10.6084/m9.figshare.5120959.v1
Hoettecke N.
Hoettecke
N.
Ludwig A.
Ludwig
A.
Foro S.
Foro
S.
Schmidt B.
Schmidt
B.
Supplementary Material for: Improved Synthesis of ADAM10 Inhibitor GI254023X
Karger Publishers
2010
Metalloproteinase
ADAM10
ADAM17
Neurodegenerative disease
Inflammation
Cancer
2010-02-27 00:00:00
Dataset
https://karger.figshare.com/articles/dataset/Supplementary_Material_for_Improved_Synthesis_of_ADAM10_Inhibitor_GI254023X/5120959
<i>Background:</i> The metalloproteinases ADAM10 and ADAM17 are involved in various diseases: neurodegeneration, cancer and inflammation. <i>Objective:</i> The inhibition of these proteases is a promising target in the treatment of inflammation and cancer. <i>Methods and Results:</i> In this study, we present an improved synthesis of the ADAM10 reference inhibitor GI254023X with a higher overall yield, enhanced detection ability and increased acid stability, providing easier handling. <i>Conclusion:</i> This upscaled synthesis, free of diastereomeric intermediates, ensures single-batch identity, thus warranting its reproducibility in further biological investigations.