[HTML][HTML] Structure and chemical inhibition of the RET tyrosine kinase domain
The RET proto-oncogene encodes a receptor tyrosine kinase for the glial cell line-derived
neurotrophic factor family of ligands. Loss-of-function mutations in RET are implicated in
Hirschsprung disease, whereas activating mutations in RET are found in human cancers,
including familial medullar thyroid carcinoma and multiple endocrine neoplasias 2A and 2B.
We report here the biochemical characterization of the human RET tyrosine kinase domain
and the structure determination of the non-phosphorylated and phosphorylated forms. Both …
neurotrophic factor family of ligands. Loss-of-function mutations in RET are implicated in
Hirschsprung disease, whereas activating mutations in RET are found in human cancers,
including familial medullar thyroid carcinoma and multiple endocrine neoplasias 2A and 2B.
We report here the biochemical characterization of the human RET tyrosine kinase domain
and the structure determination of the non-phosphorylated and phosphorylated forms. Both …