1200-05-1Relevant articles and documents
A new strategy applied to the synthesis of an α-helical bicyclic peptide constrained by two overlapping i, i+7 side-chain bridges of novel design
Yu, Chongxi,Taylor, John W.
, p. 1731 - 1734 (1996)
A conformationally constrained, bicyclic, 14-residue peptide containing two overlapping i, i+7 side-chain bridges has been synthesized. The design of the side-chain linkage, which is built around a p-substituted benzene ring for rigidity, and the solid-phase approach applied to the peptide synthesis, are both new. A Boc/Benzyl peptide chain assembly method was combined with Fmoc/OFm orthogonal side-chain deprotection and solid-phase cyclization to form the first side-chain lactam bridge. A 2-(2-pyridyl)ethyl group (2-Pet), activated by methylation with CH3I in DMF, was then used in combination with Fmoc to allow a second orthogonal side-chain deprotection and solid-phase cyclization to form the second bridge. The circular dichroism spectrum of the product indicates that it is highly helical.
HETEROARYL-CARBOXYLIC ACIDS AS HISTONE DEMETHYLASE INHIBITORS
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Page/Page column 131, (2018/01/17)
The invention relates to heteroaryl-carboxylic acids as described herein, useful as histone demethylase inhibitors. The invention also relates to pharmaceutical compositions comprising these compounds and to their use in therapy, including e.g., in the treatment of cancer.
CONJUGATES FOR TREATING DISEASES CAUSED BY PSMA EXPRESSING CELLS
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Page/Page column 68, (2014/06/11)
The invention described herein pertains to the diagnosis, imaging, and/or treatment of pathogenic cell populations. In particular, the invention described herein pertains to the diagnosis, imaging, and/or treatment of diseases caused by PSMA expressing cells, such as prostate cancer cells, using compounds capable of targeting PSMA expressing cells.