Molecular Modeling, Total Synthesis, and Biological Evaluations of C9-Deoxy Bryostatin 1

2010 ◽  
Vol 122 (27) ◽  
pp. 4684-4688 ◽  
Author(s):  
Gary E. Keck ◽  
Yam B. Poudel ◽  
Arnab Rudra ◽  
Jeffrey C. Stephens ◽  
Noemi Kedei ◽  
...  
Keyword(s):  
Molecular Modeling ◽  
Total Synthesis ◽  
Bryostatin 1

scholarly journals Molecular Modeling, Total Synthesis, and Biological Evaluations of C9-Deoxy Bryostatin 1

2010 ◽  
Vol 49 (27) ◽  
pp. 4580-4584 ◽  
Author(s):  
Gary E. Keck ◽  
Yam B. Poudel ◽  
Arnab Rudra ◽  
Jeffrey C. Stephens ◽  
Noemi Kedei ◽  
...  
Keyword(s):  
Molecular Modeling ◽  
Total Synthesis ◽  
Bryostatin 1

ChemInform Abstract: Total Synthesis of Bryostatin 1: A Short Route

ChemInform ◽  
2012 ◽  
Vol 43 (5) ◽  
pp. no-no
Author(s):  
Soraya Manaviazar ◽  
Karl J. Hale
Keyword(s):  
Total Synthesis ◽  
Bryostatin 1 ◽  
Short Route

Total Synthesis of Bryostatin 1: A Short Route

2011 ◽  
Vol 50 (38) ◽  
pp. 8786-8789 ◽  
Author(s):  
Soraya Manaviazar ◽  
Karl J. Hale
Keyword(s):  
Total Synthesis ◽  
Bryostatin 1 ◽  
Short Route

scholarly journals Evaluation of Toxic Amyloid β42 Oligomers in Rat Primary Cerebral Cortex Cells and Human iPS-derived Neurons Treated with 10-Me-Aplog-1, a New PKC Activator

2020 ◽  
Vol 21 (4) ◽  
pp. 1179
Author(s):  
Kazuma Murakami ◽  
Mayuko Yoshimura ◽  
Shota Nakagawa ◽  
Toshiaki Kume ◽  
Takayuki Kondo ◽  
...  
Keyword(s):  
Cerebral Cortex ◽  
Total Synthesis ◽  
Bryostatin 1 ◽  
Oligomer Formation ◽  
Promising Strategy ◽  
Secretase Activity ◽  
Drug Lead ◽  
Protein Kinase Cα ◽  
Aβ Production ◽  
Ad Therapy

Amyloid β42 (Aβ42), a causative agent of Alzheimer’s disease (AD), is derived extracellularly from Aβ precursor protein (APP) following the latter’s cleavage by β-secretase, but not α-secretase. Protein kinase Cα (PKCα) activation is known to increase α-secretase activity, thereby suppressing Aβ production. Since Aβ42 oligomer formation causes potent neurotoxicity, APP modulation by PKC ligands is a promising strategy for AD treatment. Although bryostatin-1 (bryo-1) is a leading compound for this strategy, its limited natural availability and the difficulty of its total synthesis impedes further research. To address this limitation, Irie and colleagues have developed a new PKC activator with few side effects, 10-Me-Aplog-1, (1), which decreased Aβ42 in the conditioned medium of rat primary cerebral cortex cells. These results are associated with increased α-secretase but not PKCε-dependent Aβ-degrading enzyme. The amount of neuronal embryonic lethal abnormal vision (nELAV), a known β-secretase stabilizer, was reduced by treatment with 1. Notably, 1 prevented the formation of intracellular toxic oligomers. Furthermore, 1 suppressed toxic oligomerization within human iPS-derived neurons such as bryo-1. Given that 1 was not neurotoxic toward either cell line, these findings suggest that 1 is a potential drug lead for AD therapy.

scholarly journals Total Synthesis of Bryostatin 1

2011 ◽  
Vol 133 (4) ◽  
pp. 744-747 ◽  
Author(s):  
Gary E. Keck ◽  
Yam B. Poudel ◽  
Thomas J. Cummins ◽  
Arnab Rudra ◽  
Jonathan A. Covel
Keyword(s):  
Total Synthesis ◽  
Bryostatin 1
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