发明授权
US07238682B1 Methods and compositions for degradation and/or inhibition of HER-family tyrosine kinases 有权
用于降解和/或抑制HER-家族酪氨酸激酶的方法和组合物

Methods and compositions for degradation and/or inhibition of HER-family tyrosine kinases
摘要:
Bifunctional molecules comprising two hsp-binding moieties which bind to hsp90 in the pocket to which ansamycin antibiotics bind connected via a linker are effective for inducing the degradation and/or inhibition of HER-family tyrosine kinases. For example, a compound of two geldanamycin moities joined by a four-carbon linker provides selective degradation of HER-family tyrosine kinases, without substantially affecting other kinases. These compounds can be used for treatment of HER-positive cancers with reduced toxicity, since these compounds potently kill cancer cells but affect fewer proteins than geldanamycin.
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