timtraxanib

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Ligands
timtraxanib

GtoPdb Ligand ID: 11673

Synonyms: AVI-3207 | AVI3207 | N2-acetyl-L-arginyl-L-leucyl-L-tyrosyl-L-glutamic acid

Compound class: Peptide or derivative

Comment: Timtraxanib (AVI-3207) is an angiogenesis inhibitor [2]. Structurally it is modified tetrapeptide that acts as a selective VEGF receptor-2 (VEGFR-2) inhibitor [1,3-4]. The N terminal acylation improves the peptide's stability against serum peptidase degradation [5]. Functionally, timtraxanib blocks VEGFR-2-mediated neovascularization, whilst sparing the function of VEGFR-1. Intravitreal administration of timtraxanib reduces neovascularization in animal models of age-related macular degeneration.

References
1. Baek YY, Lee DK, Kim J, Kim JH, Park W, Kim T, Han S, Jeoung D, You JC, Lee H et al.. (2017) Arg-Leu-Tyr-Glu tetrapeptide inhibits tumor progression by suppressing angiogenesis and vascular permeability via VEGF receptor-2 antagonism. Oncotarget, 8 (7): 11763-11777. [PMID:28052029]
2. Baek YY, Lee DK, So JH, Kim CH, Jeoung D, Lee H, Choe J, Won MH, Ha KS, Kwon YG et al.. (2015) The tetrapeptide Arg-Leu-Tyr-Glu inhibits VEGF-induced angiogenesis. Biochem Biophys Res Commun, 463 (4): 532-7. [PMID:26051280]
3. Koo HC, Baek YY, Choi JS, Kim YM, Sung B, Kim MJ, Kim JG, You JC. (2021) Therapeutic Efficacy of a Novel Acetylated Tetrapeptide in Animal Models of Age-Related Macular Degeneration. Int J Mol Sci, 22 (8): 3893. DOI: 10.3390/ijms22083893 [PMID:33918777]
4. Park W, Baek YY, Kim J, Jo DH, Choi S, Kim JH, Kim T, Kim S, Park M, Kim JY et al.. (2019) Arg-Leu-Tyr-Glu Suppresses Retinal Endothelial Permeability and Choroidal Neovascularization by Inhibiting the VEGF Receptor 2 Signaling Pathway. Biomol Ther (Seoul), 27 (5): 474-483. DOI: 10.4062/biomolther.2019.041 [PMID:31042676]
5. Yun JA, Kim J, Baek YY, Park W, Park M, Kim S, Kim T, Choi S, Jeoung D, Lee H et al.. (2019) N-Terminal Modification of the Tetrapeptide Arg-Leu-Tyr-Glu, a Vascular Endothelial Growth Factor Receptor-2 (VEGFR-2) Antagonist, Improves Antitumor Activity by Increasing its Stability against Serum Peptidases. Mol Pharmacol, 96 (6): 692-701. [PMID:31594790]

References

1. Baek YY, Lee DK, Kim J, Kim JH, Park W, Kim T, Han S, Jeoung D, You JC, Lee H et al.. (2017)
Arg-Leu-Tyr-Glu tetrapeptide inhibits tumor progression by suppressing angiogenesis and vascular permeability via VEGF receptor-2 antagonism.
Oncotarget, 8 (7): 11763-11777. [PMID:28052029]

2. Baek YY, Lee DK, So JH, Kim CH, Jeoung D, Lee H, Choe J, Won MH, Ha KS, Kwon YG et al.. (2015)
The tetrapeptide Arg-Leu-Tyr-Glu inhibits VEGF-induced angiogenesis.
Biochem Biophys Res Commun, 463 (4): 532-7. [PMID:26051280]

3. Koo HC, Baek YY, Choi JS, Kim YM, Sung B, Kim MJ, Kim JG, You JC. (2021)
Therapeutic Efficacy of a Novel Acetylated Tetrapeptide in Animal Models of Age-Related Macular Degeneration.
Int J Mol Sci, 22 (8): 3893. DOI: 10.3390/ijms22083893 [PMID:33918777]

4. Park W, Baek YY, Kim J, Jo DH, Choi S, Kim JH, Kim T, Kim S, Park M, Kim JY et al.. (2019)
Arg-Leu-Tyr-Glu Suppresses Retinal Endothelial Permeability and Choroidal Neovascularization by Inhibiting the VEGF Receptor 2 Signaling Pathway.
Biomol Ther (Seoul), 27 (5): 474-483. DOI: 10.4062/biomolther.2019.041 [PMID:31042676]

5. Yun JA, Kim J, Baek YY, Park W, Park M, Kim S, Kim T, Choi S, Jeoung D, Lee H et al.. (2019)
N-Terminal Modification of the Tetrapeptide Arg-Leu-Tyr-Glu, a Vascular Endothelial Growth Factor Receptor-2 (VEGFR-2) Antagonist, Improves Antitumor Activity by Increasing its Stability against Serum Peptidases.
Mol Pharmacol, 96 (6): 692-701. [PMID:31594790]