+ 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

Synthesis, biological studies and molecular dynamics of new anticancer RGD-based peptide conjugates for targeted drug delivery

, : Synthesis, biological studies and molecular dynamics of new anticancer RGD-based peptide conjugates for targeted drug delivery. Bioorganic & Medicinal Chemistry 24(2): 294-303

New cyclic RGD peptide-anticancer agent conjugates, with different chemical functionalities attached to the parent peptide were synthesized in order to evaluate their biological activities and to provide a comparative study of their drug release profiles. The Integrin binding c(RGDfK) penta-peptide was used for the synthesis of Camptothecin (CPT) carbamate and Chlorambucil (CLB) amide conjugates. Substitution of the amino acid Lys with Ser resulted in a modified c(RGDfS) with a new attachment site, which enabled the synthesis of an ester CLB conjugate. Functional versatility of the conjugates was reflected in the variability of their drug release profiles, while the conserved RGD sequence of a selective binding to the αv integrin family, likely preserved their recognition by the Integrin and consequently their favorable toxicity towards targeted cancer cells. This hypothesis was supported by a computational analysis suggesting that all conjugates occupy conformational spaces similar to that of the Integrin bound bio-active parent peptide.


PMID: 26719208

DOI: 10.1016/j.bmc.2015.12.020

Other references

Abbott, N.J., 1991: Glial-neuronal Interaction. Annals of the New York Academy of Sciences 633: 1-636

Daqiq, L.; Larroque, O.R.; Stoddard, F.L.; Bekes, F., 2000: Extractability and size distribution studies on wheat proteins using flow-field flow fractionation. Ways to optimize solubilization of wheat polymeric proteins with the minimum possible changes from their native state were investigated. The molecular size of wheat polymeric proteins using different sonication times were also determined. Protein...

Waterhouse, J.; Kao, S.; Edwards, B.; Weinert, D.; Atkinson, G.; Reilly, T., 2005: Transient changes in the pattern of food intake following a simulated time-zone transition to the east across eight time zones. Twelve healthy adults were studied, singly or in groups of Lip to four, in an Isolation Unit before (control days) and for 3 days after a simulated time-zone transition to the east across 8 time zones (the clock being changed from 15:00 to 23:0011...

Amano, K.; Amano, K., 1999: Filter leukapheresis for patients with ulcerative colitis: clinical results and the possible mechanism. To certify the feasibility of leukapheresis, 37 ulcerative colitis (UC) patients, who had failed to recover by conventional treatment were enrolled in this treatment. Imugard (Terumo Co., Ltd., Tokyo Japan) or Cellsorba (Asahi Medical) filters wer...

Baker, C.D.; Balasubramaniam, V.; Mourani, P.M.; Sontag, M.K.; Black, C.P.; Ryan, S.L.; Abman, S.H., 2013: Cord blood angiogenic progenitor cells are decreased in bronchopulmonary dysplasia. Bronchopulmonary dysplasia (BPD), the chronic lung disease of prematurity, is associated with impaired vascular and alveolar growth. Antenatal factors contribute to the risk for developing BPD by unclear mechanisms. Endothelial progenitor cells, s...

Bennett F.C.; Silver G.; Leung E.J.; Mack L.A., 1989: The usefulness of periventricular echodensities on cranial ultrasound in predicting neurodevelopmental outcome in low birthweight premature infants. Clinical Research 37(1): 169A

Chazalette, J.P.; Dain, M.P.; Castaigne, J.P., 1988: Efficacy of pancrease: crossover comparative study versus eurobiol in cystic fibrosis. An open crossover study in patients with documented cystic fibrosis (CF) compared the efficacy and acceptability of Pancrease (Cilag, PC), consisting of pH-sensitive, enteric-coated microspheres, with those of Eurobiol, consisting of lyophilized t...

Rossova, M.M., 1960: Hygienic characteristics of vegetable oils subjected to thermal treatment. Gigiena i Sanitariia 25: 97-98

Tarumi, Y.; Pereira, J.; Watanabe, S., 2002: Methadone and fluconazole: respiratory depression by drug interaction. A 60-year-old man with advanced gastric cancer achieved good pain control on a stable dose of methadone for 10 days. However, he developed respiratory depression 2 days after intravenous fluconazole was administrated for refractory oral candidiasi...

Falebita, O.A.; Mancini, S.; Kiely, E.; Comber, H., 2008: Rising incidence of renal cell carcinoma in Ireland. To determine the trend in the incidence of renal cell carcinoma in Ireland, and evaluate changes in the modes of presentation and outcomes. Data on all histologically diagnosed renal cancers in Ireland over a 12-year period (1994-2005) were retrie...