Browsing by Author "Chen, Yi-Rong"

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A High-throughput Cell-based Screening for L858R/T790M Mutant Epidermal Growth Factor Receptor Inhibitors
(2012-01-01)
Lin, Wen-Hsing
;
Song, Jen-Shin
;
Lien, Tzu-Wen
;
Chang, Chun-Yu
;
Wu, Szu-Huei
A high-throughput 32D(L858R/T790M) cell-based assay to identify inhibitors of the L858R/T790M mutant epidermal growth factor receptor (EGFR) pathway was established. After screening, ten hits from among 60,000 compounds in our in-house compound library were initially identified. In the secondary assays, one hit, 1-[2-(decyloxy)-2-oxoethyl]-3-methyl-2-[(4-methylphenoxy) methyl]-1H-benzimidazol-3-ium, was confirmed to directly inhibit the kinase activity of recombinant L858R/T790M EGFR and the phosphorylation of EGFR-L858R/T790M in gefitinib-resistant H1975 cells. Thus, this high-throughput assay system may be useful for identifying novel inhibitors which suppress mutant EGFR-T790M signalling and for overcoming T790M-mediated acquired resistance for future anticancer drug discovery.
A novel design of pulsating heat pipe with fewer turns applicable to all orientations
(2012-10-01)
Chien, Kuo-Hsiang
;
Lin, Yur-Tsai
;
Chen, Yi-Rong
;
Yang, Kai-Shing
;
Wang, Chi-Chuan
This study presents a novel pulsating heat pipe (PHP) concept that is functional even when PHP is with fewer turns and is operated horizontally. Two heat pipes were made of copper capillary tubes with an overall size of 122 mm x 57 mm x 5.5 mm is investigated, one had 16 parallel square channels having a uniform cross-section of 2 mm x 2 mm (uniform CLPHP), and the other had 16 alternative size of parallel square channels (non-uniform CLPHP; a cross-section 2 mm x 2 mm and a cross-section of 1 mm x 2 mm in alternating sequence). Test results showed that the performance of PHP rises with the inclination but the uniform channel CLPHP is not functional at horizontal configuration whereas the proposed non-uniform design is still functional even at horizontal arrangement. The thermal resistance for uniform PHP is relative insensitive to change of inclination when the inclination angle exceeds certain threshold value. (c) 2012 Elsevier Ltd. All rights reserved.
Design and Synthesis of Tetrahydropyridothieno[2,3-d]pyrimidine Scaffold Based Epidermal Growth Factor Receptor (EGFR) Kinase Inhibitors: The Role of Side Chain Chirality and Michael Acceptor Group for Maximal Potency
(2010-10-28)
Wu, Chia-Hsien
;
Coumar, Mohane Selvaraj
;
Chu, Chang-Ying
;
Lin, Wen-Hsing
;
Chen, Yi-Rong
HTS hit 7 was modified through hybrid design strategy to introduce a chiral side chain followed by introduction of Michael acceptor group to obtain potent EGFR kinase inhibitors 11 and 19. Both 11 and 19 showed over 3 orders of magnitude enhanced HCC827 antiproliferative activity compared to HTS hit 7 and also inhibited gefitinib-resistant double mutant (DM, T790M/L858R) EGFR kinase at nanomolar concentration. Moreover, treatment with 19 shrinked tumor in nude mice xenograft model.
Design and Synthesis of Tetrahydropyridothieno[2,3-d]pyrimidine Scaffold Based Epidermal Growth Factor Receptor (EGFR) Kinase Inhibitors: The Role of Side Chain Chirality and Michael Acceptor Group for Maximal Potency
(2010-10-28)
Wu, Chia-Hsien
;
Coumar, Mohane Selvaraj
;
Chu, Chang-Ying
;
Lin, Wen-Hsing
;
Chen, Yi-Rong
HTS hit 7 was modified through hybrid design strategy to introduce a chiral side chain followed by introduction of Michael acceptor group to obtain potent EGFR kinase inhibitors 11 and 19. Both 11 and 19 showed over 3 orders of magnitude enhanced HCC827 antiproliferative activity compared to HTS hit 7 and also inhibited gefitinib-resistant double mutant (DM, T790M/L858R) EGFR kinase at nanomolar concentration. Moreover, treatment with 19 shrinked tumor in nude mice xenograft model.
TSV-Based 3D-IC Placement for Timing Optimization
(2011)
Chen, Yi-Rong
;
Chen, Hung-Ming
;
Liu, Shih-Ying
;
電子工程學系及電子研究所
;
Department of Electronics Engineering and Institute of Electronics
The semiconductor technology continue its advnacement in 3D-IC circuit. The concept of 3D-IC introduces additional dimension in latest designs by using stack structures with through-silicon via (TSV). 3D ICs replace long interconnect in 2D ICs with TSV cells. However, optimization in terms of 3D-IC is still immature in many aspects. There still exist problems in placement of standard cells and TSV cells in terms of timing optimization. In this paper, we proposed a methodology on cell placement by applying min-cut partitioning in one layer after layer assignment and address alignment constraint simultaneously. We applied Simulated Annealing to optimize timing and wirelength reduction. In final stage, a greedy legalization procedure is implemented to remove operlaps between cells and TSV cells. Experimental results show that both the wirelengths and the delay of critical paths in 3DICs are much superior compare to 2D ICs.