22 research outputs found
Low‐molecular mimetics of nerve growth factor and brain‐derived neurotrophic factor: Design and pharmacological properties
Bivalent Peptidomimetic Ligands of TrkC Are Biased Agonists and Selectively Induce Neuritogenesis or Potentiate Neurotrophin-3 Trophic Signals
Cyclic-AMP Response Element-Based Signaling Assays for Characterization of Trk Family Tyrosine Kinases Modulators
A role for transferrin receptor in triggering apoptosis when targeted with gambogic acid
Transferrin receptor (TfR) has been shown to be significantly overexpressed in different types of cancers. We discovered TfR as a target for gambogic acid (GA), used in traditional Chinese medicine and a previously undiscovered link between TfR and the rapid activation of apoptosis. The binding site of GA on TfR is independent of the transferrin binding site, and it appears that GA potentially inhibits TfR internalization. Down-regulation of TfR by RNA interference decreases sensitivity to GA-induced apoptosis, further supporting TfR as the primary GA receptor. In summary, GA binding to TfR induces a unique signal leading to rapid apoptosis of tumor cells. These results suggest that GA may provide an additional approach for targeting the TfR and its use in cancer therapy