This subproject is one of many research subprojects utilizing the resources provided by a Center grant funded by NIH/NCRR. Primary support for the subproject and the subproject's principal investigator may have been provided by other sources, including other NIH sources. The Total Cost listed for the subproject likely represents the estimated amount of Center infrastructure utilized by the subproject, not direct funding provided by the NCRR grant to the subproject or subproject staff. Small molecules are valuable as tool compounds for biomedical research and as the beginning of drug discovery programs. High-throughput screening (HTS) provides a platform for the identification of commercial compound """"""""hits"""""""" having some desired biological properties, but truly useful compounds almost always require fine-tuning through reiterative analogue design and synthesis. A Medicinal Chemistry Core (MDC) is proposed to carry out these activities in conjunction with the work of the HTS Core and in collaboration with the COBRE Center and other researchers. The tasks of the Medicinal Chemistry Core will be (1) to perform synthesis of known compounds necessary for biochemical studies, (2) to design and synthesize novel drug compounds as probes for ongoing studies, (3) to work with the HTS Core and its biology collaborators in carrying out optimization of hits obtained in screening campaigns, and (4) to synthesize fluorescent or affinity tagged analogs of existing probes when necessary for cell localization or target identification studies. A Medicinal Chemistry Core (MDC)will fine-tune compounds through reiterative analogue design and synthesis in conjunction with the work of the HTS Core and in collaboration with the COBRE Center and other researchers.

Agency
National Institute of Health (NIH)
Institute
National Center for Research Resources (NCRR)
Type
Center Core Grants (P30)
Project #
5P30RR030926-02
Application #
8364922
Study Section
Special Emphasis Panel (ZRR1-RI-2 (01))
Project Start
2011-06-01
Project End
2012-05-31
Budget Start
2011-06-01
Budget End
2012-05-31
Support Year
2
Fiscal Year
2011
Total Cost
$234,274
Indirect Cost
Name
University of Kansas Lawrence
Department
Pharmacology
Type
Schools of Pharmacy
DUNS #
076248616
City
Lawrence
State
KS
Country
United States
Zip Code
66045
Yu, Jia; Lan, Lan; Lewin, Seth J et al. (2017) Identification of novel small molecule Beclin 1 mimetics activating autophagy. Oncotarget 8:51355-51369
Gold, Ben; Smith, Robert; Nguyen, Quyen et al. (2016) Novel Cephalosporins Selectively Active on Nonreplicating Mycobacterium tuberculosis. J Med Chem 59:6027-44
Gowthaman, Ragul; Miller, Sven A; Rogers, Steven et al. (2016) DARC: Mapping Surface Topography by Ray-Casting for Effective Virtual Screening at Protein Interaction Sites. J Med Chem 59:4152-70
Wu, Xiaoqing; Lan, Lan; Wilson, David Michael et al. (2015) Identification and validation of novel small molecule disruptors of HuR-mRNA interaction. ACS Chem Biol 10:1476-84
Lan, Lan; Appelman, Carl; Smith, Amber R et al. (2015) Natural product (-)-gossypol inhibits colon cancer cell growth by targeting RNA-binding protein Musashi-1. Mol Oncol 9:1406-20
Shishido, Stephanie N; Delahaye, Adélaïde; Beck, Amanda et al. (2014) The anticancer effect of PQ1 in the MMTV-PyVT mouse model. Int J Cancer 134:1474-83
Shishido, Stephanie N; Prasain, Keshar; Beck, Amanda et al. (2013) Bioavailability and efficacy of a gap junction enhancer (PQ7) in a mouse mammary tumor model. PLoS One 8:e67174
Johnson, David K; Karanicolas, John (2013) Druggable protein interaction sites are more predisposed to surface pocket formation than the rest of the protein surface. PLoS Comput Biol 9:e1002951
Kambhampati, Suman; Rajewski, Roger A; Tanol, Mehmet et al. (2013) A second-generation 2-Methoxyestradiol prodrug is effective against Barrett's adenocarcinoma in a mouse xenograft model. Mol Cancer Ther 12:255-63
Diaz, Francisco J; McDonald, Peter R; Roy, Anuradha et al. (2013) Compound ranking based on a new mathematical measure of effectiveness using time course data from cell-based assays. Comb Chem High Throughput Screen 16:168-79

Showing the most recent 10 out of 19 publications