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| Type |
Poster Presentation |
| Area |
Medicinal Chemistry |
| Room No. |
Exhibition Hall 2 |
| Time |
4월 18일 (목요일) 11:00~12:30 |
| Code |
MEDI.P-381 |
| Subject |
EGFR exon 20 insertion mutations to NSCLC |
| Authors |
Jiwon Kim, Chong Hak Chae1, Kwangho Lee1,*
medicinal chemistry and pharmacology, Korea Research Institute of Chemical Technology, Korea
1Korea Research Institute of Chemical Technology, Korea
|
| Abstract |
Non-small cell lung cancer (NSCLC) is one of the leading causes of cancer-related death globally. Exon 20 insertion mutations are the third EGFR mutations in NSCLC. It reportedly relates from 1.5% to 10 % of all EGFR mutations. Most of the mutations occur at the short loop connecting the αC-helix and β4 strand after Methionine 766. NSCLC patients caused by Exon 20 insertion mutations have received little benefits with the approved EGFR first-generation TKIs. So, there is unmet medical needs for exon 20 insertion mutation inhibitors for NSCLC patients. So far the detail mechanism for this mutation to EGFR overexpression is not fully understood. Cell-based mutation screening reveals the exact location, length, and sequence of the insert mutation matter. Also, it was found that it is important for ligand-independent EGFR activation and down signaling pathway. As a result, N771 P772 INSN, D770N771 INSG, D770> GY were identified as the major factors activating EGFR. |
| E-mail |
rlawl22@krict.re.kr |
|
123rd General Meeting of the KCS