Phone: 491-7628
Fax: 491-1815
Email: Michio.Kurosu@colostate.edu
Office: B222 Microbiology Building
Lab: B305 Microbiology Building

 

Education

• Research Fellow, Harvard University
• Ph.D., Osaka University
• M.Sc., Osaka University
• B.Sc., Tokyo University of Pharmacy and Life Science

Research Interests

Our group has a broad interest in target-oriented rational drug design and bioorganic chemistry.

• Rational Drug-lead Design
  • Target Selection & Validation
    We are working primarily on MDR-TB and MDR-Gram-positive drug targets whose 3D structures have not been previously determined. We are interested in electron transport associated proteins, glycosyltrasferases, fatty acid synthease, peptidoglycan synthease, and kinases.
  • Lead Generation
    Based on (hypothetical) biosynthetic intermediates we design lead compounds for target proteins. We try to eliminate possible cross-reactivates against none-targeted proteins at early stage of drug discovery.
    We use a variety of lead generation techniques, including scaffold-based chemical screening, and a computational technique known as virtual ligand screening with closely related target proteins that have been characterized by X-ray crystallography.
  • Lead Optimization
    Generation of small optimized library is our foundation for optimizing lead compounds. We typically deliver 100-150 molecules on polymer-support.
• Bioorganic Chemistry
  • We are interested in unusual biological transformation found in bacterial system. We are currently elucidating a formal decarboxylative carbon-aromatic bond forming reaction found in the menaquinone synthesis. We are also interested in the decarboxylative pyruvate addition to aldehydes to form optically pure α-hydroxy ketones. Optimization of these reactions that can be utilized in the syntheses of a variety of substrates and immobilization of biocatalysts are our current goal.
• Development of Polymer-supported Chemistries
  • We are developing novel linkers for polymer-supported chemistries. Novel linkers possessing appropriate spacers are indispensable for generating library molecules efficiently. We are currently demonstrating our linkers in the syntheses of lipid I and II, and their analogues.

Recent Patents

• Menaquine A Inhibitors, Kurosu, M.; Crick, D. C. US Patent 2007 pending.
• A New Linker for Solid-Phase Organic Synthesis, Kurosu, M.; Crick, D. C. US Provisional Patent Application, 2007.

Selected Publications

Pub Med for Kurosu M.

• Polymer-Supported (2,6-Dichloro-4-alkoxyphenyl)(2,4-dichlorophenyl)methanol: A New Linker for Solid-Phase Organic Synthesis, Kurosu, M.; Biswas, K.; Crick, D. C. Org. Lett. 2007, 9, 1141.
• Chemoenzymatic Synthesis of Park's Nucleotide: Towards the Development of High-throughput Screening for MraY Inhibitors, Kurosu, M.; Mahapatra, S.; Narayanasamy, P.; Crick, D. C. Tetrahedron Lett. 2007, 48, 799.
• Synthetic Studies Towards the Generation of Uridine-Amino Alcohol-Based Small Optimized Library, Kurosu, M.; Narayanasamy, P.; Crick, D. C. Heterocycles 2007, in press.
• Ganglioside GM3 Derivatives with Truncated Ceramide Moiety: Facial Synthesis and Inhibitiory Activity Against KB Cell Growth, Kurosu, M.; Kitagawa, I. J. Carbohydrate.Chem. 2006, 25, 427.
• Novel Strategy for Oligopeptide Synthesis Using a Polymer-supported Ammonium Fluoride, Kurosu, M.; Crick, D. C. Tetrahedron Lett. 2006, 47, 5325.
• Small-Molecule Microarrays: Development of Novel Linkers and an Efficient Detection Method for Bound Proteins, Kurosu, M.; Mowers, W. A. Bioorganic & Medicinal Chemistry Letters 2006, 16, 3392.
• Fe/Cr-and Co/Cr Mediated catalytic Asymmetric 2-Haloallylations of Aldehydes, Kurosu, M.; Lin, M-H.; Kishi, Y, J. Am. Chem. Soc. 2004, 126, 12248.
• Studies on the Total Synthesis of Batrachotoxin, Kurosu, M; Kishi, Y, Review: Yuki Gosei Kagaku Kyokaishi 2004, 62, 1205
• An Efficient Synthesis of Indane-Derived Bis(Oxazoline) and its Application to Hetero Diels-Alder Reaction on Polymer Support, Kurosu, M; Porter, J. R; Foley, M. A. Tetrahedron Lett. 2004, 45, 145.
• Highly Diastereofacial Anti-Aldol Reaction: Practical Synthesis of Optically Active anti-2-Alkyl-3-Hydroxycarboxylic Acid Ester Units, Kurosu, M.; Lorca, M. J. Org. Chem. 2001, 66, 1205.
• Selective Reduction of Aldehydes via BINOL-Zr Complex, Kurosu, M.; Lorca, M.; Kuhn D. Tetrahedron Lett. 2001, 42, 6243.
• A Practical Synthesis of the Lipophilic Side Chain of the Polyoxypeptins, Lorca, M. Kurosu, M. Tetrahedron Lett. 2001, 42, 2431.
• Expeditious Amide-Forming Reactions Using Thiol Esters, Kurosu, M. Tetrahedron Lett. 2000 41, 591.
• Total Synthesis of (±)-Batrachotoxinin A, Kurosu, M.; Marcin, L. R.; Grinsteiner, T. J.; Kishi. Y. J. Am. Chem. Soc. 1998, 120, 6627.