Mercapturic acids are conjugates of S-(N-acetyl)-L-cysteine formed during the detoxification of xenobiotics and during the metabolism of such endogenous agents as estrogens and leukotrienes. Many mercaturates are formed from the corresponding glutathione S-conjugates. This chapter focuses on (a) the discovery of the cysteine S-conjugate beta-lyases; (b) the involvement of pyridoxal-5-phosphate; (c) the influence of the electron-withdrawing properties of the group attached to the sulfur atom; and (d) the potential of cysteine S-conjugates as pro-drugs.