66389-80-8Relevant articles and documents
Cyanine compound containing tetrazine unit and preparation method and application thereof
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Paragraph 0022; 0032-0033, (2021/06/09)
The invention provides a cyanine compound containing a tetrazine unit, a preparation method of the cyanine compound and application of the cyanine compound to near-infrared fluorescence labeling of tumor cells by utilizing a biological orthogonal reaction
Selective CRAF Inhibition Elicits Transactivation
Morgan, Charles W.,Dale, Ian L.,Thomas, Andrew P.,Hunt, James,Chin, Jason W.
supporting information, p. 4600 - 4606 (2021/05/04)
Discovering molecules that regulate closely related protein isoforms is challenging, and in many cases the consequences of isoform-specific pharmacological regulation remains unknown. RAF isoforms are commonly mutated oncogenes that serve as effector kinases in MAP kinase signaling. BRAF/CRAF heterodimers are believed to be the primary RAF signaling species, and many RAF inhibitors lead to a "paradoxical activation"of RAF kinase activity through transactivation of the CRAF protomer; this leads to resistance mechanisms and secondary tumors. It has been hypothesized that CRAF-selective inhibition might bypass paradoxical activation, but no CRAF-selective inhibitor has been reported and the consequences of pharmacologically inhibiting CRAF have remained unknown. Here, we use bio-orthogonal ligand tethering (BOLT) to selectively target inhibitors to CRAF. Our results suggest that selective CRAF inhibition promotes paradoxical activation and exemplify how BOLT may be used to triage potential targets for drug discovery before any target-selective small molecules are known.
Inverse Electron-Demand Diels-Alder Bioconjugation Reactions Using 7-Oxanorbornenes as Dienophiles
Agramunt, Jordi,Ginesi, Rebecca,Grandas, Anna,Pedroso, Enrique
, p. 6593 - 6604 (2020/07/14)
Oligonucleotides, peptides, and peptide nucleic acids incorporating 7-oxanorbornene as a dienophile were reacted with tetrazines linked to either a peptide, d-biotin, BODIPY, or N-acetyl-d-galactosamine. The inverse electron-demand Diels-Alder (IEDDA) cycloaddition, which was performed overnight at 37 °C, in all cases furnished the target conjugate in good yields. IEDDA reactions with 7-oxanorbornenes produce a lower number of stereoisomers than that of IEDDA cycloadditions with other dienophiles.