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Transcription factor drug target prediction technology based on KeyGen Human Genomic
Regulatory Database (HGRD)
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Transcription factors’ target discovery and drug design. http://www.keygentec.com.cn/grn
KeyGen’s drug discovery platform, HGRD, was built with the collaboration of Huada
Gene Research Center in Beijing. This database collected the information of over
two thousand genes including: promoter, enhancer, stop code, and transcription factor.
Human Genomic Regulation Database (HGRD) v1.0 received Software & Copyright
Registration Certificate 2003SR 8400 in Aug. 2003.
This database also provides:
• Information of protein-protein interaction and interaction binding site;
• Relationship between genes and diseases;
• The regulatory network of phenotype related multiple genes which will provide the platform for discovery of new drug targets and designs of new drugs for multi-gene
diseases at transcription level.
Recent Important Results of the use of KeyGen’s HGRD:
• Sixty-eight KGCGS series anti-cancer drug candidates have been designed by using
KeyGen’s HGRD.
• Thirty-eight sequences have been synthesized by DNA automatic synthesizer at the
laboratory level. The QC of sequence and purity has been set up.
• In-vitro assay proved that eleven of the new chemical entities (NCEs) had inhibitory
effect on multiple human cancer cells including lung cancer, breast cancer and hepatocarcinoma
cells. At very low dosage (nmol concentration) the inhibitory percentage is 68-82%.
• KGCGS102 showed significant anti-cancer effect with very low toxicity in nude
mice xenografts of human lung cancer and hepatocarcinoma with the inhibitory percentage
of 67% （ IC 50 is 5 mg/kg ）
• K102 has been patented in China, USA, Europe and Japan. Patent application number
is 02148492. 9, 10/411.692, 03007054.4 and 2003-87846, respectively.
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