- Synthesis and calcium mobilization activity of cADPR analogues which integrate nucleobase, northern and southern ribose modifications
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Novel cADPR mimics, which integrate nucleobase, northern and southern ribose modifications were synthesized. The key steps of the synthesis were a Cu(I)-catalyzed Hueisgen [3+2] cycloaddition and a microwave-assisted intramolecular pyrophosphorylation. Preliminary biological investigations showed that these cADPR mimics are membrane-permeating agonists of the calcium signaling pathway. The introduction of chlorine or fluorine at the 2'-position of the southern riboses led to a decrease of activity. The existence of a hydrophobic group on the 3'-OH of the southern riboses does not obviously alter the agonistic activity.
- Zhou, Yue,Yu, Peilin,Jin, Hongwei,Yang, Zhenjun,Yue, Jianbo,Zhang, Liangren,Zhang, Lihe
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- SITE-SPECIFIC ANTIBODY-DRUG CONJUGATES BY ADP-RIBOSYL CYCLASES
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Antibody-drug conjugates, compositions thereof, and methods use. The antibody-drug conjugates include a fusion protein comprising an antibody covalently linked to an ADP-ribosyl cyclase protein via a peptide linker moiety at one or more of a C-terminus or N-terminus of a heavy or light chain of the antibody, a NAD or NMN analogue, and a payload such that the NAD or NMN analogue is conjugated to both the payload and the ADP-ribosyl cyclase protein.
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- Isolation, synthesis, and characterization of impurities and degradants from the clofarabine process
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The identification of clofarabine process impurities and their subsequent isolation, synthesis, and characterization is described. Two isomeric process impurities resulting from N6-attachment of a fluoroarabinose to clofarabine were found. Clofarabine's base degradation products, which were different from the process impurities, were also synthesized and characterized. These compounds resulted from modifications to the sugar moiety, the purine ring, or both. A mechanistic rationale for the formation of the various process impurities and degradation products is provided.
- Anderson, Bruce G.,Bauta, William E.,Cantrell Jr., William R.,Engles, Tracy,Lovett, Dennis P.
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p. 1229 - 1237
(2013/01/03)
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