In this review, we focus on four key metabolic GPCRs—GPR40, GPR120, GLP-1R, and β-adrenergic receptors (ADRB1, ADRB2, and ADRB3)—with respect to their roles in metabolic physiology and significance in obesity and related metabolic diseases (Figure 1). The gene discussed is GLP1R; the disease is metabolic disease.