Drug Transporter (DT) Information

General Information of DT
DT ID DTD0022
Gene Name SLC15A2
Protein Name Peptide transporter 2
Gene ID
6565
UniProt ID
Q16348
TCDB ID
2.A.17.4.8
3D Structure

Modelled DT Structure

Method:homology modeling

Template PDB:2XUT_A

Identity:30.7%

Minimized Score:-615.174 kcal/mol

Detail: Structure Info

Synonyms Kidney H(+)/peptide cotransporter; Oligopeptide transporter, kidney isoform; PEPT2; SLC15A2; Solute carrier family 15 member 2
DT Family Proton-Dependent Oligopeptide Transporter (POT/PTR) Family ;
Tissue Specificity Expressed in kidney. Not detected inintestine.
Function This tranporter mediates intake of oligopeptides of 2 to 4 amino acids with a preference for dipeptides. Transports the dipeptide-like aminopeptidase inhibitor bestatin. Can also transport the aminocephalosporin antibiotic cefadroxil.
Disease(s) High blood pressure [ICD-11:BA00]
Peripheral T-cell lymphoma [ICD-11:2A90.C]
Streptococcal pharyngitis [ICD-11:1B51]
Shingles [ICD-11:1.00E+91]
Endogenous Substrate(s) Peptides
Variability Data of This Drug Transporter (DT)

Regulatory Variability Data of This DT (VARIDT 4.0)

(α) Tissue Distribution Level of Peptide transporter 2
Tissue Distribution Level (TD)

(β) Cell Distribution Level of Peptide transporter 2
Cell Distribution Level (CD)

(γ) Organelle Distribution Level of Peptide transporter 2
Organelle Distribution Level (Subc)

Regulatory Variability Data of This DT

(α) Microbiota Influence of Peptide transporter 2
Microbiota Influence (MBI)

(β) Post-translational Modification of Peptide transporter 2
Post-translational Modification (PTM)

(γ) Transcriptional Regulation of Peptide transporter 2
Transcriptional Regulation (TSR)

(δ) Epigenetic Regulation of Peptide transporter 2
Epigenetic Regulation (EGR)

(ε) Exogenous Modulation of Peptide transporter 2
Exogenous Modulation (EGM)

Structural Variability Data of This DT

(α) Mutation-induced Structural Variation
Mutation-induced Structural Variation (MSV)

(β) Inter-species Structural Differences
Inter-species Structural Differences (ISD)

(γ) Outward/inward-facing Conformation
Outward/inward-facing Conformation (OIC)

(δ) Xenobiotics-regulated Structural Variability
Xenobiotics-regulated Structural Variability (XSV)

General Variability Data of This DT

(α) Genetic Polymorphisms of Peptide transporter 2
Genetic Polymorphisms of This DT (GPD)

(β) Disease-specific Protein Abundances of Peptide transporter 2
Disease-specific Protein Abundances of This DT (DPAD)

(γ) Species- and Tissue-specific DT Abundances
Species/Tissue-specific Protein Abundances of This DT (S/TPAD)
Molecular Transporting Profile of This DT

Full List of Drug(s) Transported by This DT

 Approved Drug

 Click to Show/Hide the Full List of Drug:         25 Drugs in Total
Drug Name Highest Status Detail Indication ICD 11 Ref
Aminolevulinic acid
 Approved Drug Info Photodynamic therapy EK90.0 [1]
Amoxicillin
 Approved Drug Info Streptococcal pharyngitis 1B51 [2]
Ampicillin
 Approved Drug Info Bacterial infections 1A00-1H0Z [3]
Ampicillin
 Approved Drug Info Bacterial infections 1A00-1H0Z [3]
Benazepril
 Approved Drug Info High blood pressure BA00 [4]
Bestatin
 Approved Drug Info Acute myeloid leukemia 2A60 [5]
Cefaclor
 Approved Drug Info Gram-positive & negative bacteria infections 1A00-1H0Z [2]
Cefadroxil
 Approved Drug Info Gram-positive & negative bacteria infections 1A00-1H0Z [6]
Cefixime
 Approved Drug Info Streptococcus bacterial infections 1C41 [3]
Cefixime
 Approved Drug Info Streptococcus bacterial infections 1C41 [3]
Ceftibuten
 Approved Drug Info Chronic bronchitis CA20.1 [3]
Cephalexin
 Approved Drug Info Gram-positive bacteria infections 1A00-1H0Z [3]
Cephradine
 Approved Drug Info Streptococcus pneumoniae infections CA40.0Y [3]
Cyclacillin
 Approved Drug Info Bacterial infections 1A00-1H0Z [3]
Dicloxacillin
 Approved Drug Info Susceptible gram-positive bacteria infections 1A00-1H0Z [3]
Enalapril
 Approved Drug Info High blood pressure BA00 [7]
Entecavir
 Approved Drug Info Chronic hepatitis B infection 1E51.0 [8]
Fosinopril
 Approved Drug Info High blood pressure BA00 [9]
Moexipril
 Approved Drug Info High blood pressure BA00 [4]
Moxalactam
 Approved Drug Info Bacterial infections 1A00-1H0Z [3]
Perindopril
 Approved Drug Info High blood pressure BA00 [4]
Ramipril
 Approved Drug Info High blood pressure BA00 [4]
Spirapril
 Approved Drug Info High blood pressure BA00 [4]
Trandolapril
 Approved Drug Info High blood pressure BA00 [4]
Valacyclovir
 Approved Drug Info Shingles 1.00E+91 [10]

 Withdrawn, Discontinued or Preclinical Drug

 Click to Show/Hide the Full List of Drug:           1 Drugs in Total
Drug Name Highest Status Detail Indication ICD 11 Ref
Metampicillin
 Preclinical Drug Info Bacterial infections 1A00-1H0Z [3]

Drug-DT Affinity Assessed by Cell Line

 Approved Drug

 Click to Show/Hide the Full List of Drug:         17 Drugs in Total
Drug Name Highest Status Detail Cell Line Affinity Ref
Aminolevulinic acid Approved Drug Info Oocytes-PEPT2 Km =227 microM [11]
Aminolevulinic acid Approved Drug Info Oocytes-PEPT2 Km =227 microM [11]
Aminolevulinic acid Approved Drug Info Oocytes-PEPT2 Km =227 microM [11]
Amoxicillin Approved Drug Info Madin-Darby canine kidney (MDCK) cells-PEPT2 Km =1040 microM [2]
Amoxicillin Approved Drug Info Madin-Darby canine kidney (MDCK) cells-PEPT2 Km =1040 microM [2]
Amoxicillin Approved Drug Info Madin-Darby canine kidney (MDCK) cells-PEPT2 Km =1040 microM [2]
Amoxicillin Approved Drug Info Madin-Darby canine kidney (MDCK) cells-PEPT2 Km =1040 microM [2]
Cefaclor Approved Drug Info Madin-Darby canine kidney (MDCK) cells-PEPT2 Km =72 microM [2]
Cefaclor Approved Drug Info Madin-Darby canine kidney (MDCK) cells-PEPT2 Km =72 microM [2]
Cefaclor Approved Drug Info Madin-Darby canine kidney (MDCK) cells-PEPT2 Km =72 microM [2]
Cefaclor Approved Drug Info Madin-Darby canine kidney (MDCK) cells-PEPT2 Km =72 microM [2]
Cefadroxil Approved Drug Info In vivo model (human) Km =150.8 microM [6]
Cefadroxil Approved Drug Info In vivo model (human) Km =150.8 microM [6]
Cefadroxil Approved Drug Info In vivo model (human) Km =150.8 microM [6]
Cefadroxil Approved Drug Info In vivo model (human) Km =150.8 microM [6]
Cefadroxil Approved Drug Info In vivo model (human) Km =150.8 microM [6]
Cefadroxil Approved Drug Info In vivo model (human) Km =150.8 microM [6]
References
1 PEPT2-mediated transport of 5-aminolevulinic acid and carnosine in astrocytes. Brain Res. 2006 Nov 29;1122(1):18-23.
2 Interactions of amoxicillin and cefaclor with human renal organic anion and peptide transporters. Drug Metab Dispos. 2006 Apr;34(4):547-55.
3 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.
4 Transport of angiotensin-converting enzyme inhibitors by H+/peptide transporters revisited. J Pharmacol Exp Ther. 2008 Nov;327(2):432-41.
5 Molecular mechanism of dipeptide and drug transport by the human renal H+/oligopeptide cotransporter hPEPT2. Am J Physiol Renal Physiol. 2008 Jun;294(6):F1422-32.
6 Species Differences in Human and Rodent PEPT2-Mediated Transport of Glycylsarcosine and Cefadroxil in Pichia Pastoris Transformants. Drug Metab Dispos. 2017 Feb;45(2):130-136.
7 Ethanol inhibits functional activity of the human intestinal dipeptide transporter hPepT1 expressed in Xenopus oocytes. Alcohol Clin Exp Res. 2008 May;32(5):777-84.
8 The oligopeptide transporter 2-mediated reabsorption of entecavir in rat kidney. Eur J Pharm Sci. 2014 Feb 14;52:41-7.
9 Mechanism of intestinal absorption and renal reabsorption of an orally active ace inhibitor: uptake and transport of fosinopril in cell cultures. Drug Metab Dispos. 2001 Oct;29(10):1307-15.
10 Valacyclovir: a substrate for the intestinal and renal peptide transporters PEPT1 and PEPT2. Biochem Biophys Res Commun. 1998 May 19;246(2):470-5.
11 Delta-aminolevulinic acid transport by intestinal and renal peptide transporters and its physiological and clinical implications. J Clin Invest. 1998 Jun 15;101(12):2761-7.

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