T.cntdot.C.cntdot.G triplet in an antiparallel purine.cntdot.purine.cntdot.pyrimidine DNA triplex. conformational studies by NMR

Biochemistry ◽  
1994 ◽  
Vol 33 (14) ◽  
pp. 4111-4120 ◽  
Author(s):  
Karen Dittrich ◽  
Juan Gu ◽  
Robert Tinder ◽  
Michael Hogan ◽  
Xiaolian Gao
Keyword(s):  
Conformational Studies ◽  
Dna Triplex

Antigene and Antiproliferative Effects of Triplex-Forming Oligonucleotide (TFO) Targeted on hmgb1 Gene in Human Hepatoma Cells

2020 ◽  
Vol 20 (16) ◽  
pp. 1943-1955
Author(s):  
Neelam Lohani ◽  
Moganty R. Rajeswari
Keyword(s):  
Apoptotic Cell ◽  
Isothermal Calorimetry ◽  
High Mobility ◽  
Rational Drug Design ◽  
Human Hepatoma Cells ◽  
Aberrant Expression ◽  
Bioinformatic Tools ◽  
Hmgb1 Expression ◽  
Dna Triplex ◽  
Triplex Forming Oligonucleotide

Background: The high mobility group box 1 (hmgb1) is one of the frequently over-expressed genes whose aberrant expression is reported in a number of human cancers. Various strategies are underway to inhibit hmgb1 expression in cancer cells having considerable therapeutic value. Objective: The present work involves selective transcriptional inhibition of the hmgb1 gene using selective DNA triplex structure-based gene technology. Here, the promoter region of the hmgb1 gene at position (-183 to -165) from the transcription start site as a target was selected using bioinformatic tools. Methods: The DNA triplex formation by the DNA of the target gene and TFO was confirmed using UV absorption spectroscopy, Circular Dichroism, and Isothermal Calorimetry. Results: Treatment of HepG2 cell with specific Triplex-forming Oligonucleotide significantly downregulated HMGB1 expression level at mRNA and protein levels by 50%, while the classical anticancer drugs, actinomycin/ adriamycin as positive controls showed 65% and the combination of TFO and drug decreased by 70%. The anti-proliferative effects of TFO correlated well with the fact of accumulation of cells in the Go phase and apoptotic cell death. Further, the binding of anti-cancer drugs to hmgb1 is stronger in DNA triplex state as compared to hmgb1 alone, suggesting the combination therapy as a better option. Conclusion: Therefore, the ability of hmgb1 targeted triplex-forming oligonucleotide in combination with triplex selective anticancer drug holds promise in the treatment of malignancies associated with hmgb1 overexpression. The result obtained may open up new vistas to provide a basis for the rational drug design and searching for high-affinity ligands with a high triplex selectivity.

Synthesis and conformational studies on 1-aryl-cis-2,6-diphenylpiperidines

2021 ◽  
Vol 1232 ◽  
pp. 130065
Author(s):  
H. Surya Prakash Rao ◽  
E. Poonguzhali ◽  
Jayaraman Muthukumaran
Keyword(s):  
Conformational Studies

Conformational studies by dynamic NMR. IX. Activation parameters for the barrier to C-N rotation in N,N-dimethylbenzamidine : a correction

1977 ◽  
Vol 18 (12) ◽  
pp. 1079-1080 ◽  
Author(s):  
Lodovico Lunazzi ◽  
Alessandro Dondoni ◽  
Gaetano Barbaro ◽  
Dante Macciantelli
Keyword(s):  
Activation Parameters ◽  
Dynamic Nmr ◽  
Conformational Studies
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