MIKIW 2019
April 12 - 14, 2019
The University of Kansas | Lawrence, KS
Keynote Speaker:
Nicholas A. Meanwell, Ph.D., FRSC, Executive Director Bristol-Myers Squibb
Details
The first Medicinal Chemistry Meeting-in-Miniature was organized by faculty from the Departments of Medicinal Chemistry and Pharmacognosy at the Universities of University of Minnesota, University of Illinois at Chicago, The University of Kansas, and The University of Iowa in 1963. Since then, the Departments of Medicinal Chemistry and Pharmacognosy at these universities have alternately hosted the MIKI meeting. MIKI is the longest running and largest regional medicinal chemistry meeting in the U.S., and brings together over 200 graduate students, post-doctoral fellows, and faculty members from the four universities on an annual basis. In 2018, the University of Wisconsin-Madison joined MIKI, giving the conference the new name MIKIW. This year, the graduate students at The University of Kansas are excited to host the 57th Annual MIKIW Meeting and continue this great tradition.
Graduate students from the hosting university have the opportunity to organize and moderate the entire meeting, providing the valuable experience of coordinating a professional event. In addition, participating students receive professional experiences by delivering oral and/or poster presentations, as well as vital networking opportunities. Furthermore, these annual meetings also act as a catalyst for sharing and exchanging ideas among students, postdoctoral researchers, and faculty of the different universities. The meeting features a keynote address from a distinguished scientist in academia, industry, or government, who is a leader in the field of medicinal chemistry.
MIKI Founders
| Minnesota | Illinois | Kansas | Iowa |
|---|---|---|---|
| O. Gisvold | L. Bauer | M.P. Mertes | J.G. Cannon |
| P.S. Portoghese | D. Coviello | E.E. Smissman | D.T. Witiak |
| T.O. Soine | R. Daniels | R.A. Wiley | |
| J.E. Gearien |
MIKIW 2019 Schedule
Friday, April 12, 2019
| Time | Agenda Item | Location |
|---|---|---|
| 3:00 – 6:00 p.m. | • Registration open • Hotel check-in | Springhill Suites » - Minnesota and Illinois Quality Inn and Suites » - Iowa Days Inn » - Wisconsin |
| 7:00 p.m. | Welcome reception | Arterra Event Gallery |
Saturday, April 13, 2019
* ISB = KU Integrated Science Building
| Time | Agenda Item | Location |
|---|---|---|
| 8:00 – 8:40 a.m. | Breakfast and poster setup | ISB Atrium |
| 8:40 – 9:00 a.m. | Opening remarks | ISB Auditorium |
| Oral presentation session 1 Moderators: Patrick Ross, Bo Han | ISB Auditorium | |
| 9:00 – 9:25 a.m. | Yuwen Yin Blake Peterson lab, KU Phorbol Carbamates as Novel Tools for Controlling Cellular Signal Transduction | |
| 9:25 – 9:50 a.m. | Arturo L. Aguirre Robert Kerns lab, UI Investigating Quinazoline-2,4-dione and Fluoroquinolone Scaffolds for Antibiotic Activity and Metabolic Stability | |
| 9:50 – 10:15 a.m. | Stephanie Blaszczyk Weiping Tang lab, UW-Madison S-Adamantyl Group Directed Site-Selective Acylation and Its Applications in the Streamlined Assembly of Oligosaccharides | |
| 10:15 – 10:40 a.m. | Kellan T. Passow Daniel A. Harki lab, UMN The Discovery of 4CIN: Indoles as a Platform for Novel Nucleoside Fluorophore Development | |
| 10:40 – 11:00 a.m. | Break | ISB Atrium |
| 11:00 a.m. – noon | Keynote address "Inhibitors of HIV-1 Maturation" Nicholas A. Meanwell, Ph.D., FRSC Dept. of Chemistry and Molecular Technologies, Bristol-Myers Squibb Research and Development | ISB Auditorium |
| 12:00 – 1:30 p.m. | Lunch and poster setup | ISB Atrium |
| Oral presentation session 2 Moderators: Sahishna Phaniraj, Bo Han | ISB Auditorium | |
| 1:30 – 1:55 p.m. | Jacob P. Sorrentino Ryan Altman lab, KU Fluorinated Dextromethorphan Analogs to Prevent the Formation of Psychoactive Metabolites | |
| 1:55 – 2:20 p.m. | Brian P. David Terry W. Moore lab, UIC Structure-Activity Relationship and Evaluation of Non-electrophilic NRF2 Activators in a Diabetic Mouse Model | |
| 2:20 – 2:45 p.m. | Muhammad M. Khalifa Jennifer E. Golden lab, UW-Madison Convergent Annulative Platform for the Synthesis of Ring-Fused Quinolinones | |
| 2:45 – 3:45 p.m. | Poster session: Odd numbered posters present | ISB Atrium |
| 3:45 – 4:45 p.m. | Poster session: Even numbered posters present | ISB Atrium |
| 4:45 – 5:15 p.m. | Faculty meeting | ISB 1160 |
| 6:00 – 7:00 p.m. | Faculty mixer (open bar) | Van Go inc. |
| 7:00 p.m. | Formal banquet dinner | Van Go inc. |
Sunday, April 14, 2019
* ISB = KU Integrated Science Building
| Time | Agenda Item | Location |
|---|---|---|
| Check-out of hotel prior to breakfast | Springhill Suites » - Minnesota and Illinois Quality Inn and Suites » - Iowa Days Inn » - Wisconsin | |
| 8:00 – 8:40 a.m. | Breakfast | ISB Atrium |
| Oral presentation session 3 Moderators: Patrick Ross, Bo Han | ISB Auditorium | |
| 8:40 - 9:05 a.m. | Erick J. Carlson Gunda I. Georg lab, UMN The Discovery and Characterization of Steroidal Blockers of CatSper | |
| 9:05 - 9:30 a.m. | Alanna Condren Laura Sanchez lab, UIC Biofilm Inhibition Alters Specialized Metabolism and Increases Virulence in Pseudomonas Aeruginosa | |
| 9:30 - 9:55 a.m. | Sanjay Bhattarai Michael S. Wolfe lab, KU Substrate transmembrane mimetic inhibitors of gamma-secretase: probes for chemical structural biology | |
| 9:55 - 10:20 a.m. | Pratik Rajesh Chheda Robert J. Kerns lab, UI Allosteric Inhibitors of Apicoplast DNA Polymerase: New Antimalarials That Bind a Novel Allosteric Binding Site | |
| 10:20 - 10:40 a.m. | Break | ISB Atrium |
| Oral presentation session 4 Moderators: Tomas Smith, Bo Han | ISB Auditorium | |
| 10:40 - 11:05 a.m. | Matthew Worth Jiaoyan Jiang lab, UW-Madison Covalent Inhibitors Target O-GlcNAc Transferase in Cells | |
| 11:05 - 11:30 a.m. | Ozgun Kilic Cartson Rick Wagner lab, UMN Nanorings with Engineered Fibronectins for Cancer Therapeutics | |
| 11:30 - 11:55 a.m. | Katherine E. Zink Laura M. Sanchez lab, UIC A Novel Imaging Mass Spectrometry Method for Identifying Preventative Approaches in High Grade Serous Ovarian Cancer | |
| 12:00 p.m. | • Concluding remarks • Box lunch served • Buses depart | ISB Atrium |
"Inhibitors of HIV-1 Maturation"
Nicholas A. Meanwell, Ph.D., FRSC
Dept. of Chemistry and Molecular Technologies, Bristol-Myers Squibb Research and Development
Abstract: Maturation of the HIV-1 capsid (CA) peptide by HIV-1 protease-mediated cleavage at the CA-SP1 junction is the final step in the formation of infectious virus capsid. A phenotypic screen identified the betulinic acid derivative bevirimat as an inhibitor specific to this step in virion production and this compound demonstrated antiviral effects in Phase 2a clinical trials. However, naturally-occurring polymorphisms proximal to the cleavage site conferred much reduced sensitivity to the effects of bevirimat in vitro which correlated with the clinical response. Guided by assays incorporating the natural polymorphisms, we identified GSK-3532795/BMS-955176 as a second generation HIV-1 maturation inhibitor that exhibits a broader spectrum of antiviral effect in vitro that translated into improved efficacy in clinical trials. In this presentation, we will describe the strategy and tactics adopted by the drug discovery team that led to the discovery of GSK-3532795/BMS-955176, the antiviral and pharmacokinetic profiles of the molecule and the results of early clinical studies.
Acknowledgements
The 57th Annual MIKIW Medicinal Chemistry Meeting would not be possible without the support of the following sponsors. The MIKIW 2019 Organizing Committee and the Department of Medicinal Chemistry at The University of Kansas express our appreciation and sincere gratitude for these generous financial contributions. Thank you to all of the 2019 MIKIW supporters!
Platinum-level Sponsors
- ACS Medicinal Chemistry Division
- Pfizer
Gold-level Sponsors
- KU School of Pharmacy
- Advion
- KU Chemical Biology of Infectious Disease
Silver-level Sponsors
- Waters
- Teledyne ISCO
- Deciphera
- The University of Kansas Cancer Center
- KU Madison & Lila Self Graduate Fellowship
- Biotage
- Vertex
- Corning
- KU Higuchi Bioscience Center
- Journal of Medicinal Chemistry
- Journal of Natural Products
- ACS Medicinal Chemistry Letters
- Abbvie
Bronze-level Sponsors
- Thincnext
- Strem Chemicals, Inc.
- Bristol-Myers Squibb
- Norell
- Avanti Polar Lipids, Inc.
- Orion Bioscience, Inc.
- Sekisui Xenotech
- BioTools
- KU Alumni Association
- New England Biolabs
The previous keynote speakers are among the most accomplished scientists. This group includes Nobel laureates, members of the National Academy of Sciences, leaders in the pharmaceutical industry, and many members of the ACS Medicinal Chemistry Division Hall of Fame. In 2019, we are pleased to have Dr. Nicholas A. Meanwell of Bristol-Myers Squibb deliver the keynote address.
Past Keynote Lectures
| Year | Host | Speaker | Association |
|---|---|---|---|
| 2018 | University of Illinois at Chicago | Dr. Michelle Arkin | University of California, San Francisco |
| 2017 | University of Minnesota | Dr. Uttam K. Tambar | UT Southwestern Medical Center |
| 2016 | The University of Iowa | Dr. Amy Hauck Newman | NIH-NIDA |
| 2015 | The University of Kansas | Dr. Bruce Roth | Genentech |
| 2014 | University of Illinois at Chicago | Dr. Paul Wender | Stanford University |
| 2013 | University of Minnesota | Dr. Marvin J. Miller | University of Notre Dame |
| 2012 | The University of Iowa | Dr. Heidi E. Hamm | Vanderbilt University |
| 2011 | The University of Kansas | Dr. Dennis C. Liotta | Emory University |
| 2010 | University of Illinois at Chicago | Dr. Tomáš Hudlický | Brock University |
| 2009 | University of Minnesota | Dr. Dale Boger | Scripps Research Institute |
| 2008 | The University of Iowa | Dr. Daniel Kahne | Harvard University |
| 2007 | The University of Kansas | Dr. Albert Padwa | Emory University |
| 2006 | University of Illinois at Chicago | Dr. William Fenical | University of California, San Diego |
| 2005 | University of Minnesota | Dr. Christopher Lipinski | Pfizer, Inc. |
| 2004 | The University of Iowa | Dr. Kenner Rice | NIH |
| 2003 | The University of Kansas | Dr. C. Dale Poulter | University of Utah |
| 2002 | University of Illinois at Chicago | Dr. Richard B. Silverman | Northwestern University |
| 2001 | University of Minnesota | Dr. Andrew Hamilton | Yale University |
| 2000 | The University of Iowa | Dr. Michael Marletta | University of Michigan |
| 1999 | The University of Kansas | Dr. Roger M. Friedinger | Merck Research Laboratories |
| 1998 | University of Illinois at Chicago | Dr. Richard A. Lerner | Scripps Research Institute |
| 1997 | University of Minnesota | Dr. John Montgomery | Biocryst Pharmaceuticals, Inc. |
| 1996 | The University of Iowa | Dr. David Nichols | Purdue University |
| 1995 | The University of Kansas | Dr. Paul Anderson | Dupont Merck Pharmaceuticals |
| 1994 | University of Illinois at Chicago | Dr. Arthur Patchett | Merck Research Laboratories |
| 1993 | University of Minnesota | Dr. Daniel Rich | University of Wisconsin, Madison |
| 1992 | The University of Iowa | Dr. Laurence Hurley | University of Texas, Austin |
| 1991 | The University of Kansas | Dr. Julius Rebek | Massachusetts Institute of Technology |
| 1990 | University of Illinois at Chicago | Dr. Koji Nakanishi | Columbia University |
| 1989 | University of Minnesota | Dr. John Katzenellenbogen | University of Illinois, Urbana-Champaign |
| 1988 | The University of Iowa | Dr. Carl Djerrasi | Stanford University |
| 1987 | The University of Kansas | Dr. William Roush | Indiana University |
| 1986 | University of Illinois at Chicago | Dr. Joseph Fried | University of Chicago |
| 1985 | University of Minnesota | Dr. David Triggle | SUNY Buffalo |
| 1984 | The University of Iowa | Dr. Alan Katritzky | University of Florida |
| 1983 | University of Wisconsin | Dr. Paul Bartlett | University of California, Berkeley |
| 1982 | The University of Kansas | Dr. Henry Rapoport | University of California, Berkeley |
| 1981 | University of Illinois at Chicago | Dr. Harry Wasserman | Yale University |
| 1980 | University of Minnesota | Dr. Eugene Jorgensen | University of California, San Francisco |
| 1979 | The University of Iowa | Dr. Alan Sartorelli | Yale University |
| 1978 | The University of Kansas | Dr. Albert Meyers | Colorado State University |
| 1977 | University of Illinois at Chicago | Dr. Heinz Floss | Purdue University |
| 1976 | University of Minnesota | Dr. Donald Jerina | NIH |
| 1975 | The University of Iowa | Dr. Everett May | NIH |
| 1974 | The University of Kansas | Dr. Marjorie Horning | Baylor University |
| 1973 | University of Illinois at Chicago | Dr. Arnold Brossi | Hoffman-LaRoche |
| 1972 | University of Minnesota | Dr. Gertrude Elion | Burroughs-Wellcome |
| 1971 | The University of Iowa | Dr. Bernard Belleau | University of Ottawa |
| 1970 | The University of Kansas | Dr. Corwin Hansch | Pomona College |
| 1969 | University of Illinois at Chicago | Dr. Everett Maynert | University of Illinois |
| 1968 | University of Minnesota | Dr. Bernard Baker | University of California, Santa Barbara |
| 1967 | The University of Iowa | Dr. Julius Axelrod | NIH |
| 1966 | The University of Kansas | Dr. Richard Schowen | The University of Kansas |
For questions about MIKIW 2019, contact KU Medicinal Chemistry at medchem@ku.edu.