Enzymatic Synthesis of 3′–5′, 3′–5′ Cyclic Dinucleotides, Their Binding Properties to the Stimulator of Interferon Genes Adaptor Protein, and Structure/Activity Correlations

Biochemistry ◽  
2021 ◽  
Author(s):  
Barbora Novotná ◽  
Lucie Holá ◽  
Monika Staś ◽  
Ondrej Gutten ◽  
Miroslav Smola ◽  
...  
Keyword(s):  
Enzymatic Synthesis ◽  
Adaptor Protein ◽  
Binding Properties ◽  
Structure Activity ◽  
Cyclic Dinucleotides

Quantifying Target Occupancy of Small Molecules Within Living Cells

2020 ◽  
Vol 89 (1) ◽  
pp. 557-581 ◽  
Author(s):  
M.B. Robers ◽  
R. Friedman-Ohana ◽  
K.V.M. Huber ◽  
L. Kilpatrick ◽  
J.D. Vasta ◽  
...  
Keyword(s):  
Cultured Cells ◽  
Drug Efficacy ◽  
Living Cells ◽  
Drug Binding ◽  
Therapeutic Window ◽  
Target Engagement ◽  
Binding Properties ◽  
Structure Activity ◽  
Sar Analysis ◽  
Kinetics Of

The binding affinity and kinetics of target engagement are fundamental to establishing structure–activity relationships (SARs) for prospective therapeutic agents. Enhancing these binding parameters for operative targets, while minimizing binding to off-target sites, can translate to improved drug efficacy and a widened therapeutic window. Compound activity is typically assessed through modulation of an observed phenotype in cultured cells. Quantifying the corresponding binding properties under common cellular conditions can provide more meaningful interpretation of the cellular SAR analysis. Consequently, methods for assessing drug binding in living cells have advanced and are now integral to medicinal chemistry workflows. In this review, we survey key technological advancements that support quantitative assessments of target occupancy in cultured cells, emphasizing generalizable methodologies able to deliver analytical precision that heretofore required reductionist biochemical approaches.

scholarly journals Tunable Enzymatic Synthesis of the Immunomodulator Lipid IVATo Enable Structure–Activity Analysis

2019 ◽  
Vol 141 (24) ◽  
pp. 9474-9478 ◽  
Author(s):  
Karthik Sankaranarayanan ◽  
Xirui X. Antaris ◽  
Brad A. Palanski ◽  
Abrahim El Gamal ◽  
Camilla M. Kao ◽  
...  
Keyword(s):  
Enzymatic Synthesis ◽  
Activity Analysis ◽  
Structure Activity

Chemo-enzymatic synthesis and structure-activity study of artificially N-glycosylated eel calcitonin derivatives with a complex type oligosaccharide

2004 ◽  
Vol 21 (6) ◽  
pp. 377-386 ◽  
Author(s):  
Katsuji Haneda ◽  
Mizuka Tagashira ◽  
Eiichi Yoshino ◽  
Midori Takeuchi ◽  
Toshiyuki Inazu ◽  
...  
Keyword(s):  
Enzymatic Synthesis ◽  
Complex Type ◽  
Structure Activity
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