ErbB family

Denny WA. Irreversible inhibitors of the erbB family of protein tyrosine kinases. Pharmacol Ther 2002 93 253-61. 

Conceivably, lessons learned in yeast on internalization of membrane proteins are relevant to both the constitutive and the inducible pathways of receptor endocytosis in mammals. The constitutive pathway is the least understood, and it may bypass a requirement for ubiquitination by utilizing intrinsic di-leucine and other signals for protein internalization (Covers et al. 1998). In the ErbB family, the pathway may be exemplified by the relatively slow internalization rate of mutant RTKs, either the kinase- defective ErbB-3 (Baulida et al. 1996 Baulida and Carpenter 1997 Waterman et al. 1998), or artificial kinase-defective mutants (Chen et al. 1989 Felder et al. 1990). 

Selective Inhibitors Targeting Individual ErbB Family Members. 96... 

AEE788 is the second pyrrolopyrimidine inhibitor of the ErbB family that Novartis has progressed into the clinic. The first one was PKI166, which was discontinued due to elevated, but reversible, liver enzyme levels (17% of patients experienced grade 3 levels of elevated transaminases) [96]. In AEE788, the phenol of PKI166 is replaced with a methylene-linked N-ethylpiperazine moiety that may have been designed in an effort to increase solubility and de-... 

Rao GS, Murray S, Ethier SP. Radiosensitization of human breast cancer cells by a novel ErbB family receptor tyrosine kinase inhibitor. Int J Radiat Oncol Biol Phys 2000 48(5) 1519-1528. 

The epidermal growth factor receptor (EGFR) is a receptor tyrosine kinase (RTK) with pleiotropic developmental functions in metazoans. It is the prototypical member of the ErbB family of RTKs, which can form homodimers or heterodimers with other... 

ErbB family members upon ligation with a variety of EGF-related extraeellular ligands to faeilitate transphosphorylation and downstream signaling. 

Ito, Y., Takeda, T., Sasaki, Y., Sakon, M., Yamada, T., Ishiguro, S., Imaoka, S., Tsujimoto, M., Higashiyama, S., Monden, M., and Matsuura, N. 2001. Expression and clinical significance of the erbB family in intrahepatic cholangiocellular carcinoma. Pathol. Res. Pract. 197 95-100. 

Chang H, Riese DJ II, Gilbert W, Stern DF, McMahan UJ. 1997. Ligands for ErbB-family receptors encoded by a neuregulin-like gene. Nature 387 509-512. 

Hobbs SS, Coffing SL, Le AT, Cameron EM, Williams EE, et al. 2002. Neuregulin isoforms exhibit distinct patterns of ErbB family receptor activation. Oncogene 21 8442-8452. 

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