Advances in Small-Molecule Dual Inhibitors Targeting EGFR and HER2 Receptors as Anti-Cancer Agents.

As members of the protein tyrosine kinase family, the Epidermal Growth Factor Receptor (EGFR) and Human Epidermal Growth Factor Receptor 2 (HER2) play essential roles in cellular signal transduction pathways. Overexpression or abnormal activation of EGFR and HER2 can lead to the development of various solid tumors. Therefore, they have been confirmed as biological targets for the development of anticancer drugs. Due to the fact that many cancers are highly susceptible to developing resistance to single-target EGFR inhibitors in clinical practice, dual inhibitors that target both EGFR and HER2 have been developed to increase efficacy, reduce drug resistance and interactions, and improve patient compliance. Currently, a variety of EGFR/HER2 dual inhibitors have been developed, with several drugs already approved for marketing or in clinical trials. In this review, we summarize recent advancements in small-molecule EGFR/HER2 dual inhibitors by focusing on structure-activity relationships and share novel insights into developing anticancer agents.

Effect of three different proteases on horsemeat tenderness during postmortem aging.

In this study, the semitendinosus of horse meat was used as the raw material. The study assessed the variation of the tenderness of horse meat during postmortem aging through the injection of papain, bromelain and fungal protease. The cooking loss of the horse meat became worse during postmortem aging. Low concentration of protease improved water retention properties of horse meat. Papain, bromelain and fungal protease had significant influence on MFI and shear force. MFI increased obviously but the shear force decreased significantly with the addition of more protease (p <0.05). During postmortem aging, many small molecules popeptide appeared in treatment group. Myosin light chain 2, 20 KDa, 32 KDa and 75 KDa bands appeared at first, however later they disappeared in the group with high concentration of protease treatment in addition to the disappearance of Desmin and Troponin I. The muscle fiber, perimysium and endomysium were degraded because of papain, bromelain and fungal protease treatment. More muscle fiber fragments appeared during postmortem aging.Thus, the tenderness and eating quality of horse meat were improved by adding three kinds of protease.