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Chemistry and Biology of Cancer ----------- Drug Discovery in Academia Waldemar Priebe, Ph.D. Professor of Chemistry and Professor of Medicinal Chemistry.

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Presentation on theme: "Chemistry and Biology of Cancer ----------- Drug Discovery in Academia Waldemar Priebe, Ph.D. Professor of Chemistry and Professor of Medicinal Chemistry."— Presentation transcript:

1 Chemistry and Biology of Cancer ----------- Drug Discovery in Academia Waldemar Priebe, Ph.D. Professor of Chemistry and Professor of Medicinal Chemistry Destination Europe POLAND San Francisco December 7, 2012

2 2 Waldemar Priebe Professor, Medicinal Chemistry, UT MD Anderson Cancer CenterProfessor, Medicinal Chemistry, UT MD Anderson Cancer Center Over 25 years research experience in drug discovery and developmentOver 25 years research experience in drug discovery and development Founder or Founding Scientist of 5 Biotech Co.Founder or Founding Scientist of 5 Biotech Co. Aronex PharmaceuticalsAronex Pharmaceuticals Houston PharmaceuticalsHouston Pharmaceuticals Reata PharmaceuticalsReata Pharmaceuticals Moleculin, LLCMoleculin, LLC IntertechBioIntertechBio Licensed 7 compounds to industry with 4 drugs in clinical studies in humansLicensed 7 compounds to industry with 4 drugs in clinical studies in humans Over 180 research papers and 50 patentsOver 180 research papers and 50 patents Importance of Entrepreneurial Scientists to the Future of the EU and American Economy

3 TEXAS: an overview Population: 23 mln Labor Force: 11 mln Unemployment Rate: 4.2 % 2 nd Most Populous State 261,797 square miles of land (twice as Germany)

4 History of The University of Texas MD Anderson Cancer Center Monroe Dunaway Anderson created a charitable foundation in 1936. After his death, the MD Anderson Foundation provided funding and land to build a cancer hospital to serve the citizens of Texas.

5 LeMaistre Clinic Building opened in 1996 -- 15,756 sq. m.

6 Alkek Hospital Building opened in 1998 -- 70,212 sq. m.

7 Mays Clinical Building opened in 2004 --113,112 sq. m.

8 Texas Medical Center

9 Co-Branded Institutions Sister Institutions Breast Awareness and Research Partnerships MDACC UT MD Andersons Sister Institution Network

10 France Institut Gustave Roussy, Villejuif Germany German Cancer Research Center, Heidelberg Norway The Norwegian Cancer Consortium Poland The Polish Cancer Consortium Sister Institutions 10

11 Structure of the WP631–AC/GTAC/GT Complex K obs = 3 x 10 11 M -1 WP631 inhibits (at 60 nM) Sp1-activated transcription initiation in vitro WP631 1 J. Med. Chem., 40: 261-266, 1997 Biochemistry, 36: 5940-5946, 1997 Biochemistry, 36: 8663-8670, 1997 Biochemistry, 37: 1743-1753, 1998 Nucleic Acid Res., 27: 3402-3409, 1999 Curr. Med Chem. 8: 1-8, 2001 J. Biol. Chem., 276: 34486, 2001 Methods in Enzymology, Vol. 340, 529-555, 2001 Waldemar Priebe Biochem. Pharmacol. 63, 1251-1258, 2002 Eur. J. Biochem., 270: 764-770, 2003 Biochemistry. 43(23):7584-7592, 2004 Eur. J. Biochem., 271, 3556–3566, 2004 J. Med. Chem., 48, 8209-8219, 2005

12 Patient Examples in Phase I Trial of WP744 (RTA744, Berubicin) Before RTA 744 Oct 20, 2006 After 2 Cycles Patient 119 Achieves Partial Response After 2 Cycles of RTA 744 at a Dose of 7.5 mg/m 2 /day x 3 52 Year-old female Diagnosed with AO December 2000 Previous treatments include resection, RT, resection, Tmz, resection 81% reduction in lesion

13 Before RTA 744 Jan 20 After 2 Cycles Mar 7 After 6 Cycles July 11 After 7 Cycles Aug 1 Patient 104 Achieves Complete Response After 7 Cycles of RTA 744 at a Dose 2.4 mg/m 2 /day x 3 52 year-old male Recurrent GBM progressed from AA Previous treatments include resection, RT + Tmz, Tmz + Thalidomide + Accutane + Celebrex (8 cycles) Complete Response ongoing 3 years later Evidence of Clinical Activity of Berubicin (RTA744/WP744) in Phase I

14 F 18 -FDG PET Baseline Study F 18 -FDG PET Scan of Hot Tumor Treated with 2-DG 24 Hours Repeat F 18 -FDG PET Post Treatment with 2-DG


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