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Chemistry and biology of the aeruginosin family of serine protease inhibitors.
TLDR
The first comprehensive review on the chemistry and biology of the aeruginosins is provided, with an emphasis on their sources, structural revisions, and total syntheses.
Inhibition of ER stress-associated IRE-1/XBP-1 pathway reduces leukemic cell survival.
TLDR
Data indicate that targeting XBP-1 has potential as a treatment strategy, not only for multiple myeloma, but also for mature B cell leukemia and lymphoma.
Regulated IRE1-dependent mRNA decay sets the threshold for dendritic cell survival
TLDR
Mulosal DCs differentially mount ATF4- and IRE1-dependent adaptive mechanisms to survive in the face of ER stress, and loss of IRE2 endonuclease on top of XBP1 led to cDC1 loss in the intestine.
Overexpression of TCL1 activates the endoplasmic reticulum stress response: a novel mechanism of leukemic progression in mice.
TLDR
It is shown for the first time that the previously unexplored endoplasmic reticulum (ER) stress response is aberrantly activated in Eμ-TCL1 mouse and human CLL, and the ER stress-response pathway is a novel molecular target for the treatment of CLL.
Agonist-Mediated Activation of STING Induces Apoptosis in Malignant B Cells.
TLDR
It is shown that the IRE-1/XBP-1 pathway functions downstream of STING and that STING agonists selectively trigger mitochondria-mediated apoptosis in normal and malignant B cells, implying that prolonged activation of STing can lead to apoptosis.
IRE1&agr; RNase–dependent lipid homeostasis promotes survival in Myc-transformed cancers
TLDR
It is shown that Myc overexpression induces endoplasmic reticulum (ER) stress and engages the inositol-requiring enzyme 1&agr;/X-box binding protein 1 (XBP1) pathway through multiple molecular mechanisms in a variety of c-Myc– and N- myc–dependent cancers.
Phosphorylation of IRE1 at S729 regulates RIDD in B cells and antibody production after immunization
TLDR
S729 is critically important for lipopolysaccharide-stimulated plasmablasts to respond to additional ER stress and for antibody production in response to immunization and a critical role for S729 in regulating RIDD in B cells is discovered.
Synthesis of enantiopure ε-oxapipecolic acid.
TLDR
The enantiopure building block was employed in the synthesis of a short model peptide to determine the amide rotamer preference N-terminal to the cyclic residue, exerting a strong trans substantiating effect through lone pair repulsion in oxapipecolic acid.
Total synthesis and structural confirmation of chlorodysinosin A.
TLDR
The first enantiocontrolled total synthesis of the marine sponge metabolite chlorodysinosin A is described, which is the most potent inhibitor of the serine proteases thrombin, factor VIIa, and factor Xa, which are critical enzymes in the process leading to platelet aggregation and fibrin mesh formation in humans.
Synthetic studies in the intramolecular carbocyclization of N-acyloxyiminium ions. Stereoelectronic and steric implications of nucleophilic alkene, alkyne, and allene tethers.
TLDR
Reactions of alkenes and alkynes with terminal alkyl or aryl substituents, as well as allenes, proceed through transient vinylic carbocations that are attacked internally by the N-Boc group to give tricyclic dihydrooxazinones.
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