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[Retinoid antagonists].
Umemiya H, Kagechika H, Fukasawa H, Hashimoto Y, Shudo K. Umemiya H, et al. Yakugaku Zasshi. 1996 Dec;116(12):928-41. doi: 10.1248/yakushi1947.116.12_928. Yakugaku Zasshi. 1996. PMID: 8993231 Review. Japanese.
Structure-activity relationships of LE135 (20) showed that the naphthalenyl analogs [LE540 (21) and LE550 (22)] are more potent retinoid antagonists in HL-60 assay. ...
Structure-activity relationships of LE135 (20) showed that the naphthalenyl analogs [LE540 (21) and LE550 (22)] are more potent retin …
Retinoic acid receptor antagonist LE540 attenuates wakefulness via the dopamine D1 receptor in mice.
Kitaoka K, Shimizu M, Shimizu N, Chikahisa S, Nakagomi M, Shudo K, Yoshizaki K, Séi H. Kitaoka K, et al. Brain Res. 2011 Nov 14;1423:10-6. doi: 10.1016/j.brainres.2011.09.023. Epub 2011 Sep 17. Brain Res. 2011. PMID: 22000589
To address this problem, we investigated whether the chronic administration of LE540 (30mg/kg/day), an antagonist of RARs, for 1 or 4weeks attenuated EEG delta power during sleep in mice. Consequently, 4-week LE540 administration induced a significant attenuation of …
To address this problem, we investigated whether the chronic administration of LE540 (30mg/kg/day), an antagonist of RARs, for 1 or 4 …
Encapsulation of the synthetic retinoids Am80 and LE540 into polymeric micelles and the retinoids' release control.
Satoh T, Higuchi Y, Kawakami S, Hashida M, Kagechika H, Shudo K, Yokoyama M. Satoh T, et al. J Control Release. 2009 Jun 19;136(3):187-95. doi: 10.1016/j.jconrel.2009.02.024. Epub 2009 Mar 14. J Control Release. 2009. PMID: 19289148
The objective of this study was to encapsulate two synthetic retinoids Am80 and LE540 into polymeric micelles and to control the retinoids' release rate in vitro. Highly efficient encapsulation yields of these retinoids were obtained for micelles forming from PEG-poly(benz …
The objective of this study was to encapsulate two synthetic retinoids Am80 and LE540 into polymeric micelles and to control the reti …
Encapsulation of a hydrophobic drug into a polymer-micelle core explored with synchrotron SAXS.
Akiba I, Terada N, Hashida S, Sakurai K, Sato T, Shiraishi K, Yokoyama M, Masunaga H, Ogawa H, Ito K, Yagi N. Akiba I, et al. Langmuir. 2010 May 18;26(10):7544-51. doi: 10.1021/la904355p. Langmuir. 2010. PMID: 20361731
Synchrotron small-angle X-ray scattering (SAXS) at the SPring-8 40B2 and 45XU beamlines was carried out on aqueous solutions of (PEG-P(Asp(Bzl))): partially benzyl-esterified poly(ethylene glycol)-block-poly(aspartic acid) with LE540 loaded up to 8.3 wt %, where LE540
Synchrotron small-angle X-ray scattering (SAXS) at the SPring-8 40B2 and 45XU beamlines was carried out on aqueous solutions of (PEG-P(Asp(B …
The isoflavone puerarin induces Foxp3+ regulatory T cells by augmenting retinoic acid production, thereby inducing mucosal immune tolerance in a murine food allergy model.
Yamamoto T, Matsunami E, Komori K, Hayashi S, Kadowaki M. Yamamoto T, et al. Biochem Biophys Res Commun. 2019 Aug 27;516(3):626-631. doi: 10.1016/j.bbrc.2019.06.051. Epub 2019 Jun 22. Biochem Biophys Res Commun. 2019. PMID: 31235250
In addition, the preventive effect of puerarin was suppressed in the FA model by pretreatment with LE540, an RA receptor (RAR) antagonist. The induction of Foxp3(+)CD4(+) cells and CD103(+)CD11c(+) DCs by puerarin was reduced by pretreatment with LE540. ...
In addition, the preventive effect of puerarin was suppressed in the FA model by pretreatment with LE540, an RA receptor (RAR) antago …
Retinoid antagonists inhibit normal patterning during limb regeneration in the axolotl, Ambystoma mexicanum.
Del Rincón SV, Scadding SR. Del Rincón SV, et al. J Exp Zool. 2002 Apr 1;292(5):435-43. doi: 10.1002/jez.10050. J Exp Zool. 2002. PMID: 11857478
We have investigated whether endogenous retinoids are essential for patterning during axolotl (Ambystoma mexicanum) limb regeneration by using retinoid antagonists that bind to specific RAR (retinoic acid receptor) or RXR (retinoid X receptor) retinoid receptor subtypes. Retinoid …
We have investigated whether endogenous retinoids are essential for patterning during axolotl (Ambystoma mexicanum) limb regeneration by usi …
Retinoid receptor-based signaling plays a role in voltage-dependent inhibition of invertebrate voltage-gated Ca2+ channels.
de Hoog E, Lukewich MK, Spencer GE. de Hoog E, et al. J Biol Chem. 2019 Jun 28;294(26):10076-10093. doi: 10.1074/jbc.RA118.006444. Epub 2019 May 2. J Biol Chem. 2019. PMID: 31048374 Free PMC article.
This inhibition appeared to be independent of G proteins and was largely restricted to Ca(v)2 Ca(2+) channels. Of note, an RAR pan-antagonist, LE540, also inhibited I(Ca) but produced G protein-dependent, voltage-dependent inhibition of VGCCs. ...
This inhibition appeared to be independent of G proteins and was largely restricted to Ca(v)2 Ca(2+) channels. Of note, an RAR pan-antagonis …
Identification of a novel class of retinoic acid receptor beta-selective retinoid antagonists and their inhibitory effects on AP-1 activity and retinoic acid-induced apoptosis in human breast cancer cells.
Li Y, Hashimoto Y, Agadir A, Kagechika H, Zhang Xk. Li Y, et al. J Biol Chem. 1999 May 28;274(22):15360-6. doi: 10.1074/jbc.274.22.15360. J Biol Chem. 1999. PMID: 10336422 Free article.
Four candidate retinoid antagonists (LE135, LE511, LE540, and LE550) were designed on the basis of the ligand superfamily concept and synthesized. ...Both LE135 and LE540 inhibited retinoic acid (RA)-induced transcriptional activation of RARbeta, but not RARalpha, R …
Four candidate retinoid antagonists (LE135, LE511, LE540, and LE550) were designed on the basis of the ligand superfamily concept and …
ATRA Regulates Innate Immunity in Liver Ischemia/Reperfusion Injury via RARα/Akt/Foxo1 Signaling.
Zhong C, Pu L, Fang M, Rao J, Wang X. Zhong C, et al. Biol Pharm Bull. 2018;41(4):530-535. doi: 10.1248/bpb.b17-00832. Biol Pharm Bull. 2018. PMID: 29607925 Free article.
In vitro, RAW264.7 macrophages were treatment with ATRA (1 M) or LE540 (5 M, a retinoic acid receptor alpha (RARalpha) receptor antagonist) before lipopolysaccharide (100 ng/mL) stimulation. In vivo, ATRA protected the liver from IR injury by improving hepatocellular funct …
In vitro, RAW264.7 macrophages were treatment with ATRA (1 M) or LE540 (5 M, a retinoic acid receptor alpha (RARalpha) receptor antag …
Retinoic acid receptor α promotes autophagy to alleviate liver ischemia and reperfusion injury.
Zhong C, Pu LY, Fang MM, Gu Z, Rao JH, Wang XH. Zhong C, et al. World J Gastroenterol. 2015 Nov 21;21(43):12381-91. doi: 10.3748/wjg.v21.i43.12381. World J Gastroenterol. 2015. PMID: 26604645 Free PMC article.
Reverse transcription-polymerase chain reaction and Western blot were used to detect the expression levels of related factors. To demonstrate the role of RARalpha, LE540, a RARalpha inhibitor, was used to treat hepatocytes injured by H2O2 in vitro. ...Apoptosis was also in …
Reverse transcription-polymerase chain reaction and Western blot were used to detect the expression levels of related factors. To demonstrat …
47 results