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RISS 인기검색어
- 검색키워드
- 저자 : Jong-Hee Chae(Jong-Hee Ch (검색결과 3 건)
- 무료
- 기관 내 무료
- 유료
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Yun, Jiyeon,Hong, Min Hee,Kim, Seok-Young,Park, Chae-Won,Kim, Soyoung,Yun, Mi Ran,Kang, Han Na,Pyo, Kyoung-Ho,Lee, Sung Sook,Koh, Jong Sung,Song, Ho-Juhn,Kim, Dong Kyun,Lee, Young-Sung,Oh, Se-Woong,Ch American Association for Cancer Research 2019 Clinical Cancer Research Vol.25 No.8
<P><B>Purpose:</B></P><P>Given that osimertinib is the only approved third-generation EGFR-TKI against <I>EGFR</I> activating and resistant T790M mutated non–small cell lung cancer (NSCLC), additional mutant-selective inhibitors with a higher efficacy, especially for brain metastases, with favorable toxicity profile are still needed. In this study, we investigated the antitumor efficacy of YH25448, an oral, mutant-selective, irreversible third-generation EGFR-TKI in preclinical models.</P><P><B>Experimental Design:</B></P><P>Antitumor activity of YH25448 was investigated <I>in vitro</I> using mutant <I>EGFR</I>-expressing Ba/F3 cells and various lung cancer cell lines. <I>In vivo</I> antitumor efficacy, ability to penetrate the blood–brain barrier (BBB), and skin toxicity of YH25448 were examined and compared with those of osimertinib using cell lines and PDX model.</P><P><B>Results:</B></P><P>Compared with osimertinib, YH25448 showed a higher selectivity and potency in kinase assay and mutant <I>EGFR</I>-expressing Ba/F3 cells. In various cell line models harboring <I>EGFR</I> activating and T790M mutation, YH25448 effectively inhibited EGFR downstream signaling pathways, leading to cellular apoptosis. When compared <I>in vivo</I> at equimolar concentrations, YH25448 produced significantly better tumor regression than osimertinib. Importantly, YH25448 induced profound tumor regression in brain metastasis model with excellent brain/plasma and tumor/brain area under the concentration–time curve value. YH25448 rarely suppressed the levels of p-EGFR in hair follicles, leading to less keratosis than osimertinib in animal model. The potent systemic and intracranial activity of YH25448 has been shown in an ongoing phase I/II clinical trial for advanced <I>EGFR</I> T790M mutated NSCLC (NCT03046992).</P><P><B>Conclusions:</B></P><P>Our findings suggest that YH25448 is a promising third-generation EGFR inhibitor, which may be more effective and better tolerated than the currently approved osimertinib.</P>
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Discovery of novel tetrahydroisoquinoline-containing pyrimidines as ALK inhibitors
Achary, Raghavendra,Yun, Jeong In,Park, Chi Min,Mathi, Gangadhar Rao,Lee, Joo Yun,Ha, Jae Du,Chae, Chong Hak,Ahn, Sunjoo,Park, Chi Hoon,Lee, Chong Ock,Hwang, Jong Yeon,Yun, Chang-Soo,Jung, Hee Jung,Ch Pergamon 2016 Bioorganic & medicinal chemistry Vol.24 No.2
<P>Exploration of the two-position side chain of pyrimidine in LDK378 with tetrahydroisoquinolines (THIQs) led to discovery of 8 and 17 as highly potent ALK inhibitors. THIQs 8 and 17 showed encouraging in vitro and in vivo xenograft efficacies, comparable with those of LDK378. Although THIQ analogs (8a-o and 17a-i) prepared were not as active as their parent compounds, both 8 and 17 have significant inhibitory activities against various ALK mutant enzymes including G1202R, indicating that this series of compounds could be further optimized as useful ALK inhibitors overcoming the resistance issues found from crizotinib and LDK378. (C) 2015 Elsevier Ltd. All rights reserved.</P>
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Hye Jin Kim(Hye Jin Kim),Young Joon Ko(Young Joon Ko),Soo Yeon Kim(Soo Yeon Kim),Anna Cho(Anna Cho),Hunmin Kim(Hunmin Kim),Byung Chan Lim(Byung Chan Lim),Hee Hwang(Hee Hwang),Jong-Hee Chae(Jong-Hee Ch 대한소아신경학회 2022 대한소아신경학회지 Vol.30 No.4
Purpose: Patients with self-limited epilepsy with centrotemporal spikes (SLECTS) rarely experience generalized tonic-clonic seizures (GTCS) after remission, and post-remission GTCS has not been thoroughly described in earlier studies. Herein, we describe the clinical and electrographic features of GTCS after a substantial period of seizure freedom in patients with SLECTS. Methods: This study included six patients (three boys and three girls) diagnosed with SLECTS who later developed GTCS after or near remission. Medical records, including clinical data and serial electroencephalography (EEG) recordings, were retrospectively reviewed for all patients. Results: Patients’ age at SLECTS onset ranged from 5.2 to 10.2 years (mean, 8.4 years), while seizure cessation was achieved between 8 and 12.2 years. During SLECTS, typical centrotemporal spikes were observed in all patients, and generalized spike-and-wave discharges were observed in three patients. The age at the first episode of subsequent GTCS ranged from 14.4 to 17.3 years (mean, 15.8 years), constituting an average interval of 5.6 years after the last episode of seizures (range, 4.1 to 8.1 years). EEG at subsequent episodes of GTCS revealed generalized discharges in two patients, focal discharges in two other patients, and normal discharges in the remaining two patients. Two patients had multiple episodes of GTCS. Conclusion: Although rare, GTCS may occur near or after remission in patients with SLECTS, and clinicians should be aware of this. Subsequent GTCS may be a manifestation of idiopathic generalized epilepsy. However, large-scale studies are needed to determine the nature of such episodes of GTCS and their associated risk factors.
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