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- W2941154489 abstract "Novel pyridine- and pyrimidine-based allosteric inhibitors are reported that achieve PDE4D subtype selectivity through recognition of a single amino acid difference on a key regulatory domain, known as UCR2, that opens and closes over the catalytic site for cAMP hydrolysis. The design and optimization of lead compounds was based on iterative analysis of X-ray crystal structures combined with metabolite identification. Selectivity for the activated, dimeric form of PDE4D provided potent memory enhancing effects in a mouse model of novel object recognition with improved tolerability and reduced vascular toxicity over earlier PDE4 inhibitors that lack subtype selectivity. The lead compound, 28 (BPN14770), has entered midstage, human phase 2 clinical trials for the treatment of Fragile X Syndrome." @default.
- W2941154489 created "2019-05-03" @default.
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- W2941154489 date "2019-04-23" @default.
- W2941154489 modified "2023-09-25" @default.
- W2941154489 title "Design and Synthesis of Selective Phosphodiesterase 4D (PDE4D) Allosteric Inhibitors for the Treatment of Fragile X Syndrome and Other Brain Disorders" @default.
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- W2941154489 cites W1963768723 @default.
- W2941154489 cites W1968714547 @default.
- W2941154489 cites W1968946845 @default.
- W2941154489 cites W1970164987 @default.
- W2941154489 cites W1973617706 @default.
- W2941154489 cites W1973966511 @default.
- W2941154489 cites W1976344568 @default.
- W2941154489 cites W1977390447 @default.
- W2941154489 cites W1983682905 @default.
- W2941154489 cites W1991168687 @default.
- W2941154489 cites W1992591110 @default.
- W2941154489 cites W1994337546 @default.
- W2941154489 cites W1995808589 @default.
- W2941154489 cites W1997277329 @default.
- W2941154489 cites W2001641653 @default.
- W2941154489 cites W2002780348 @default.
- W2941154489 cites W2003646327 @default.
- W2941154489 cites W2006701954 @default.
- W2941154489 cites W2007786396 @default.
- W2941154489 cites W2010899661 @default.
- W2941154489 cites W2016270023 @default.
- W2941154489 cites W2022959185 @default.
- W2941154489 cites W2023704692 @default.
- W2941154489 cites W2024515004 @default.
- W2941154489 cites W2034445959 @default.
- W2941154489 cites W2034986487 @default.
- W2941154489 cites W2035892299 @default.
- W2941154489 cites W2038840577 @default.
- W2941154489 cites W2042935819 @default.
- W2941154489 cites W2043379639 @default.
- W2941154489 cites W2051473177 @default.
- W2941154489 cites W2056348676 @default.
- W2941154489 cites W2064759622 @default.
- W2941154489 cites W2067738389 @default.
- W2941154489 cites W2069566702 @default.
- W2941154489 cites W2073503004 @default.
- W2941154489 cites W2074923758 @default.
- W2941154489 cites W2075634772 @default.
- W2941154489 cites W2078329648 @default.
- W2941154489 cites W2087942365 @default.
- W2941154489 cites W2088031242 @default.
- W2941154489 cites W2089627181 @default.
- W2941154489 cites W2090814246 @default.
- W2941154489 cites W2096271770 @default.
- W2941154489 cites W2101175089 @default.
- W2941154489 cites W2103105948 @default.
- W2941154489 cites W2104119127 @default.
- W2941154489 cites W2106753244 @default.
- W2941154489 cites W2108921801 @default.
- W2941154489 cites W2118462346 @default.
- W2941154489 cites W2119774957 @default.
- W2941154489 cites W2124026197 @default.
- W2941154489 cites W2124161234 @default.
- W2941154489 cites W2128858680 @default.
- W2941154489 cites W2130479394 @default.
- W2941154489 cites W2136827845 @default.
- W2941154489 cites W2148003974 @default.
- W2941154489 cites W2154714625 @default.
- W2941154489 cites W2166329705 @default.
- W2941154489 cites W2167089957 @default.
- W2941154489 cites W2229830115 @default.
- W2941154489 cites W2402700043 @default.
- W2941154489 cites W2613270122 @default.
- W2941154489 cites W2734770672 @default.
- W2941154489 cites W2749059461 @default.
- W2941154489 cites W2766431378 @default.
- W2941154489 cites W2773011191 @default.
- W2941154489 cites W2807318456 @default.
- W2941154489 cites W2809193491 @default.
- W2941154489 cites W2883573930 @default.