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A tagged triazine library having a built-in linker that provides a straight-forward transition from phenotypic screening to target identification is discussed. The successful target identification has helped to make a breakthrough in showing the mechanism for the observed phenotype.

A mitochondria-targeted rosamine library in C2C12 myogenesis was applied to identify the compound that regulates the muscle differentiation during the remarkable changes undergone by mitochondria. The findings from the study provide insight into the potential application of fluorescent small molecules in the discovery of a bioactive probe that induces a specific cellular response.

The design and synthesis of a reliable fluorescent probe for use in cell-based screening for myogenesis is described. The results provide insight into the cell-state selectivity of compound flourescence which are used as probes for high-throughput screening.

The first rosamine library is developed by using solidphase chemistry as a potential fluorescent sensor set. The potential of H22 as a glutathione fluorescent probe for monitoring cellular glutathione levels is described.

A fluorescent dye library approach for the development of a bioanalyte sensor was sought. The screening of a rosamine dye library against diverse macromolecules led to the discovery of a highly sensitive human serum albumin binder, G13, with ∼36-fold fluorescence intensity change. G13showed a highly selective response to HSA over other macromolecules including albumins from other species. The potential use of G13for the detection of HSA in biofluids is described. [ABSTRACT FROM AUTHOR]

Chemical genetics is a powerful method which utilizes small molecule regulators to reveal the molecular basis of diverse biological processes. However, the current chemical genetic approach sometimes meets a serious bottleneck during the process of target identification. One faces difficulty in conjugating the active compound to an affinity matrix without losing or reducing its activity that leads to laborious structure–activity relationship (SAR) studies. To facilitate this process, we have developed a tagged triazine library containing a built-in linker that provides a straightforward transition from phenotypic screening to target identification. A strategy for constructinig a tagged library and applications with a streamlined target identification and subsequent mechanistic study are discussed in this Account. [ABSTRACT FROM AUTHOR]

The combinatorial fluorescent dapoxyl dye library was prepared by both solution- and solid-phase synthesis, generating 80 unique dapoxyl derivatives. A fluorescence-based screening toward human serum albumin (HSA) found one highly sensitive HSA binder ( A41-S) with over 55-fold intensity change. Displacement assay showed the selective binding of A41-Sto the site I of HSA, addressing its potential to be a highly selective and sensitive HSA probe. [ABSTRACT FROM AUTHOR]