To sum up, we generated a versatile library of fully synthetic disaccharide lipid A mimetics (DLAMs), embracing potent TLR4 antagonists with nanomolar affinity for MD-2 and powerful TLR4 agonists with picomolar affinity for TLR4/MD-2 as potential anti-inflammatory drug candidates for sepsis, acute and chronic inflammation as well as unique TLR4-activating immunomodulators with broad therapeutic potential for cancer and prophylactic capacity as vaccine adjuvants. The gene discussed is TLR4; the disease is cancer.