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Discovery and Preclinical Pharmacology of NX-2127, an Orally Bioavailable Degrader of Bruton’s Tyrosine Kinase with Immunomodulatory Activity for the Treatment of Patients with B Cell Malignancies
Bruton’s tyrosine kinase (BTK), a member of the TEC kinase family, is a key component of B-cell receptor (BCR) signaling, which controls B cell development, activation, and survival. Loss-of-function mutations in BTK lead to X-linked agammaglobulinemia, an inherited disorder characterized by an inability to produce antibodies due to defective B cell development. (1) Src kinases activate BTK via phosphorylation, thereby leading to subsequent phosphorylation of phospholipase C gamma (PLC-γ).
Discovery and Preclinical Pharmacology of NX-2127, an Orally Bioavailable Degrader of Bruton’s Tyrosine Kinase with Immunomodulatory Activity for the Treatment of Patients with B Cell Malignancies
Bruton’s tyrosine kinase (BTK), a member of the TEC kinase family, is a key component of B-cell receptor (BCR) signaling, which controls B cell development, activation, and survival. Loss-of-function mutations in BTK lead to X-linked agammaglobulinemia, an inherited disorder characterized by an inability to produce antibodies due to defective B cell development. (1) Src kinases activate BTK via phosphorylation, thereby leading to subsequent phosphorylation of phospholipase C gamma (PLC-γ).
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