Recent progress and advanced technology in carbohydrate-based drug development.

[Display omitted] • A brief overview of CBD development in recent decades is presented. • Approaches for accessing specific carbohydrates and glycoconjugates are clarified. • Microarray and library are critical for rapid screening of bioactive carbohydrates. • Gut microbiota system is promising for evaluation of orally administrated CBD. • Advanced technologies and toolkit accelerated the CBD discovery. Carbohydrates, one of the most abundant and widespread biomolecules in nature, play indispensable roles in diverse biological functions, and represent a treasure trove of untapped potential for pharmaceutical applications. Here, we provide a brief overview of carbohydrate-based drug development (CBDD) over the past two decades. More importantly, advanced techniques and methodologies related to CBDD are emerging, including enzymatic synthesis, metabolic engineering, site-specific glycoconjugation, carbohydrate libraries and microarrays as well as carbohydrate-gut microbiome evaluation. These technologies have dramatically accelerated the speed of CBDD. The recently approved drugs and emerging techniques summarized herein will inspire new sights into potential opportunities to discover novel carbohydrate drugs. [ABSTRACT FROM AUTHOR]