Description
Reversin 121 is a hydrophobic peptide chemosensitizer that can reverse P-glycoprotein-mediated multidrug resistance. It binds to the P-glycoprotein multidrug transporter (MDR1) with a K
d value of 77 nM. Reversin 121 modulates P-glycoprotein ATPase activity in S
f9 insect cell membranes expressing human MDR1, plasma membrane vesicles from multidrug-resistant cells, and reconstituted proteoliposomes as well as in a variety of MDR1-expressing intact tumor cells.
Uses
Reversin 121 has been used to determine the activity of P-glycoprotein in human retinal pigment epithelium.
General Description
Reversin 121 is an analog of reversin and a dipeptide derivative.
Biochem/physiol Actions
Peptide chemosensitizer, inhibitor of P-glycoprotein.
in vivo
Reversin 121 (2.5 mg/kg, plus 5-fluorouracil, 35 mg/kg/day, i.p.) decreases tumor size and prevalence of metastases[1].
| Animal Model: | Orthotopic pancreatic carcinoma mouse model[1]. |
| Dosage: | 2.5 mg/kg, plus 5-fluorouracil, 35 mg/kg/day |
| Administration: | Intraperitoneal injection (i.p.), 5 days a week |
| Result: | Decreased in MRP3-positive cells. |
References
[1] FRANCES J SHAROM . Interaction of the P-glycoprotein multidrug transporter (MDR1) with high affinity peptide chemosensitizers in isolated membranes, reconstituted systems, and intact cells[J]. Biochemical pharmacology, 1999, 58 4: Pages 571-586. DOI:
10.1016/s0006-2952(99)00139-2[2] EUNICE L KWAK. Irreversible inhibitors of the EGF receptor may circumvent acquired resistance to gefitinib.[J]. Proceedings of the National Academy of Sciences of the United States of America, 2005, 102 21: 7665-7670. DOI:
10.1073/pnas.0502860102[3] PRIYANKA S. RANA . Calibration and characterization of intracellular Asante Potassium Green probes, APG-2 and APG-4[J]. Analytical biochemistry, 2019, 567: Pages 8-13. DOI:
10.1016/j.ab.2018.11.024
