Wu, Zining published the artcileCell-Based Selection Expands the Utility of DNA-Encoded Small-Molecule Library Technology to Cell Surface Drug Targets: Identification of Novel Antagonists of the NK3 Tachykinin Receptor, Computed Properties of 475216-25-2, the publication is ACS Combinatorial Science (2015), 17(12), 722-731, database is CAplus and MEDLINE.
DNA-encoded small-mol. library technol. has recently emerged as a new paradigm for identifying ligands against drug targets. To date, this technol. has been used with soluble protein targets that are produced and used in a purified state. Here, we describe a cell-based method for identifying small-mol. ligands from DNA-encoded libraries against integral membrane protein targets. We use this method to identify novel, potent, and specific inhibitors of NK3, a member of the tachykinin family of G-protein coupled receptors (GPCRs). The method is simple and broadly applicable to other GPCRs and integral membrane proteins. We have extended the application of DNA-encoded library technol. to membrane-associated targets and demonstrate the feasibility of selecting DNA-tagged, small-mol. ligands from complex combinatorial libraries against targets in a heterogeneous milieu, such as the surface of a cell.
ACS Combinatorial Science published new progress about 475216-25-2. 475216-25-2 belongs to amides-buliding-blocks, auxiliary class Fluoride,Nitro Compound,Amine,Benzene,Amide,Benzene Compounds, name is 4-Fluoro-N-methyl-3-nitrobenzamide, and the molecular formula is C9H9ClN2, Computed Properties of 475216-25-2.
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