CA22 Lung tissue 8.28E-01 2.72E-02 1.72E-01
Chronic obstructive pulmonary disease CA22 Small airway epithelium 9.20E-01 2.66E-02 1.51E-01
Chronic rhinosinusitis CA0A Sinus mucosa tissue 2.96E-01 3.29E-02 3.09E-01
Colon cancer 2B90 Colon tissue 2.26E-13 -3.30E-01 -6.83E-01
Coronary artery disease BA80-BA8Z Peripheral blood 1.72E-02 -1.88E-01 -2.37E+00
Diffuse large B-cell lymphoma 2A81 Tonsil tissue 4.26E-01 -7.99E-02 -5.90E-01
Endometriosis GA10 Endometrium tissue 1.60E-03 4.78E-02 8.61E-02
Familial hypercholesterolemia 5C80.00 Peripheral blood 8.40E-01 9.36E-03 8.70E-02
Familial hypercholesterolemia 5C80.00 Whole blood 2.06E-08 -2.55E-01 -1.20E+00
Gastric cancer 2B72 Gastric tissue 4.43E-01 -9.42E-02 -4.71E-01
Glioblastopma 2A00.00 Nervous tissue 7.91E-20 -1.08E-01 -4.95E-01
Glioma 2A00.0Y-2A00.0Z White matter tissue 3.18E-02 -2.81E-01 -5.64E-01
Head and neck cancer 2D42 Head and neck tissue 2.94E-07 1.87E-01 6.51E-01
HIV-associated neurocognitive impairment 8A2Y-8A2Z White matter tissue 6.42E-01 -1.94E-02 -1.21E-01
Huntington's disease 8A01.10 Whole blood 1.34E-01 -8.16E-02 -5.38E-01
Idiopathic pulmonary fibrosis CB03.4 Lung tissue 8.20E-01 -2.45E-02 -1.48E-01
Immunodeficiency 4A00-4A20 Peripheral blood 1.71E-01 -5.24E-02 -7.18E-01
Influenza 1.00E+30 Whole blood 1.57E-03 4.03E-01 5.12E+00
Interstitial cystitis GC00.3 Bladder tissue 9.85E-02 9.09E-02 2.10E+00
Intracranial aneurysm 8B01.0 Intracranial artery 4.95E-01 7.97E-02 3.40E-01
Irritable bowel syndrome DD91.0 Rectal colon tissue 5.95E-01 -4.54E-02 -8.40E-02
Ischemic stroke 8B11 Peripheral blood 6.82E-01 3.14E-02 1.95E-01
Juvenile idiopathic arthritis FA24 Peripheral blood 5.61E-01 9.60E-03 5.00E-02
Lateral sclerosis 8B60.4 Cervical spinal cord 6.49E-01 -9.41E-02 -3.92E-01
Lateral sclerosis 8B60.4 Skin 5.01E-01 1.44E-02 1.27E-01
Liver cancer 2C12.0 Liver tissue 5.86E-03 -1.33E-01 -3.55E-01
Liver failure DB99.7-DB99.8 Liver tissue 5.97E-03 -3.24E-01 -4.09E+00
Lung cancer 2C25 Lung tissue 3.38E-39 1.68E-01 1.05E+00
Lupus erythematosus 4A40 Whole blood 5.97E-05 7.35E-02 2.41E-01
Major depressive disorder 6A70-6A7Z Whole blood 8.98E-01 7.59E-03 3.18E-02
Major depressive disorder 6A70-6A7Z Hippocampus 6.91E-01 8.30E-03 7.24E-02
Melanoma 2C30 Skin 3.63E-04 -1.57E+00 -1.20E+00
Multiple myeloma 2A83.1 Bone marrow 7.60E-03 -2.12E-01 -1.22E+00
Multiple myeloma 2A83.1 Peripheral blood 2.32E-01 4.19E-02 3.72E-01
Multiple sclerosis 8A40 Plasmacytoid dendritic cells 3.21E-01 -1.66E-01 -8.74E-01
Myelodysplastic syndrome 2A36-2A3Z Bone marrow 1.77E-01 7.03E-03 8.68E-02
Myelofibrosis 2A20.2 Whole blood 8.39E-01 6.47E-03 7.08E-02
Myocardial infarction BA41-BA50 Peripheral blood 4.40E-01 1.28E-01 1.52E-01
Myopathy 8C70.6 Muscle tissue 9.01E-02 -9.48E-02 -8.24E-01
Neonatal sepsis KA60 Whole blood 2.21E-02 4.49E-02 2.53E-01
Neuroectodermal tumour 2A00.11 Brain stem tissue 6.33E-02 -2.95E-01 -9.56E-01
Non-alcoholic fatty liver disease DB92 Liver tissue 5.29E-01 1.26E-02 4.98E-02
Obesity related type 2 diabetes 5A11 Omental adipose tissue 2.60E-01 -7.43E-02 -1.15E+00
Olive pollen allergy CA08.00 Peripheral blood 5.91E-01 1.93E-01 7.08E-01
Oral cancer 2B6E Oral tissue 7.13E-01 -1.44E-01 -5.69E-01
Osteoarthritis FA00-FA0Z Synovial tissue 2.44E-01 -5.55E-01 -1.29E+00
Osteoporosis FB83.1 Bone marrow 1.92E-02 3.03E-01 3.20E+00
Ovarian cancer 2C73 Ovarian tissue 1.94E-01 1.56E-04 6.10E-04
Pancreatic cancer 2C10 Pancreas 2.33E-02 -4.57E-01 -8.68E-01
Parkinson's disease 8A00.0 Substantia nigra tissue 1.74E-01 -8.96E-02 -5.59E-01
Pediatric respiratory syncytial virus infection CA40.11 Peripheral blood 3.64E-01 -6.25E-02 -4.95E-01
Pituitary cancer 2D12 Pituitary tissue 8.20E-02 1.96E-01 9.40E-01
Pituitary gonadotrope tumour 2D12 Pituitary tissue 3.49E-01 1.64E-01 7.68E-01
Polycystic ovary syndrome 5A80.1 Vastus lateralis muscle 8.18E-01 -5.00E-02 -5.59E-01
Polycythemia vera 2A20.4 Whole blood 4.82E-03 7.08E-02 6.37E-01
Pompe disease 5C51.3 Biceps muscle 8.69E-02 -7.68E-02 -1.03E+00
Preterm birth KA21.4Z Myometrium 4.60E-01 -7.84E-02 -2.96E-01
Prostate cancer 2C82 Prostate 1.31E-04 5.67E-01 1.00E+00
Psoriasis EA90 Skin 4.78E-28 6.76E-01 1.50E+00
Rectal cancer 2B92 Rectal colon tissue 6.98E-02 -5.31E-01 -1.46E+00
Renal cancer 2C90-2C91 Kidney 2.56E-01 -3.85E-01 -9.21E-01
Retinoblastoma 2D02.2 Uvea 8.27E-01 9.03E-03 8.47E-02
Rheumatoid arthritis FA20 Synovial tissue 4.41E-04 -7.89E-01 -2.51E+00
Rhinovirus infection CA42.1 Nasal epithelium tissue 3.82E-01 -2.23E-02 -1.99E-01
Schizophrenia 6A20 Prefrontal cortex 2.28E-01 -5.07E-02 -2.49E-01
Schizophrenia 6A20 Superior temporal cortex 9.68E-01 5.37E-02 5.24E-01
Scleroderma 4A42.Z Whole blood 1.67E-05 2.89E-01 2.55E+00
Seizure 8A60-8A6Z Whole blood 4.59E-01 -5.37E-02 -3.81E-01
Sensitive skin EK0Z Skin 8.33E-01 -4.90E-02 -4.03E-01
Sepsis with septic shock 1G41 Whole blood 2.36E-05 3.31E-02 1.64E-01
Shwachman-Diamond syndrome 3A70.0 Bone marrow 3.09E-01 2.24E-01 1.28E+00
Sickle cell disease 3A51.0-3A51.3 Peripheral blood 4.58E-01 -1.87E-02 -1.30E-01
Simpson golabi behmel syndrome LD2C Adipose tissue 6.78E-01 4.53E-02 3.86E-01
Sjogren's syndrome 4A43.2 Salivary gland tissue 4.21E-01 -1.77E-01 -1.30E+00
Skin cancer 2C30-2C3Z Skin 1.12E-25 -1.01E+00 -1.49E+00
Thrombocythemia 3B63 Whole blood 3.49E-01 4.47E-03 4.96E-02
Thrombocytopenia 3B64 Whole blood 6.44E-01 4.48E-02 1.51E-01
Thyroid cancer 2D10 Thyroid 4.52E-03 5.05E-02 2.20E-01
Tibial muscular dystrophy 8C75 Muscle tissue 1.45E-04 -1.96E-01 -1.71E+00
Tuberous sclerosis complex LD2D.2 Perituberal tissue 1.42E-01 1.17E-01 6.61E-01
Type 2 diabetes 5A11 Liver tissue 7.75E-01 7.79E-02 3.48E-01
Ureter cancer 2C92 Urothelium 7.36E-01 6.01E-03 3.44E-02
Uterine cancer 2C78 Endometrium tissue 2.25E-09 -2.86E-01 -3.05E-01
Vitiligo ED63.0 Skin 7.61E-01 9.29E-02 2.28E-01
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⏷ Show the Full List of Expression Under 107 Diseases

Drug Affinity of This DTP Assessed by Cell Line

Approved Drug(s)
Drug Name Highest Status Cell Line Affinity REF
Aminolevulinic acid hci Approved Oocytes-PEPT1 Km = 394.0 microM [35]
Aminolevulinic acid hci Approved Oocytes-PEPT1 Km = 1600.0 microM [4]
Bestatin Approved Human enterocyte-like 2 cells (Caco-2)-PEPT1 Km = 340.0 microM [8]
Cefadroxil Approved Human cervical cancer cell line (Hela)-PEPT1 Km = 7.97 microM [11]
Cephalexin Approved Human enterocyte-like 2 cells (Caco-2)-PEPT1 Km = 7.97 microM [36]
Oseltamivir Approved Human cervical cancer cell line (Hela)-PEPT1 Km = 8590.0 microM [25]
Oseltamivir Approved Human enterocyte-like 2 cells (Caco-2)-PEPT1 Km = 6540.0 microM [25]
Valaciclovir Approved Chinese hamster ovary (CHO) cells-PEPT1 Km = 1640.0 microM [37]
Valaciclovir Approved Chinese hamster ovary (CHO) cells-PEPT1 Km = 2200.0 microM [38]
Valaciclovir Approved Chinese hamster ovary (CHO) cells-PEPT1 Km = 2700.0 microM [38]
Valaciclovir Approved Chinese hamster ovary (CHO) cells-PEPT1 Km = 5400.0 microM [38]
Valaciclovir Approved Chinese hamster ovary (CHO) cells-PEPT1 Km = 6600.0 microM [38]
Valaciclovir Approved Chinese hamster ovary (CHO) cells-PEPT1 Km = 7400.0 microM [38]
Valaciclovir Approved Chinese hamster ovary (CHO) cells-PEPT1 Km = 2.2 microM [39]
Valaciclovir Approved Chinese hamster ovary (CHO) cells-PEPT1 Km = 7.4 microM [39]
Valaciclovir Approved Human enterocyte-like 2 cells (Caco-2)-PEPT1 Km = 292.0 microM [40]
Valaciclovir Approved Madin-Darby canine kidney (MDCK) cells-PEPT1 Km = 3.8 microM [39]
Valaciclovir Approved Oocytes-PEPT1 Km = 5940.0 microM [41]
Valaciclovir Approved Xenopus oocytes-PEPT1 Km = 5.9 microM [39]
⏷ Show the Full List of 19 Approved Drug(s)

The Drug Therapeutic Target (DTT) Role of This DTP

DTP DTT Name Solute carrier family 15 member 1 (SLC15A1) DTT Info
DTP DTT Type Literature-reported
5 Investigative Drug(s) Targeting This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
4-AMBA DMYNASR Discovery agent N.A. Investigative [1]
Lys[Z(NO2)]-Pro DMJX4GA Discovery agent N.A. Investigative [2]
[11C]GlySar DM5Q08F Discovery agent N.A. Investigative [3]
[14C]GlySar DMGLQ72 Discovery agent N.A. Investigative [3]
[3H]GlySar DMFEYLS Discovery agent N.A. Investigative [3]
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References

1 Activation of vagal afferents in the rat duodenum by protein digests requires PepT1. J Nutr. 2005 Jun;135(6):1491-5.
2 A novel inhibitor of the mammalian peptide transporter PEPT1. Biochemistry. 2001 Apr 10;40(14):4454-8.
3 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. (Target id: 984).
4 Transport of the photodynamic therapy agent 5-aminolevulinic acid by distinct H+-coupled nutrient carriers coexpressed in the small intestine. J Pharmacol Exp Ther. 2010 Jan;332(1):220-8.
5 Interactions of amoxicillin and cefaclor with human renal organic anion and peptide transporters. Drug Metab Dispos. 2006 Apr;34(4):547-55.
6 Several hPepT1-transported drugs are substrates of the Escherichia coli proton-coupled oligopeptide transporter YdgR. Res Microbiol. 2017 Jun;168(5):443-449.
7 Transport of angiotensin-converting enzyme inhibitors by H+/peptide transporters revisited. J Pharmacol Exp Ther. 2008 Nov;327(2):432-41.
8 Dipeptide transporters in apical and basolateral membranes of the human intestinal cell line Caco-2. Am J Physiol. 1993 Aug;265(2 Pt 1):G289-94.
9 Membrane transporters in drug development. Nat Rev Drug Discov. 2010 Mar;9(3):215-36.
10 Protein hydrolysate-induced cholecystokinin secretion from enteroendocrine cells is indirectly mediated by the intestinal oligopeptide transporter PepT1. Am J Physiol Gastrointest Liver Physiol. 2011 May;300(5):G895-902.
11 High-affinity interaction of sartans with H+/peptide transporters. Drug Metab Dispos. 2009 Jan;37(1):143-9.
12 Intestinal transport of beta-lactam antibiotics: analysis of the affinity at the H+/peptide symporter (PEPT1), the uptake into Caco-2 cell monolayers and the transepithelial flux. Pharm Res. 1999 Jan;16(1):55-61.
13 Three-dimensional quantitative structure-activity relationship analyses of beta-lactam antibiotics and tripeptides as substrates of the mammalian H+/peptide cotransporter PEPT1. J Med Chem. 2005 Jun 30;48(13):4410-9.
14 Transporter-mediated drug delivery: recent progress and experimental approaches. Drug Discov Today. 2004 Aug 15;9(16):712-20.
15 Flavonoids with epidermal growth factor-receptor tyrosine kinase inhibitory activity stimulate PEPT1-mediated cefixime uptake into human intestinal epithelial cells. J Pharmacol Exp Ther. 2001 Oct;299(1):351-7.
16 Recognition of beta-lactam antibiotics by rat peptide transporters, PEPT1 and PEPT2, in LLC-PK1 cells. Am J Physiol. 1997 Nov;273(5 Pt 2):F706-11.
17 Increased protein level of PEPT1 intestinal H+-peptide cotransporter upregulates absorption of glycylsarcosine and ceftibuten in 5/6 nephrectomized rats. Am J Physiol Gastrointest Liver Physiol. 2005 Apr;288(4):G664-70.
18 Direct evidence for efficient transport and minimal metabolism of L-cephalexin by oligopeptide transporter 1 in budded baculovirus fraction. Biol Pharm Bull. 2009 Aug;32(8):1459-61.
19 Pharmaceutical and pharmacological importance of peptide transporters. J Pharm Pharmacol. 2008 May;60(5):543-85.
20 Transport characteristics of a novel peptide transporter 1 substrate, antihypotensive drug midodrine, and its amino acid derivatives. J Pharmacol Exp Ther. 2006 Jul;318(1):455-60.
21 Peptide transporter substrate identification during permeability screening in drug discovery: comparison of transfected MDCK-hPepT1 cells to Caco-2 cells. Arch Pharm Res. 2007 Apr;30(4):507-18.
22 The intestinal H+/peptide symporter PEPT1: structure-affinity relationships. Eur J Pharm Sci. 2004 Jan;21(1):53-60.
23 Transporter-mediated Drug Interactions. Drug Metab Pharmacokinet. 2002;17(4):253-74.
24 Absorption of lisdexamfetamine dimesylate and its enzymatic conversion to d-amphetamine. Neuropsychiatr Dis Treat. 2010 Jun 24;6:317-27.
25 Oseltamivir (tamiflu) is a substrate of peptide transporter 1. Drug Metab Dispos. 2009 Aug;37(8):1676-81.
26 Transport of levovirin prodrugs in the human intestinal Caco-2 cell line. J Pharm Sci. 2006 Jun;95(6):1318-25.
27 Studies on intestinal absorption of sulpiride (2): transepithelial transport of sulpiride across the human intestinal cell line Caco-2. Biol Pharm Bull. 2002 Oct;25(10):1345-50.
28 The role of transporters in drug interactions. Eur J Pharm Sci. 2006 Apr;27(5):501-17.
29 Valacyclovir: a substrate for the intestinal and renal peptide transporters PEPT1 and PEPT2. Biochem Biophys Res Commun. 1998 May 19;246(2):470-5.
30 Transport of valganciclovir, a ganciclovir prodrug, via peptide transporters PEPT1 and PEPT2. J Pharm Sci. 2000 Jun;89(6):781-9.
31 Drug transport in corneal epithelium and blood-retina barrier: emerging role of transporters in ocular pharmacokinetics. Adv Drug Deliv Rev. 2006 Nov 15;58(11):1136-63.
32 Tripeptides of RS1 (RSC1A1) inhibit a monosaccharide-dependent exocytotic pathway of Na+-D-glucose cotransporter SGLT1 with high affinity. J Biol Chem. 2007 Sep 28;282(39):28501-13.
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