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| Type |
Symposium |
| Area |
The Cutting Edge of Drug Discovery Chemistry |
| Room No. |
Room 304 |
| Time |
THU 16:10-16:40 |
| Code |
MEDI-2 |
| Subject |
Development of NOV1701, direct c-Myc-DNA inhibitor, for novel anti-cancer treatment |
| Authors |
Hwan Jung Lim
Information-Based Drug Research Center, Korea Research Institute of Chemical Technology, Korea |
| Abstract |
c-Myc has been known as one of the most potent oncoproteins. According to the report in 2005, more than 1/7 cancer deaths in US were related to deregulated c-Myc. Moreover, there are large numbers of studies which showed that c-Myc amplification induced diverse cancers, such as gastric cancer, colon cancer, small cell lung cancer, breast cancer, and leukemia.
Although these clear evidences that c-Myc could be an effective target to develop a new anti-cancer drug, direct and selective regulation of c-Myc by a small-molecule is believed to be almost impossible. A few of direct c-Myc inhibitors such as F4 were reported, but none of them is enough to be a preclinical candidate. Other molecular targets such as BRD4 and SUMO activating enzyme 1/2 (SAE1/2) that can indirectly regulate c-Myc transcription has been actively pursued by many groups.
In this presentation, brief developmental history of our small-molecular direct inhibitor NOV1701 will be shown. NOV1701 showed exceptional potencies toward our in-vitro and in-vivo assay systems. To other transcription factors such as AP-1 and Max-Max homodimer, it showed very high selectivities. ADME-T studies showed that NOV1701 have proper drug-like properties with low toxicities. In xenograft studies, PO administrated NOV1701 showed exceptional anti-tumor effects without body weight loss.
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| E-mail |
indium@krict.re.kr |
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123rd General Meeting of the KCS