This review provides an overview of glycation, its molecular mechanisms, impact on proteins, pathogenesis, and inhibition. Glycation is a non-enzymatic process where reducing sugars or their autoxidation products react with amino groups of proteins, DNA, or lipids, leading to the formation of advanced glycation end-products (AGEs). These AGEs can alter the biological function of biomacromolecules and contribute to the development of various diseases, including diabetes-related conditions, obesity, and chronic renal failure. The review discusses the similarities and differences between glycation and glycosylation, the molecular mechanisms underlying glycation reactions, and the bio-molecular targets most susceptible to glycation. It also explores the effects of glycation on protein structure, function, and aggregation, and how computational chemistry provides insights into these aspects. The review highlights the most prevalent diseases associated with glycation and the endogenous mechanisms and current therapeutic interventions aimed at combating it. It also discusses the role of glycation in protein aggregation and the protective mechanisms evolved by cells to prevent it. The review emphasizes the importance of understanding glycation in the context of disease pathogenesis and the need for further research to develop effective therapeutic strategies.This review provides an overview of glycation, its molecular mechanisms, impact on proteins, pathogenesis, and inhibition. Glycation is a non-enzymatic process where reducing sugars or their autoxidation products react with amino groups of proteins, DNA, or lipids, leading to the formation of advanced glycation end-products (AGEs). These AGEs can alter the biological function of biomacromolecules and contribute to the development of various diseases, including diabetes-related conditions, obesity, and chronic renal failure. The review discusses the similarities and differences between glycation and glycosylation, the molecular mechanisms underlying glycation reactions, and the bio-molecular targets most susceptible to glycation. It also explores the effects of glycation on protein structure, function, and aggregation, and how computational chemistry provides insights into these aspects. The review highlights the most prevalent diseases associated with glycation and the endogenous mechanisms and current therapeutic interventions aimed at combating it. It also discusses the role of glycation in protein aggregation and the protective mechanisms evolved by cells to prevent it. The review emphasizes the importance of understanding glycation in the context of disease pathogenesis and the need for further research to develop effective therapeutic strategies.