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Volumn 7, Issue 6, 2003, Pages 917-920

Efficient Synthesis of Antisense Phosphorothioate Oligonucleotides: Evaluation of Dichloroacetic Acid at Higher Concentration to Reduce Cycle Time

Author keywords

[No Author keywords available]

Indexed keywords

ANTISENSE OLIGONUCLEOTIDE; ANTISENSE PHOSPHOROTHIOATE OLIGONUCLEOTIDE; DICHLOROACETIC ACID; PHOSPHOROTHIOIC ACID DERIVATIVE; PROPIONIC ACID DERIVATIVE; UNCLASSIFIED DRUG;

EID: 0347996086     PISSN: 10836160     EISSN: None     Source Type: Journal    
DOI: 10.1021/op030006j     Document Type: Article
Times cited : (6)

References (52)
  • 2
    • 0348101270 scopus 로고    scopus 로고
    • Special Issues for Synthetic Antisense Oligonucleotides
    • Sofer, G., Zabriskie, D. W., Eds.; Marcel Dekker: New York, Chapter 16
    • Srivatsa, G. S.; Ravikumar, V. T.; Scozzari, A. N.; Cole, D. L. Special Issues for Synthetic Antisense Oligonucleotides. In Biopharmaceutical Process Validation; Sofer, G., Zabriskie, D. W., Eds.; Marcel Dekker: New York, 2000; Chapter 16, pp 309-327.
    • (2000) Biopharmaceutical Process Validation , pp. 309-327
    • Srivatsa, G.S.1    Ravikumar, V.T.2    Scozzari, A.N.3    Cole, D.L.4
  • 4
    • 0000904633 scopus 로고    scopus 로고
    • Barton, D. H. R., Nakanishi, K., Eds.; DNA and Aspects of Molecular Biology, Kool, E. T., Vol. Ed.; Pergamon Press: Elmsford, NY
    • Iyer, R. P.; Beaucage, S. L. In Comprehensive Natural Product Chemistry; Barton, D. H. R., Nakanishi, K., Eds.; DNA and Aspects of Molecular Biology, Vol. 7; Kool, E. T., Vol. Ed.; Pergamon Press: Elmsford, NY, 1999; p 105.
    • (1999) Comprehensive Natural Product Chemistry , vol.7 , pp. 105
    • Iyer, R.P.1    Beaucage, S.L.2
  • 12
    • 0031963427 scopus 로고    scopus 로고
    • Affinitak (ISIS 3521) is targeted to the 3́-untranslated region of PKC-α mRNA selectively inhibiting PKC-α gene expression. This oligonucleotide inhibits the growth of a variety of tumor types in vivo using nude mouse tumor xenografts and sequence-specific antitumor activity supports an antisense mechanism of action in vivo. Clinical evaluation (pivotal Phase III) of this drug in humans as potential treatment for nonsmall cell lung cancer is currently ongoing. Geiger, T.; Muller, M.; Dean, N. M.; Fabbro, D. Anticancer Drug Des. 1998, 13, 35.
    • (1998) Anticancer Drug Des. , vol.13 , pp. 35
    • Geiger, T.1    Muller, M.2    Dean, N.M.3    Fabbro, D.4
  • 16
    • 0348101272 scopus 로고    scopus 로고
    • note
    • Experience has taught us that yields expressed in terms of weight/μmole of loaded support are more reliable than those expressed in terms of optical density/μmol.
  • 19
    • 0346840606 scopus 로고    scopus 로고
    • note
    • The 91% full-length is typical when the entire DMT-on peak is collected. Much higher purity (∼96-97%% full-length) is easily achieved by efficient fractionation of the DMT-on peak. Fractionation of DMT-on peak results in less than a 5% loss of full-length material.
  • 20
    • 0346840607 scopus 로고    scopus 로고
    • note
    • The purified full-length by IP-LC-MS is less than CGE values since the former analytical tool is efficiently able to distinguish and quantify process-related species such as depurinated oligonucleotides that comigrate in CGE.
  • 48
    • 0346840604 scopus 로고    scopus 로고
    • note
    • DPA has viscosity of 1.4540 vs 1.4660 for DCA.
  • 51
    • 0348101269 scopus 로고    scopus 로고
    • note
    • It was found that 40-60% of total eluted DMT groups are in the "colorless" initial eluent.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.