ABSTRACT: Globally, two billion people suffer from micronutrient deficiencies. Cereal grains provide more than 50% of the daily requirement of calories in human diets, but they often fail to provide adequate essential minerals and vitamins. Cereal crop production in developing countries achieved remarkable yield gains through the efforts of the Green Revolution (117% in rice, 30% in wheat, 530% in maize, and 188% in pearl millet). However, modern varieties are often deficient in essential micronutrients compared to traditional varieties and land races. Breeding for nutritional quality in staple cereals is a challenging task; however, biofortification initiatives combined with genomic tools increase the feasibility. Current biofortification breeding activities include improving rice (for zinc), wheat (for zinc), maize (for provitamin A), and pearl millet (for iron and zinc). Biofortification is a sustainable approach to enrich staple cereals with provitamin A, carotenoids, and folates. Significant genetic variation has been found for provitamin A (96–850 ?g and 12–1780 ?g in 100 g in wheat and maize, respectively), carotenoids (558–6730 ?g in maize), and folates in rice (11–51 ?g) and wheat (32.3–89.1 ?g) in 100 g. This indicates the prospects for biofortification breeding. Several QTLs associated with carotenoids and folates have been identified in major cereals, and the most promising of these are presented here. Breeding for essential nutrition should be a core objective of next-generation crop breeding. This review synthesizes the available literature on folates, provitamin A, and carotenoids in rice, wheat, maize, and pearl millet, including genetic variation, trait discovery, QTL identification, gene introgressions, and the strategy of genomics-assisted biofortification for these traits. Recent evidence shows that genomics-assisted breeding for grain nutrition in rice, wheat, maize, and pearl millet crops have good potential to aid in the alleviation of micronutrient malnutrition in many developing countries.