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Volumn 21, Issue 14, 2011, Pages 4332-4336

Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP

Author keywords

Apoptosis; Monovalent Smac mimietics; Probe compounds; XIAP

Indexed keywords

SECOND MITOCHONDRIAL ACTIVATOR OF CASPASE; TRIPEPTIDE DERIVATIVE; X LINKED INHIBITOR OF APOPTOSIS;

EID: 79959871720     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.05.049     Document Type: Article
Times cited : (29)

References (29)
  • 25
    • 79959882179 scopus 로고    scopus 로고
    • 13C). The yields for the first two steps ranged from 70 - 90% while the yields for the last step ranged from 20 - 90%. The purity of each final product was greater than 95% as determined by HPLC/MS analysis
    • 13C). The yields for the first two steps ranged from 70 - 90% while the yields for the last step ranged from 20 - 90%. The purity of each final product was greater than 95% as determined by HPLC/MS analysis.
  • 26
    • 79959892682 scopus 로고    scopus 로고
    • Fluorescence polarization assays were run in 20 μL volume in 384 well format with black plates. The assay solution was 25 mM Hepes at pH 7.5/1 mM tris(2-carboxyethyl)phosphine/0.005% Tween 20 and 20 nM AVPIAQK-rhodamine. XIAP BIR2 was present at 1 μM or XIAP BIR3 at 0.2 μM. Compound was present within a range of 100 μM to 6.1 nM using two fold dilutions starting at 100 μM generating a 16 point curve. Plates were read on an Analyst HT in fluorescence polarization mode with excitation at 530 nm, emission at 580 nm and a dichroic mirror at 565 nm. Resulting data in mP was fit in GraphPad Prism 5 with a non-linear regression using a sigmodial curve with variable slope
    • Fluorescence polarization assays were run in 20 μL volume in 384 well format with black plates. The assay solution was 25 mM Hepes at pH 7.5/1 mM tris(2-carboxyethyl)phosphine/0.005% Tween 20 and 20 nM AVPIAQK-rhodamine. XIAP BIR2 was present at 1 μM or XIAP BIR3 at 0.2 μM. Compound was present within a range of 100 μM to 6.1 nM using two fold dilutions starting at 100 μM generating a 16 point curve. Plates were read on an Analyst HT in fluorescence polarization mode with excitation at 530 nm, emission at 580 nm and a dichroic mirror at 565 nm. Resulting data in mP was fit in GraphPad Prism 5 with a non-linear regression using a sigmodial curve with variable slope.
  • 28
    • 79959877553 scopus 로고    scopus 로고
    • 6) δ 169.6, 169.3, 132.6, 131.1, 127.4, 125.9, 114.5, 111.1, 110.4, 100.9, 60.2, 56.4, 55.9, 47.3, 38.2, 31.3, 30.0, 29.5, 24.7, 19.0, 18.2, 16.3. MS m/z = 414 (M+H)
    • 6) δ 169.6, 169.3, 132.6, 131.1, 127.4, 125.9, 114.5, 111.1, 110.4, 100.9, 60.2, 56.4, 55.9, 47.3, 38.2, 31.3, 30.0, 29.5, 24.7, 19.0, 18.2, 16.3. MS m/z = 414 (M+H).


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.