Diversity-oriented optical imaging probe development

The development of optical probes is receiving considerable attention due to their rising adaptation in diagnostics and medical imaging. Diversity-oriented approaches make use of combinatorial chemistry and high-throughput screenings to enrich the spectral and structural variety of these probes and effectively identify those with specific properties (e.g. molecular affinity, cellular selectivity, high photostability, and sensitivity). Herein we review recent examples in which diversity-driven strategies have assisted the discovery of new molecular imaging probes.

► Diversity generating methods differ depending on the material of imaging probe.
► Unbiased screening of fluorophore and binding enzyme revealed novel imaging tags.
► High-throughput screening of diversity-oriented library disclose novel imaging probes.
► Careful design of screening platform is crucial step in diversity-oriented approach.
► We reviewed in vitro spectrum-based, fluorescent image-based, and FACS-based screenings.