Grains including wheat, brown rice, millet, oat, and seeds from crops such as pumpkins, almonds, cashew, peas are important staple foods in many parts of the world. Grains and seeds contain proteins and bioactive peptides classified as nutraceuticals. Proteins and peptides are essential components in man’s diet because they provide the raw materials needed for protein biosynthesis and are also a good source of energy. Incorporating grains and seeds into the human diet provide nutritional, functional health benefits, reducing contracting some chronic diseases. They avail the body with a balanced nutrient profile such as carbohydrate, fatty-acid, fibre, B vitamins, minerals and protein. The quest at exploring staples for their functional and health benefits, as well as reducing risks to diseases, has resulted in the investigation of the potentials of grains and seeds, especially the underutilised ones (African yam bean, pigeon pea, Bambara groundnut etc.) for consumption and as an alternative therapy against diseases. This chapter discusses grains and seeds as sources of nutrition protagonist, their nutritive property, health benefits, and the pharmacological properties of bioactive peptides in grains and seeds. However, some under-utilised grain and seed proteins would also be explored for their nutritive potentials.