36099-95-3

Usage

Uses

Used in Pharmaceutical Applications:
H-TRP-GLU-OH is used as a pharmaceutical agent for its role as a selective and reversible PPAR antagonist. This property makes it a potential candidate for the development of drugs targeting various diseases and conditions where PPAR activity is a factor.
Used in Research and Development:
In the field of research and development, H-TRP-GLU-OH serves as a valuable tool for studying the role of PPAR in cellular processes and disease mechanisms. Its reversible antagonistic action allows researchers to investigate the effects of PPAR modulation in a controlled manner.
Used in Drug Delivery Systems:
Similar to gallotannin, H-TRP-GLU-OH can also be incorporated into drug delivery systems to enhance its bioavailability and therapeutic outcomes. By using various organic and metallic nanoparticles as carriers, the delivery, efficacy, and targeting of H-TRP-GLU-OH to specific cells or tissues can be improved, potentially leading to more effective treatments for related conditions.

Biological Activity

kd = 8.34 μmg3335 is a pparγ antagonist.the peroxisome proliferator-activated receptor gamma (ppargamma) is a key therapeutic drug target for several conditions, such as inflammation, diabetes, hypertension, dyslipidemia, and cancer.

in vitro

biacore 3000 study based on the surface plasmon resonance technique found that g3335 exhibited a highly specific binding affinity against ppargamma and was able to block rosiglitazone, a potent ppargamma agonist, in the stimulation of the interaction between the ppargamma ligand-binding domain (lbd) and rxralpha-lbd. moreover, the yeast two-hybrid assays indicated that g3335 had strong antagonistic activity in perturbing rosiglitazone in the promotion of the ppargamma-lbd-cbp interaction. in addition, g3335 could competitively bind to ppargamma against 0.1 microm rosiglitazone to repress reporter-gene expression [1].

in vivo

in a previous study, the effect of rosiglitazone was examined on spinal cord injury (sci) in rats. the animals were randomly divided into vehicle group, rosiglitazone treated group, and g3335 treated group. locomotor function recovery was evaluated. results showed that compared with the vehicle groups, the rosiglitazone could significantly ameliorate locomotor recovery, reduce nf-κb expression, and increase the proliferation of endogenous npcs. in addition, when the ppar-γ antagonist g3335 was applied, such effects were abolished [2].

references

[1] ye, f. ,zhang, z.s.,luo, h.b., et al. the dipeptide h-trp-glu-oh shows highly antagonistic activity against pparγ: bioassay with molecular modeling simulation. chembiochem 7, 74-82 (2006).[2] meng, q. q.,liang, x.j.,wang, p., et al. rosiglitazone enhances the proliferation of neural progenitor cells and inhibits inflammation response after spinal cord injury. neuroscience letters 503, 191-195 (2011).