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- W4313277735 abstract "A pulldown using a biotinylated natural product of interest in the 17β-hydroxywithanolide (17-BHW) class, physachenolide C (PCC), identified the bromodomain and extra-terminal domain (BET) family of proteins (BRD2, BRD3, and BRD4), readers of acetyl-lysine modifications and regulators of gene transcription, as potential cellular targets. BROMOscan bromodomain profiling and biochemical assays support PCC as a BET inhibitor with increased selectivity for bromodomain (BD)-1 of BRD3 and BRD4, and X-ray crystallography and NMR studies uncovered specific contacts that underlie the potency and selectivity of PCC toward BRD3-BD1 over BRD3-BD2. PCC also displays characteristics of a molecular glue, facilitating proteasome-mediated degradation of BRD3 and BRD4. Finally, PCC is more potent than other withanolide analogues and gold-standard pan-BET inhibitor (+)-JQ1 in cytotoxicity assays across five prostate cancer (PC) cell lines regardless of androgen receptor (AR)-signaling status." @default.
- W4313277735 created "2023-01-06" @default.
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- W4313277735 date "2022-12-28" @default.
- W4313277735 modified "2023-09-27" @default.
- W4313277735 title "Physachenolide C is a Potent, Selective BET Inhibitor" @default.
- W4313277735 cites W1488181101 @default.
- W4313277735 cites W1899228729 @default.
- W4313277735 cites W1964750965 @default.
- W4313277735 cites W1965925353 @default.
- W4313277735 cites W1973462980 @default.
- W4313277735 cites W1974487011 @default.
- W4313277735 cites W1976033223 @default.
- W4313277735 cites W1985143543 @default.
- W4313277735 cites W1990174038 @default.
- W4313277735 cites W1992127633 @default.
- W4313277735 cites W1994057597 @default.
- W4313277735 cites W2003872705 @default.
- W4313277735 cites W2007823692 @default.
- W4313277735 cites W2012879968 @default.
- W4313277735 cites W2017393660 @default.
- W4313277735 cites W2022635468 @default.
- W4313277735 cites W2041535798 @default.
- W4313277735 cites W2051959262 @default.
- W4313277735 cites W2056936324 @default.
- W4313277735 cites W2069427471 @default.
- W4313277735 cites W2070033262 @default.
- W4313277735 cites W2072403982 @default.
- W4313277735 cites W2074447021 @default.
- W4313277735 cites W2098167941 @default.
- W4313277735 cites W2102890558 @default.
- W4313277735 cites W2106281303 @default.
- W4313277735 cites W2108921801 @default.
- W4313277735 cites W2109184569 @default.
- W4313277735 cites W2109939279 @default.
- W4313277735 cites W2110035145 @default.
- W4313277735 cites W2115628787 @default.
- W4313277735 cites W2118055719 @default.
- W4313277735 cites W2118428599 @default.
- W4313277735 cites W2120572492 @default.
- W4313277735 cites W2123647733 @default.
- W4313277735 cites W2124026197 @default.
- W4313277735 cites W2125828985 @default.
- W4313277735 cites W2129129812 @default.
- W4313277735 cites W2131387803 @default.
- W4313277735 cites W2134201060 @default.
- W4313277735 cites W2135083090 @default.
- W4313277735 cites W2136332525 @default.
- W4313277735 cites W2144081223 @default.
- W4313277735 cites W2147874841 @default.
- W4313277735 cites W2150727212 @default.
- W4313277735 cites W2158947996 @default.
- W4313277735 cites W2163341755 @default.
- W4313277735 cites W2165810298 @default.
- W4313277735 cites W2168290086 @default.
- W4313277735 cites W2180229411 @default.
- W4313277735 cites W2193763305 @default.
- W4313277735 cites W2212015457 @default.
- W4313277735 cites W2268281268 @default.
- W4313277735 cites W2297636008 @default.
- W4313277735 cites W2335754604 @default.
- W4313277735 cites W2341087013 @default.
- W4313277735 cites W2342092981 @default.
- W4313277735 cites W2404409977 @default.
- W4313277735 cites W2477271322 @default.
- W4313277735 cites W2481128014 @default.
- W4313277735 cites W2521876448 @default.
- W4313277735 cites W2587935821 @default.
- W4313277735 cites W2592136305 @default.
- W4313277735 cites W2593538080 @default.
- W4313277735 cites W2600397718 @default.
- W4313277735 cites W2604245573 @default.
- W4313277735 cites W2625125757 @default.
- W4313277735 cites W2626284340 @default.
- W4313277735 cites W2762381618 @default.
- W4313277735 cites W2795518453 @default.
- W4313277735 cites W2804631000 @default.
- W4313277735 cites W2804719847 @default.
- W4313277735 cites W2884727950 @default.
- W4313277735 cites W2893900046 @default.
- W4313277735 cites W2904329518 @default.
- W4313277735 cites W2912348784 @default.
- W4313277735 cites W2935659406 @default.
- W4313277735 cites W2938148420 @default.
- W4313277735 cites W2948073409 @default.