The first synthetic Hsp90 inhibitor to enter clinic is CNF2024/BIIB021, an Hsp90 inhibitor developed initially by Conforma Therapeutics (currently Biogen Idec) based on the purine-scaffold discovered by investigators at Memorial Sloan-Kettering Cancer Center through structure-based design (Figure 1) [24]
The first synthetic Hsp90 inhibitor to enter clinic is CNF2024/BIIB021, an Hsp90 inhibitor developed initially by Conforma Therapeutics (currently Biogen Idec) based on the purine-scaffold discovered by investigators at Memorial Sloan-Kettering Cancer Center through structure-based design (Figure 1) [24]. regulated by the binding of the Hsp90 machinery. These include BCR-ABL in the chronic myelogenous leukemia (CML) [3], nucleophosmin-anaplastic lymphoma kinase (NPMCALK) in lymphomas [4], mutated FLT3 in acute myeloid leukemia [5], EGFR harboring kinase mutations in nonsmall cell lung malignancy (NSCLC) [6], the zeta-associated protein of 70 kDa (ZAP-70) as Mouse monoclonal to CD21.transduction complex containing CD19, CD81and other molecules as regulator of complement activation expressed in patients with aggressive chronic lymphocytic leukemia (CLL) [7], mutant B-Raf in melanoma [8], human epidermal growth factor receptor 2 (HER2) in HER2-overexpressing breast malignancy [9], mutant c-Kit in gastrointestinal stromal tumors (GIST) [10], and activated Akt in small cell lung carcinoma [11], to…