PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 17170094-7 2007 The ATRA-induced tube formation was inhibited by coincubation with RAR antagonist LE540/LE135. LE 135 88-93 retinoic acid receptor alpha Homo sapiens 67-70 18453568-7 2008 Moreover, LE135, a RA receptor antagonist, blocked the increased expression of CCR9 driven by IL-4-treated MLN-DC. LE 135 10-15 chemokine (C-C motif) receptor 9 Mus musculus 79-83 18453568-7 2008 Moreover, LE135, a RA receptor antagonist, blocked the increased expression of CCR9 driven by IL-4-treated MLN-DC. LE 135 10-15 interleukin 4 Mus musculus 94-98 11945126-6 2002 LE135 (46) is a unique antagonist with RARbeta-selectivity. LE 135 0-5 retinoic acid receptor beta Homo sapiens 39-46 12882839-10 2003 The RA receptor (RAR) antagonists, LE540 and LE135, but not the retinoic X receptor (RXR) antagonist, PA452, inhibited the effect of RA on Th1/Th2 development. LE 135 45-50 retinoic acid receptor, alpha Mus musculus 4-15 12882839-10 2003 The RA receptor (RAR) antagonists, LE540 and LE135, but not the retinoic X receptor (RXR) antagonist, PA452, inhibited the effect of RA on Th1/Th2 development. LE 135 45-50 retinoic acid receptor, alpha Mus musculus 17-20 12882839-10 2003 The RA receptor (RAR) antagonists, LE540 and LE135, but not the retinoic X receptor (RXR) antagonist, PA452, inhibited the effect of RA on Th1/Th2 development. LE 135 45-50 negative elongation factor complex member C/D, Th1l Mus musculus 139-142 12882839-10 2003 The RA receptor (RAR) antagonists, LE540 and LE135, but not the retinoic X receptor (RXR) antagonist, PA452, inhibited the effect of RA on Th1/Th2 development. LE 135 45-50 heart and neural crest derivatives expressed 2 Mus musculus 143-146 10336422-9 1999 These results demonstrate that LE135 and LE540 were a novel class of RARbeta-selective antagonists and anti-AP-1 retinoids and should be useful tools for studying the role of retinoids and their receptors. LE 135 31-36 retinoic acid receptor beta Homo sapiens 69-76 10336422-3 1999 Both LE135 and LE540 inhibited retinoic acid (RA)-induced transcriptional activation of RARbeta, but not RARalpha, RARgamma or retinoid X receptor alpha (RXRalpha), on a variety of RA response elements. LE 135 5-10 retinoic acid receptor beta Homo sapiens 88-95 32278009-5 2020 Our results confirmed this hypothesis because: i) protection of PTC by DIDS was abolished by RAR-beta antagonist LE-135; ii) DIDS increased the expression of RAR-beta in PTC and prevented its decrease in cisplatin-treated PTC but not in cisplatin-treated human cervical adenocarcinoma HeLa cells in which DIDS failed to prevent cisplatin"s toxicity; iii) while RAR-beta expression decreased in cisplatin-treated PTC, RAR-beta over-expression prevented cisplatin"s toxicity. LE 135 113-119 retinoic acid receptor alpha Homo sapiens 93-101 10336422-7 1999 Our data showed that LE135 and LE540 strongly repressed 12-O-tetradecanoylphorbol-13-acetate-induced AP-1 activity in the presence of RARbeta and RXRalpha. LE 135 21-26 retinoic acid receptor beta Homo sapiens 134-141 10336422-7 1999 Our data showed that LE135 and LE540 strongly repressed 12-O-tetradecanoylphorbol-13-acetate-induced AP-1 activity in the presence of RARbeta and RXRalpha. LE 135 21-26 retinoid X receptor alpha Homo sapiens 146-154 35608792-5 2022 Similarly, LE135 (a selective RARbeta antagonist) attenuated AD action, suggesting that AD promotes adipose browning through RARbeta. LE 135 11-16 retinoic acid receptor, alpha Mus musculus 30-37 35608792-5 2022 Similarly, LE135 (a selective RARbeta antagonist) attenuated AD action, suggesting that AD promotes adipose browning through RARbeta. LE 135 11-16 retinoic acid receptor, alpha Mus musculus 125-132 34001245-16 2021 RARbeta inhibitor Le135 partly blocked the reversal effect of ATRA. LE 135 18-23 retinoic acid receptor, alpha Mus musculus 0-7 32278009-5 2020 Our results confirmed this hypothesis because: i) protection of PTC by DIDS was abolished by RAR-beta antagonist LE-135; ii) DIDS increased the expression of RAR-beta in PTC and prevented its decrease in cisplatin-treated PTC but not in cisplatin-treated human cervical adenocarcinoma HeLa cells in which DIDS failed to prevent cisplatin"s toxicity; iii) while RAR-beta expression decreased in cisplatin-treated PTC, RAR-beta over-expression prevented cisplatin"s toxicity. LE 135 113-119 retinoic acid receptor alpha Homo sapiens 158-166 32278009-5 2020 Our results confirmed this hypothesis because: i) protection of PTC by DIDS was abolished by RAR-beta antagonist LE-135; ii) DIDS increased the expression of RAR-beta in PTC and prevented its decrease in cisplatin-treated PTC but not in cisplatin-treated human cervical adenocarcinoma HeLa cells in which DIDS failed to prevent cisplatin"s toxicity; iii) while RAR-beta expression decreased in cisplatin-treated PTC, RAR-beta over-expression prevented cisplatin"s toxicity. LE 135 113-119 retinoic acid receptor alpha Homo sapiens 158-166 32278009-5 2020 Our results confirmed this hypothesis because: i) protection of PTC by DIDS was abolished by RAR-beta antagonist LE-135; ii) DIDS increased the expression of RAR-beta in PTC and prevented its decrease in cisplatin-treated PTC but not in cisplatin-treated human cervical adenocarcinoma HeLa cells in which DIDS failed to prevent cisplatin"s toxicity; iii) while RAR-beta expression decreased in cisplatin-treated PTC, RAR-beta over-expression prevented cisplatin"s toxicity. LE 135 113-119 retinoic acid receptor alpha Homo sapiens 158-166 29926831-10 2018 Interestingly, LE135 treatment also inhibits the normal downregulation of RXRalpha in tail and spinal cord tissues at 21 dpa. LE 135 15-20 retinoid x receptor, gamma a Danio rerio 74-82 30461012-6 2019 The rosiglitazone- and ATRA-induced elevation of mRNA level, Mg 2+ influx, and promoter activity of TRPM6 were inhibited by GW-9662, a potent antagonist of peroxisome proliferator-activated receptor (PPAR)gamma, and LE135, a retinoic acid receptor (RAR) antagonist, respectively. LE 135 216-221 transient receptor potential cation channel, subfamily M, member 6 Rattus norvegicus 100-105 30461012-10 2019 A chromatin immunoprecipitation assay revealed that PPARgamma and RAR bind to the PPRE, which was blocked by GW-9662 and LE135, respectively. LE 135 121-126 peroxisome proliferator-activated receptor gamma Rattus norvegicus 52-61 31359396-4 2019 The levels of RARbeta signaling can be modulated using RARbeta agonists (e.g., all-trans retinoic acid) and antagonists (e.g., LE135). LE 135 127-132 retinoic acid receptor beta Homo sapiens 14-21 29154149-5 2017 On the other hand, we found that the inhibition of RARbeta with 5muM LE135, together with RA treatment, increased the efficiency of mouse ES cell differentiation into neurons by more than 4-fold as compared to cells treated with RA only. LE 135 69-74 retinoic acid receptor, beta Mus musculus 51-58 26967733-10 2016 Western blot assay revealed that RARbeta protein levels were increased significantly in a time-dependent manner in ARPE-19 cells treated with 10-6 mol/l ATRA from 12 h to 72 h, with a marked increase observed at 24 h and 48 h. The upregulation of RARbeta and the ATRA-induced secretion in ARPE-19 cells could be inhibited by the RARbeta antagonist LE135. LE 135 348-353 retinoic acid receptor beta Homo sapiens 33-40 21308729-1 2011 The present study aimed to investigate the role of a retinoic acid receptor-beta (RARbeta) inhibitor LE135 on TGF-beta induced chondrogenesis of human bone marrow mesenchymal stem cells (hMSCs). LE 135 101-106 retinoic acid receptor beta Homo sapiens 53-80 24308840-3 2014 Here, we demonstrate that LE135 [4-(7,8,9,10-tetrahydro-5,7,7,10,10-pentamethyl-5H-benzo[e]naphtho[2,3-b][1,4]diazepin-13-yl)benzoic acid], a selective antagonist of RARbeta , is a potent activator of the capsaicin (TRPV1) and wasabi (TRPA1) receptors, two critical pain-initiating cation channels. LE 135 26-31 retinoic acid receptor beta Homo sapiens 166-173 24308840-3 2014 Here, we demonstrate that LE135 [4-(7,8,9,10-tetrahydro-5,7,7,10,10-pentamethyl-5H-benzo[e]naphtho[2,3-b][1,4]diazepin-13-yl)benzoic acid], a selective antagonist of RARbeta , is a potent activator of the capsaicin (TRPV1) and wasabi (TRPA1) receptors, two critical pain-initiating cation channels. LE 135 26-31 transient receptor potential cation channel subfamily V member 1 Homo sapiens 216-221 24308840-3 2014 Here, we demonstrate that LE135 [4-(7,8,9,10-tetrahydro-5,7,7,10,10-pentamethyl-5H-benzo[e]naphtho[2,3-b][1,4]diazepin-13-yl)benzoic acid], a selective antagonist of RARbeta , is a potent activator of the capsaicin (TRPV1) and wasabi (TRPA1) receptors, two critical pain-initiating cation channels. LE 135 26-31 transient receptor potential cation channel subfamily A member 1 Homo sapiens 235-240 24308840-4 2014 EXPERIMENTAL APPROACH: We performed to investigate the excitatory effects of LE135 on TRPV1 and TRPA1 channels expressed in HEK293T cells and in dorsal root ganglia neurons with calcium imaging and patch-clamp recordings. LE 135 77-82 transient receptor potential cation channel subfamily V member 1 Homo sapiens 86-91 24308840-4 2014 EXPERIMENTAL APPROACH: We performed to investigate the excitatory effects of LE135 on TRPV1 and TRPA1 channels expressed in HEK293T cells and in dorsal root ganglia neurons with calcium imaging and patch-clamp recordings. LE 135 77-82 transient receptor potential cation channel subfamily A member 1 Homo sapiens 96-101 24308840-5 2014 We also used site-directed mutagenesis of the channels to determine the structural basis of LE135-induced activation of TRPV1 and TRPA1 channels and behavioural testing to examine if pharmacological inhibition and genetic deletion of the channels affected LE135-evoked pain-related behaviours. LE 135 92-97 transient receptor potential cation channel subfamily V member 1 Homo sapiens 120-125 24308840-5 2014 We also used site-directed mutagenesis of the channels to determine the structural basis of LE135-induced activation of TRPV1 and TRPA1 channels and behavioural testing to examine if pharmacological inhibition and genetic deletion of the channels affected LE135-evoked pain-related behaviours. LE 135 92-97 transient receptor potential cation channel subfamily A member 1 Homo sapiens 130-135 24308840-6 2014 KEY RESULTS: LE135 activated both the capsaicin receptor (TRPV1) and the allyl isothiocyanate receptor (TRPA1) heterologously expressed in HEK293T cells and endogenously expressed by sensory nociceptors. LE 135 13-18 transient receptor potential cation channel subfamily V member 1 Homo sapiens 38-56 24308840-6 2014 KEY RESULTS: LE135 activated both the capsaicin receptor (TRPV1) and the allyl isothiocyanate receptor (TRPA1) heterologously expressed in HEK293T cells and endogenously expressed by sensory nociceptors. LE 135 13-18 transient receptor potential cation channel subfamily V member 1 Homo sapiens 58-63 24308840-6 2014 KEY RESULTS: LE135 activated both the capsaicin receptor (TRPV1) and the allyl isothiocyanate receptor (TRPA1) heterologously expressed in HEK293T cells and endogenously expressed by sensory nociceptors. LE 135 13-18 transient receptor potential cation channel subfamily A member 1 Homo sapiens 104-109 24308840-7 2014 Mutations disrupting the capsaicin-binding site attenuated LE135 activation of TRPV1 channels and a single mutation (K170R) eliminated TRPA1 activity evoked by LE135. LE 135 59-64 transient receptor potential cation channel subfamily V member 1 Homo sapiens 79-84 24308840-9 2014 Both TRPV1 and TRPA1 channels were involved in LE135-elicited pain-related responses, as shown by pharmacological and genetic ablation studies. LE 135 47-52 transient receptor potential cation channel subfamily V member 1 Homo sapiens 5-10 24308840-9 2014 Both TRPV1 and TRPA1 channels were involved in LE135-elicited pain-related responses, as shown by pharmacological and genetic ablation studies. LE 135 47-52 transient receptor potential cation channel subfamily A member 1 Homo sapiens 15-20 23946634-10 2013 Pretreatment of the HSFs with LE135, an antagonist of retinoic acid receptor beta (RARbeta), abolished the ATRA-induced changes inactivation of ERK 1/2 and JNK. LE 135 30-35 retinoic acid receptor beta Homo sapiens 54-81 23946634-10 2013 Pretreatment of the HSFs with LE135, an antagonist of retinoic acid receptor beta (RARbeta), abolished the ATRA-induced changes inactivation of ERK 1/2 and JNK. LE 135 30-35 retinoic acid receptor beta Homo sapiens 83-90 23946634-10 2013 Pretreatment of the HSFs with LE135, an antagonist of retinoic acid receptor beta (RARbeta), abolished the ATRA-induced changes inactivation of ERK 1/2 and JNK. LE 135 30-35 mitogen-activated protein kinase 3 Homo sapiens 144-151 23946634-10 2013 Pretreatment of the HSFs with LE135, an antagonist of retinoic acid receptor beta (RARbeta), abolished the ATRA-induced changes inactivation of ERK 1/2 and JNK. LE 135 30-35 mitogen-activated protein kinase 8 Homo sapiens 156-159 22052812-6 2011 Treatment with LE135, a RARbeta-selective antagonist, caused a significant inhibition of ependymal outgrowth and a decrease in tail regenerate length. LE 135 15-20 retinoic acid receptor beta Homo sapiens 24-31 24851851-1 2014 AIM: Main objective was to investigate whether the synthetic retinoic acid receptor (RAR)-beta antagonist LE135 is able to drive in vitro chondrogenesis of human mesenchymal stromal cells (MSCs) or improve differentiation by suppressing hypertrophic chondrocyte development. LE 135 106-111 retinoic acid receptor beta Homo sapiens 85-88 23318218-12 2013 The neuronal differentiation promoting effects of all-trans retinoic acid on mesenchymal stem cells could be inhibited by siRNA silencing of retinoic acid receptor beta and by LE135, an inhibitor of retinoic acid receptor beta. LE 135 176-181 retinoic acid receptor beta Homo sapiens 199-226 21763841-14 2011 However, there was no significant difference in the ARM rescue rate between group B and Group C. CONCLUSION: The present study provides evidence that in the hindgut region, RAR selective retinoid antagonist, LE135, could rescue embryos from ARM. LE 135 208-213 Rab40B, member RAS oncogene family Mus musculus 173-176 21308729-1 2011 The present study aimed to investigate the role of a retinoic acid receptor-beta (RARbeta) inhibitor LE135 on TGF-beta induced chondrogenesis of human bone marrow mesenchymal stem cells (hMSCs). LE 135 101-106 retinoic acid receptor beta Homo sapiens 82-89