I accepted a position as a Principal Scientist at Genentech after collaborating with scientists here. I was impressed by their breadth of understanding of cancer biology. Moreover, I found it very appealing that Genentech focuses on the patient and the science, rather than on potential market size.

• My Focus

  I currently lead a group of chemists that attempts to develop small molecule inhibitors of the several oncology pathways that regulate mitosis, DNA damage repair and cell survival.

  We strive to create best-in-class and/or first-in-class drugs by working with a talented group of multidisciplinary scientists (drug metabolism, pharmacology, structural biology, toxicology, etc.) and by using various tools of drug discovery, such as structure based approaches, computational chemistry, measuring physical properties and building ADME SAR.

• Publications

  • Mechanistic Pharmacokinetic-Pharmacodynamic Modeling of BACE1 Inhibition in Monkeys: Development of a Predictive Model for Amyloid Precursor Protein Processing

    Drug Metabolism and Disposition, 2013, ISSN: 0090-9556

    Liu, Xingrong; Wong, Harvey; Scearce-Levie, Kimberly; Watts, Ryan; Coraggio, Melis; Shin, Young; Peng, Kun; Wildsmith, Kristin; Atwal, Jasvinder; Mango, Jason; Schauer, Stephen; Regal, Kelly; Hunt, Kevin; Thomas, Allen; Siu, Mike; Lyssikatos, Joseph; Deshmukh, Gauri; Hop, Cornelis

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  • Spirocyclic β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors: From hit to lowering of cerebrospinal fluid (CSF) amyloid β in a higher species

    Journal of Medicinal Chemistry, 2013, ISSN: 0022-2623

    Hunt, Kevin W.; Cook, Adam W.; Watts, Ryan J.; Clark, Christopher T.; Vigers, Guy; Smith, Darin; Metcalf, Andrew T.; Gunawardana, Indrani W.; Burkard, Michael; Cox, April A.; Geck Do, Mary K.; Dutcher, Darrin; Thomas, Allen A.; Rana, Sumeet; Kallan, Nicholas C.; Delisle, Robert K.; Rizzi, James P.; Regal, Kelly; Sammond, Douglas; Groneberg, Robert; Siu, Michael; Purkey, Hans; Lyssikatos, Joseph P.; Marlow, Allison; Liu, Xingrong; Tang, Tony P.

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  • Pyrimidoaminotropanes as Potent, Selective, and Efficacious Small Molecule Kinase Inhibitors of the Mammalian Target of Rapamycin (mTOR)

    Journal of Medicinal Chemistry, 2013, ISSN: 0022-2623

    Estrada, Anthony A; Shore, Daniel G; Blackwood, Elizabeth; Chen, Yung-Hsiang; Deshmukh, Gauri; Ding, Xiao; Dipasquale, Antonio G; Epler, Jennifer A; Friedman, Lori S; Koehler, Michael F T; Liu, Lichuan; Malek, Shiva; Nonomiya, Jim; Ortwine, Daniel F; Pei, Zhonghua; Sideris, Steve; St-Jean, Frederic; Trinh, Lan; Truong, Tom; Lyssikatos, Joseph P

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  • Evaluation of Metabolism and Disposition of GDC-0152 in Rats Using 14C Labeling Strategy at Two Different Positions: A Novel Formation of Hippuric Acid from 4-Phenyl-5-amino-1,2,3-thiadiazole

    Drug Metabolism and Disposition, 2012, ISSN: 0090-9556

    Yue, Qin; Mulder, Teresa; Rudewicz, Patrick J; Solon, Eric; Budha, Nageshwar; Ware, Joseph A; Lyssikatos, Joseph; Hop, Cornelis E C A; Wong, Harvey; Khojasteh, S Cyrus

     View on PubMed

  • Potent, selective, and orally bioavailable inhibitors of the Mammalian target of rapamycin kinase domain exhibiting single agent antiproliferative activity

    Journal of Medicinal Chemistry, 2012, ISSN: 0022-2623

    Koehler, Michael F T; Bergeron, Philippe; Blackwood, Elizabeth; Bowman, Krista K; Chen, Yung-Hsiang; Deshmukh, Gauri; Ding, Xiao; Epler, Jennifer; Lau, Kevin; Lee, Leslie; Liu, Lichuan; Ly, Cuong; Malek, Shiva; Nonomiya, Jim; Oeh, Jason; Ortwine, Daniel F; Sampath, Deepak; Sideris, Steve; Trinh, Lan; Truong, Tom; Wu, Jiansheng; Pei, Zhonghua; Lyssikatos, Joseph P

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  • Discovery and biological profiling of potent and selective mTOR inhibitor GDC-0349

    ACS Medicinal Chemistry Letters, 2012, ISSN:

    Pei, Zhonghua; Blackwood, Elizabeth; Liu, Lichuan; Malek, Shiva; Belvin, Marcia; Koehler, Michael F. T.; Ortwine, Daniel F.; Chen, Huifen; Cohen, Frederick; Kenny, Jane R.; Bergeron, Philippe; Lau, Kevin; Ly, Cuong; Zhao, Xianrui; Estrada, Anthony A.; Truong, Tom; Epler, Jennifer A.; Nonomiya, Jim; Trinh, Lan; Sideris, Steve; Lesnick, John; Bao, Linda; Vijapurkar, Ulka; Mukadam, Sophie; Tay, Suzanne; Deshmukh, Gauri; Chen, Yung-Hsiang; Ding, Xiao; Friedman, Lori S.; Lyssikatos, Joseph P.

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  • Discovery of potent and selective pyrazolopyrimidine Janus kinase 2 inhibitors

    Journal of Medicinal Chemistry, 2012, ISSN: 0022-2623

    Hanan, Emily J.; Van Abbema, Anne; Barrett, Kathy; Blair, Wade S.; Blaney, Jeff; Chang, Christine; Eigenbrot, Charles; Flynn, Sean; Gibbons, Paul; Hurley, Christopher A.; Kenny, Jane R.; Kulagowski, Janusz; Lee, Leslie; Magnuson, Steven R.; Morris, Claire; Murray, Jeremy; Pastor, Richard M.; Rawson, Tom; Siu, Michael; Ultsch, Mark; Zhou, Aihe; Sampath, Deepak; Lyssikatos, Joseph P.

     View on PubMed

  • Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors

    Journal of Medicinal Chemistry, 2012, ISSN: 0022-2623

    Estrada, Anthony A.; Liu, Xingrong; Baker-Glenn, Charles; Beresford, Alan; Burdick, Daniel J.; Chambers, Mark; Chan, Bryan K.; Chen, Huifen; Ding, Xiao; Dipasquale, Antonio G.; Dominguez, Sara L.; Dotson, Jennafer; Drummond, Jason; Flagella, Michael; Flynn, Sean; Fuji, Reina; Gill, Andrew; Gunzner-Toste, Janet; Harris, Seth F.; Heffron, Timothy P.; Kleinheinz, Tracy; Lee, Donna W.; Le Pichon, Claire E.; Lyssikatos, Joseph P.; Medhurst, Andrew D.; Moffat, John G.; Mukund, Susmith; Nash, Kevin; Scearce-Levie, Kimberly; Sheng, Zejuan; Shore, Daniel G.; Tran, Thuy; Trivedi, Naimisha; Wang, Shumei; Zhang, Shuo; Zhang, Xiaolin; Zhao, Guiling; Zhu, Haitao; Sweeney, Zachary K.

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  • Access to saturated fused pyrimidine derivatives via a flexible N - vinyl tertiary enamide synthesis.

    Synlett, 2011, no. 16, p. 2387-2391, eISSN: 1437-2096, ISSN: 0936-5214.

    Estrada, Anthony A; Lyssikatos, Joseph P; St, Jean Frederic; Bergeron, Philippe

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  • Non-oxime pyrazole based inhibitors of B-Raf kinase.

    Bioorganic & Medicinal Chemistry Letters, 2011, ISSN: 0960-894X

    Newhouse, B.J.; Hansen, J.D.; Grina, J.; Welch, M.; Topalov, G.; Littman, N.; Callejo, M.; Martinson, M.; Galbraith, S.; Laird, E.R.; Brandhuber, B.J.; Vigers, G.; Morales, T.; Woessner, R.; Randolph, N.; Lyssikatos, J.; Olivero, A.

  • Potent, Selective, and Orally Bioavailable Inhibitors of Mammalian Target of Rapamycin (mTOR) Kinase Based on a Quaternary Substituted Dihydrofuropyrimidine.

    Journal of Medicinal Chemistry, 2011, ISSN: 1520-4804

    Cohen, F.; Bergeron, P.; Blackwood, E.; Bowman, K.K.; Chen, H.; DiPasquale, A.G.; Epler, J.A.; Koehler, M.F.T.; Lau, K.; Lewis, C.; Liu, L.; Ly, C.Q.; Malek, S.; Nonomiya, J.; Ortwine, D.F.; Pei, Z.; Robarge, K.D.; Sideris, S.; Trinh, L.; Truong, T.; Wu, J.; Zhao, X.; Lyssikatos, J.P.

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  • Non-oxime inhibitors of B-Raf^V600E kinase.

    Bioorganic & Medicinal Chemistry Letters, 2010, ISSN: 0960-894X

    Ren, L.; Wenglowsky, S.; Miknis, G.; Rast, B.; Buckmelter, A.J.; Ely, R.J.; Schlachter, S.; Laird, E.R.; Randolph, N.; Callejo, M.; Martinson, M.; Galbraith, S.; Brandhuber, B.J.; Vigers, G.; Morales, T.; Voegtli, W.C.; Lyssikatos, J.

  • The Discovery of furo(2,3-c)pyridine-based indanone oximes as potent and selective B-Raf inhibitors.

    Bioorganic & Medicinal Chemistry Letters, 2010, ISSN: 0960-894X

    Buckmelter, A.J.; Ren, L.; Laird, E.R.; Rast, B.; Miknis, G.; Wenglowsky, S.; Schlachter, S.; Welch, M.; Tarlton, E.; Grina, J.; Lyssikatos, J.; Brandhuber, B.J.; Morales, T.; Randolph, N.; Vigers, G.; Martinson, M.; Callejo, M.

  • Mild and General One-Pot Reduction and Cyclization of Aromatic and Heteroaromatic 2-Nitroamines to Bicyclic 2H-Imidazoles.

    Synlett, 2010, ISSN: 0936-5214

    Hanan, E.J.; Chan, B.K.; Estrada, A.A.; Shore, D.G.; Lyssikatos, J.P.

  • Potent and selective pyrazole-based inhibitors of B-Raf kinase

    Bioorganic & Medicinal Chemistry Letters, 2008, ISSN: 0960-894X

    Hansen, J.D.; Grina, J.; Newhouse, B.; Welch, M.; Topalov, G.; Littman, N.; Callejo, M.; Gloor, S.; Martinson, M.; Laird, E.; Brandhuber, B.J.; Vigers, G.; Morales, T.; Woessner, R.; Randolph, N.; Lyssikatos, J.; Olivero, A.

• Education
  • University of California, Berkeley, Department of Chemistry Ph.D – 1992
  • College of William and Mary, Williamsburg, Department of Chemistry B.S – 1987