'glyoxalase-activating' is a compound formed from 'glyoxalase' + 'activating'. 'glyoxalase' originates from the chemical name 'glyoxal' plus the enzyme-forming suffix '-ase'; 'glyoxal' derives ultimately from Greek elements meaning 'sweet' ('glyk-') and 'sharp/acid' ('ox-'), and '-ase' was coined as an enzyme suffix in the 19th century.

'glyoxal' appeared in chemical nomenclature in the 19th century (from 'glyoxylic'), then the enzyme name 'glyoxalase' was formed by adding the modern enzymatic suffix '-ase'; later, English productivity produced the compound adjectival/participle form 'glyoxalase-activating' by combining that enzyme name with the present-participle form of 'activate'.

Originally the elements referred to a specific chemical ('glyoxal') and a general enzyme suffix ('-ase'); over time they combined into the technical enzyme name 'glyoxalase', and the extended form now specifically denotes something that activates that enzyme ('glyoxalase-activating').