+ Resolve Article
+ Follow Us
Follow on FacebookFollow on Facebook
Follow on TwitterFollow on Twitter

+ Translate
+ Subscribe to Site Feed
GeoScience Most Shared ContentMost Shared Content

Molecular modelling, synthesis and biological evaluation of peptide inhibitors as anti-angiogenic agent targeting neuropilin-1 for anticancer application

, : Molecular modelling, synthesis and biological evaluation of peptide inhibitors as anti-angiogenic agent targeting neuropilin-1 for anticancer application. Journal of Biomolecular Structure & Dynamics (): 1-20

NlmCategory="UNASSIGNED">Vascular endothelial growth factor (VEGF) and its co-receptor neuropilin-1 (NRP-1) are important targets of many pro-angiogenic factors. In this study, nine peptides were synthesized and evaluated for their molecular interaction with NRP-1 and compared to our previous peptide ATWLPPR. Docking study showed that the investigated peptides shared the same binding region as shown by tuftsin known to bind selectively to NRP-1. Four pentapeptides (DKPPR, DKPRR, TKPPR and TKPRR) and a hexapeptide CDKPRR demonstrated good inhibitory activity against NRP-1. In contrast, peptides having arginine residue at sites other than the C-terminus exhibited low activity towards NRP-1 and this is confirmed by their inability to displace the VEGF165 binding to NRP-1. Docking study also revealed that replacement of carboxyl to amide group at the C-terminal arginine of the peptide did not affect significantly the binding interaction to NRP-1. However, the molecular affinity study showed that these peptides have marked reduction in the activity against NRP-1. Pentapeptides having C-terminal arginine showed strong interaction and good inhibitory activity with NRP thus may be a good template for anti-angiogenic targeting agent.


PMID: 26766582

DOI: 10.1080/07391102.2015.1131196

Other references

Mourad, J-Jacques.; Amodeo, C.; de Champvallins, M.; Brzozowska-Villatte, R.; Asmar, R., 2017: Blood pressure-lowering efficacy and safety of perindopril/indapamide/amlodipine single-pill combination in patients with uncontrolled essential hypertension: a multicenter, randomized, double-blind, controlled trial. This 4-month, double-blind, randomized, controlled trial was designed to demonstrate the superiority of perindopril/indapamide/amlodipine single pill over perindopril/indapamide after 1 month and to determine further up-titration efficacy and safe...

Fakhri, A.; Naji, M., 2017: Degradation photocatalysis of tetrodotoxin as a poison by gold doped PdO nanoparticles supported on reduced graphene oxide nanocomposites and evaluation of its antibacterial activity. In this project, synthesis of pure and gold doped PdO-reduced graphene oxide nanocomposites by sonochemical and deposition-precipitation process was performed and characterized using X-ray diffraction (XRD), transmission electronic microscopy (TEM...

Balmukhanov, A., 1965: Oscillographic studies of the vascular tone in operations on the eyes. Vestnik Oftalmologii 78(6): 78-80

Bertuglia, S.; Colantuoni, A.; Calisi, E.; Gambardella, P.; Cifaldi, S., 1981: Relation between blood pH and flow in microcirculation in the rat. Bollettino Della Societa Italiana di Biologia Sperimentale 57(24): 2405-2409

Lagier, G.; Dally, S.; Fournier, E., 1986: Imputability is not a synonym for responsibility. Therapie 41(3): 215-217

Oyesiku, N.M.; Wilcox, J.N.; Wigston, D.J., 1997: Changes in expression of ciliary neurotrophic factor (CNTF) and CNTF-receptor alpha after spinal cord injury. To determine if ciliary neurotrophic factor (CNTF) is involved in the response to spinal cord injury, we studied changes in the expression of CNTF and that of its receptor, CNTF-receptor a (CNTFR-alpha), in the rat spinal cord after a unilateral s...

Burki B.; Cocard M.; Kahle H.G.; Zerbini S., 1999: Sea level fluctuations in the Mediterranean and their interactions with climate processes and vertical crustal movements (SELF). Pages 72 1999

Burdette L.J.; Dyer R.S., 1986: Sulfolane effects on audiogenic pentylenetetrazole and afterdischarge seizure activity. Sulfolane dosages that alter seizure susceptibility were determined using audiogenic (AG), pentylenetetrazol (PTZ) and hippocampal afterdischarge (AD) seizure models. The presence of AG seizures and potentiation of PTZ seizures were investigated i...

Mummadi, R.R.; Groce, J.R.; Raju, G.S.; Gomez, G., 2008: Endoscopic management of colocutaneous fistula in a morbidly obese woman (with video). Gastrointestinal Endoscopy 67(7): 1207-1208

Todoroff, P.; Lorion, R.; Luk, J.D.niel Lan Sun, 1998: Genetic algorithms for the identification of soil water content profiles from time-domain reflectometry traces. We developed a unidimensional microwave propagation model in a stratified medium. it calculates, from a given soil water content profile, the reflected signal trace one would measure by timedomain reflectometry along a transmission line inserted i...