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Discovery of Type II Inhibitors of TGFβ-Activated Kinase 1 (TAK1) and Mitogen-Activated Protein Kinase Kinase Kinase Kinase 2 (MAP4K2)
TLDR
A pharmacophore model for type II inhibitors was developed that was used to guide the construction of a library of kinase inhibitors that exhibited potent inhibitory activity against two mitogen-activated protein kinases, TAK1 and MAP4K2, as well as pharmacologically well interrogated kinases such as p38α (MAPK14) and ABL.
Synergistic interactions with PI3K inhibition that induce apoptosis
TLDR
This work identified 5 genes (PIM2, ZAK, TACC1, ZFR, ZNF565) whose suppression induced cell death upon PI3K inhibition and showed that small molecule inhibitors of the PIM2 and ZAK kinases synergize with PI3k inhibition.
Synthesis and anti-tumor activity of imidazopyrazines as TAK1 inhibitors.
Synthesis and evaluation of thieno[3,2-d]pyrimidine derivatives as novel FMS inhibitors.
Novel Macrocyclic Peptidomimetics Targeting the Polo-Box Domain of Polo-Like Kinase 1.
TLDR
Novel phosphorylated macrocyclic peptidomimetics targeting PBD based on acyclic phosphopeptide PMQSpTPL are designed and synthesized and should serve as valuable templates for the design of potent and novel Plk1-PBD inhibitors.
Studies on the Total Synthesis of Amphidinolide O. A Stereoselective Synthesis of C3—C11 Fragment.
TLDR
The retrosynthetic analysis of amphidinolide O led to the C1-C11 fragment 2 and C12 C17 fragment 3 through cleavage of C2-O and C11-C12 bond as proposed in the paper as well as the diastereoselective synthesis of the other C3-C 11 fragment 20 of amphide O.
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