메뉴 건너뛰기




Volumn 17, Issue 16, 2007, Pages 4518-4522

Novel prodrug approach to photodynamic therapy: Fmoc solid-phase synthesis of a cell permeable peptide incorporating 5-aminolaevulinic acid

Author keywords

5 Aminolaevulinic acid; Cell penetrating peptide; Photodynamic therapy; Prodrug; Solid phase peptide synthesis

Indexed keywords

AMINOLEVULINIC ACID; PHOTOSENSITIZING AGENT; PROTOPORPHYRIN;

EID: 34447331718     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2007.05.095     Document Type: Article
Times cited : (21)

References (28)
  • 20
    • 34447314553 scopus 로고    scopus 로고
    • note
    • R = 11.69 min. Compound 2 (285 mg, 0.13 mmol) was dissolved in TFA/thioanisole/water/DCM (16:2:1:1, 10 mL) and stirred at room temperature for 2 h. The solvent was removed in vacuo and the resulting residue partitioned between water (20 mL) and Et...
  • 23
    • 0032190770 scopus 로고    scopus 로고
    • The solid phase synthesis of a 2-ALA derivative has been reported-see
    • The solid phase synthesis of a 2-ALA derivative has been reported-see. Marcaurelle L.A., and Bertozzi C.R. Tetrahedron Lett. 39 (1998) 7279
    • (1998) Tetrahedron Lett. , vol.39 , pp. 7279
    • Marcaurelle, L.A.1    Bertozzi, C.R.2
  • 25
    • 34447317895 scopus 로고    scopus 로고
    • note
    • 4 cells per well. After 48 h, the culture medium was removed, and the wells were washed with PBS. The cells were incubated with freshly prepared solutions of 3 at 0.005, 0.01, 0.05, 0.01, and 0.5 mM. Serum-free medium (100 μL) containing varying prodrug concentrations was added to a designated series of wells. Each plate contained control wells with cells, but without added drug for determination of the background reading, and reference wells containing cells incubated with the same ALA concentrations. Fluorescence readings were taken at 4, 5, 7, 24, and 48 h after addition of 3, and the plates were incubated at 37 °C between measurements. The fluorescence signal from each well was measured using a Perkin-Elmer LS-50B spectrofluorimeter, with excitation at 405 nm and 635 nm emission, with slit widths set to 10 nm and an internal 530 longpass filter used on the emission side. The mean fluorescence was calculated after subtraction of the control values (i.e., without addition of ALA). For temperature studies, PAM212 were seeded in two 96-well plates, as before, and treated with 3 (0.3mM in clear media, 100 μL/well). The plates were wrapped in foil and incubated at 37 and 4 °C, respectively, for 12 h, whereupon the prodrug solution was removed. The cells were rinsed in PBS and clear media (100 μL) were added to each well. Generation of PpIX fluorescence was then monitored as before.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.