In the following work a new metal-complex activated mode of action for G Protein Coupled Receptors is presented.   Luteinizing hormone receptors (LHR), expressed in physiological numbers less than 30,000 receptors per cell, translocate to and signal within membrane rafts following binding of juman chorionic gonadotropin (hCG). Similarly LHR signal in cells when treated with bis(maltolato)oxovanadium(IV) (BMOV), bis(ethylmaltolato)oxovanadium(IV) (BEOV), VOSO4, or some other vanadium compounds which decrease membrane lipid packing.  Overexpressed LHR (&gt;85,000 recetros per cell) are found in larger clusters in polarized homo-transferfluorescence resonance energy transfer (home-FRET) studies that were not affected by either hCG or vanadium compounds.  Intracellular cyclic adenylate monophosphate (cAMP) levels indicate that only clustered LHR are active and producethe intracellular second messenger, cAMP.  When LHR are over-expressed, cell signaling in unaffected by binding of hCG or vanadium compounds.  To confirm the existence of intact complex, the EPR soectra of vanadium compounds in cell media were obtained using 1 mM BMOV, BEOV or VOSO4.  These data were used to determine the intact complex in a solution to verify the speciation calculations.  Effects of BMOV and BEOV were about two-fold greater than solutions prepared from VOSO<sub>4</sub>. Studies exploring these and other vanadium compounds as well as other metal compound are explored and our progress reported.

Vanadium compounds cause activation of G protein-coupled receptor signaling

ACS Fall 2020 Virtual Meeting

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