Our team's efforts made it to the cover of RSC Medicinal Chemistry in August 2020:
Structure-guided discovery of selective methionyl-tRNA synthetase inhibitors with potent activity against Trypanosoma brucei
Our team's latest paper on fighting Cryptosporidium was an editor's pick in AAC.
Buckner F.S., Ranade R.M., Gillespie J.R., Shibata S., Hulverson M.A., Zhang Z., Huang W., Choi R., Verlinde C.L.M.J., Hol W.G.J., Ochida A., Akao Y., Choy R.K.M., Van Voorhis W.C., Arnold S.L.M., Jumani R.S., Huston C.D., Fan F. (2019).Optimization of methionyl tRNA-synthetase inhibitors for treatment of Cryptosporidium infection.
Antimicrob. Agents Chemother. 63: e02061-18.
Our paper was the subject of the "Practical Fragments" blog:
Crystallography as a primary screen: the case of HisRS.
Koh C.Y., Kallur Siddaramaiah L., Ranade R., Nguyen J., Jian T., Zhang Z., Gillespie J.R., Buckner F.S., Verlinde C.L.M.J., Fan E., Hol W.G.J. (2015). A binding hotspot in the Trypanosoma cruzi
histidyl-tRNA synthetase revealed by fragment-based crystallographic cocktail screens. Acta Cryst. D71: 1684-1698.
Our latest paper on was the subject of a Nature Structural & Molecular Biology
News and Views (17, 541-543 (2010))
with the title
"A parasite calcium switch and Achilles' heel revealed"
.
Ojo K.K., Larson E.T., Keyloun K.R., Castaneda L.J., DeRocher A.E., Inampudi K.K., Kim J.E.,
Arakaki T.L., Murphy R., Zhang L., Maly D.J., Verlinde C.L.M.J., Buckner F.S., Parsons M., Hol
W.G.J., Merritt E.A., Van Voorhis W.C. (2010). A Unique Variation of the ATP binding site makes
Toxoplasma gondii Calcium-Dependent Protein Kinase 1 a drug target for selective kinase inhibitors.
Nature Struct. Mol. Biol. 17: 602-607.
Our pioneering work in "fragment-based ligand discovery" was highlighted
by Elizabeth A. Lipp in Genetic Engineering & Biotechnology News. (2008)
Link
We made it to the cover of Journal of Medicinal Chemistry
from July to December 2008.*
Bulbule V., Rivas K., Verlinde C.L.M.J., Van Voorhis W.C., Gelb M.H. (2008).
2-Oxo-Tetrahydroquinoline-Based Anti-Malarials with High Potency and
Metabolic Stability.
J. Med. Chem. 51, 384-387.
[PMID: 18198825 ].
