Transformation of PGI2 to exPGI2 by PGT

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Prostaglandin Transporter


Rate equation

R103.PNG

Transport Parameters

Kms

Literature values
Value Units Species Notes Weight Reference
0.0054 mM Human Eye Vector: HEK-OATP2A1 or HEK-OATP2B1 and the respective vector controls

Substrate: Latanoprost, a prostaglandin F2a analogue pH: 7.5 Temp: 37 °C

2048 [1]
0.000331 ± 0.000131 mM Transfected Human embryonic kidney cells (HEK293) Substrate: PGE2

pH: unknown Temp: 37 °C

512 [2]
0.007202 ± 0.000595 mM Transfected Human embryonic kidney cells (HEK293) Substrate: PGE3

pH: unknown Temp: 37 °C

512 [2]
0.000376 ± 3.4e-5 mM PGT-expressing Madin-Darby Canine Kidney Epithelial Cells (MDCK) cells Substrate: PGH2

pH: unknown Temp: unknown

192 [3]
9.40E-05 mM Human Substrate: PGE2

Species: Human Vector: HeLa Cell Line pH: 7 Temperature: 27

1024 [4]
0.000423 mM Human Substrate: TXB2

Species: Human Vector: HeLa Cell Line pH: 7 Temperature: 27

1024 [4]
0.007569 mM Human Substrate: 6-Keto-PGF1a

Species: Human Vector: HeLa Cell Line pH: 7 Temperature: 27

1024 [4]
4.87E-05 mM Human Substrate: PGE2

Species: Human Vector: HeLa Cell Line pH: 7 Temperature: 27

1024 [5]
Description of the PGT Kms distribution
Mode (mM) Confidence Interval Location parameter (µ) Scale parameter (σ)
1.10E-03 9.42E+01 -4.67E+00 1.45E+00
The estimated probability distribution for PGT Kms. The value and weight of the literature values used to define the distribution are indicated by an orange dashed line. The x axis is plotted on a log-scale.

kcat

No data available on the turnover of PGT/ an organic molecule transporter therefore based upon estimates made by http://book.bionumbers.org/what-are-the-rates-of-membrane-transporters/

Turnover Number
Value Units Transporter Notes Weight Reference
3.5 min-1 Glucose transporter ptsI Organism: Bacteria Escherichia coli

Back of the envelope calculation by BioNumbers: http://bionumbers.hms.harvard.edu/bionumber.aspx?&id=102931

8 [6]
0.33 - 0.83 min-1 Rate of transport of H+/Lactose transporter Organism: Bacteria Escherichia coli

Back of the envelop calculation on bionumbers http://bionumbers.hms.harvard.edu/bionumber.aspx?&id=103159

8 [7]
3.28 min-1 Catalytic Rate of transporter HXT7 Organism: Budding yeast Saccharomyces cerevisiae

Back of the envelope calculation http://bionumbers.hms.harvard.edu/bionumber.aspx?&id=101737

8 [8]
Description of the PGT kcat distribution
Mode (min-1) Confidence Interval Location parameter (µ) Scale parameter (σ)
1.33E+00 7.30E+00 9.20E-01 8.00E-01
The estimated probability distribution for PGT kcat. The value and weight of the literature values used to define the distribution are indicated by an orange dashed line. The x axis is plotted on a log-scale.

Transporter concentration

To convert the enzyme concentration from ppm to mM, the following equation was used.

Abundance
Value Units Species Notes Weight Reference
125 ppm Human Vector:Lung

Enzyme: SLCO2A1 pH: 7.5 Temperature: 37 °C

2048 [9]
17.4 ppm Human Expression Vector: Esophagus

Enzyme: SLCO2A1 pH: 7.5 Temperature: 37 °C

2048 [10]
2.82 ppm Human Vector:Gut

Enzyme: SLCO2A1 pH: 7.5 Temperature: 37 °C

2048 [9]
Description of the PGT concentration distribution
Mode (ppm) Mode (mM) Confidence Interval Location parameter (µ) Scale parameter (σ)
1.73E+01 9.57E-05 4.72E+00 3.90E+00 1.02E+00


The estimated probability distribution for PGT concentration. The value and weight of the literature values used to define the distribution are indicated by an orange dashed line. The x axis is plotted on a log-scale.

References

  1. M. Kraft The prostaglandin transporter OATP2A1 is expressed in human ocular tissues and transports the antiglaucoma prostanoid latanoprost. Invest Ophthalmol Vis Sci. 2010 May;51(5):2504-11. doi: 10.1167/iovs.09-4290. Epub 2009 Dec 17.
  2. 2.0 2.1 Gose T. Prostaglandin transporter (OATP2A1/SLCO2A1) contributes to local disposition of eicosapentaenoic acid-derived PGE3. Prostaglandins Other Lipid Mediat. 2016 Jan;122:10-7. doi: 10.1016/j.prostaglandins.2015.12.003. Epub 2015 Dec 10.
  3. Chi Y. The prostaglandin transporter PGT transports PGH2 Biochemical and Biophysical Research Communications, Volume 395, Issue 2, 30 April 2010, Pages 168–172
  4. 4.0 4.1 4.2 [http://science.sciencemag.org/content/sci/268/5212/866.full.pdf Kanai N. Identification and Characterization of a Prostaglandin Transporter Science 12 May 1995:Vol. 268, Issue 5212, pp. 866-869, DOI: 10.1126/science.7754369]
  5. Shigekazu I. Structural Determinants of Substrates for the Prostaglandin Transporter PGT Molecular Pharmacology October 1996, 50 (4) 736-742; DOI: https://doi.org/10.1124/mol.50.4.736
  6. Waygood EB Enzyme I of the phosphoenolpyruvate: sugar phosphotransferase system of Escherichia coli. Purification to homogeneity and some properties.Can J Biochem. 1980 Jan;58(1):40-8.
  7. Naftalin R. J. ELactose permease H+-lactose symporter: mechanical switch or Brownian ratchet?Biophys J. 2007 May 15;92(10):3474-91. Epub 2007 Feb 26.
  8. Ye L. Expression and activity of the Hxt7 high-affinity hexose transporter of Saccharomyces cerevisiaeYeast. 2001 Sep 30;18(13):1257-67.
  9. 9.0 9.1 M. Kim A draft map of the human proteome Nature, 2014 509, 575–581
  10. M. Wilhelm Mass-spectrometry-based draft of the human proteome Nature, 2014 509, 582–587