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The Daniel Bachovchin Lab: Publications

View a full listing of Daniel Bachovchin’s journal articles.


28.  Buckley B.J.; Aboelela, A.; Minaei, E.; Jiang, L.X.; Xu, Z.; Ali, U; Fildes, K; Cheung, C.Y.; Cook, S.M.; Johnson, D.C.; Bachovchin, D.A.; Cook, G.M.; Apte, M.; Huang, M.; Ranson, M.; Kelso, M.J. “6-Substituted Hexamethylene Amiloride (HMA) Derivatives as Potent and Selective Inhibitors of the Human Urokinase Plasminogen Activator for Use in Cancer.” J Med Chem. 2018, in press.

27.  Johnson, D. C. *; Taabazuing, C. Y. *; Okondo, M. C.; Chui, A. J.; Rao, S. D.; Brown, F. C; Reed, C.; Peguero, E.; de Stanchina, E.; Kentsis, A.; Bachovchin, D. A. # “DPP8/9 inhibitor-induced pyroptosis for treatment of acute myeloid leukemia.” Nat Med. 2018, 24, 1151-1156.

26.  Okondo, M. C.*; Rao, S. D.*; Taabazuing, C. Y.*; Chui, A. J.; Poplawski, S. E.; Johnson, D. C.; Bachovchin, D. A. # “Inhibition of Dpp8/9 Activates the Nlrp1b Inflammasome.” Cell Chem Biol. 2018, 25, 262-267.

25.  Goel, P.; Jumpertz, T.; Mikles, D.C.; Tichá, A.; Nguyen, M.T.N.; Verhelst, S.; Hubalek, M.; Johnson, D.C.; Bachovchin, D.A.; Ogorek, I.; Pietrzik, C.U.; Strisovsky, K.; Schmidt, B.; Weggen, S. “Discovery and Biological Evaluation of Potent and Selective N-Methylene Saccharin-Derived Inhibitors for Rhomboid Intramembrane Proteases.” Biochemistry. 2017, 56, 6713-6725.

24.  Tichá, A.; Stanchev, S.; Vinothkumar, K.R.; Mikles, D.C.; Pachl, P.; Began, J.; Škerle, J.; Švehlová, K.; Nguyen, M.T.N.; Verhelst, S.H.L.; Johnson, D.C.; Bachovchin, D.A.; Lepšík, M.; Majer, P.; Strisovsky, K. “General and Modular Strategy for Designing Potent, Selective, and Pharmacologically Compliant Inhibitors of Rhomboid Proteases.” Cell Chem Biol. 2017, 24, 1523-1536.

23.  Taabazuing, C. Y.; Okondo, M. C.; Bachovchin, D. A. # “Pyroptosis and apoptosis pathways engage in bidirectional crosstalk in monocytes and macrophages.” Cell Chem Biol. 2017, 24, 507-514.

22. Keckesova, Z.; Donaher, J.; DeCock, J.; Freinkman, E.; Lingrell, S.; Bachovchin, D. A.; Bierie, B.; Tischler, V.; Noske, A.; Reinhardt, F.; Thiru, P.; Golub, T.R.; Vance, J., Okondo, M.; Weinberg, R. “LACTB, a tumor suppressor that modulates lipid metabolism and differentiation.” Nature. 2017, 543, 681-686.

21. Okondo, M.C.; Johnson,D. C., Sridharan, R., Go, E. B., Chui, A. J., Wang, M. S., Poplawski, S. E., Wu, W., Liu, Y.; Lai, J. H.; Sanford, D. G.; Arciprete, M. O.; Golub, T. R.; Bachovchin, W. W.; Bachovchin, D. A.# “Inhibition of DPP8/9 induces pro-caspase-1-dependent pyroptosis in monocytes and macrophages.” Nat Chem Biol. 2017, 13, 46-53.

20.  Hatzios, S. K.; Abel, S.; Martell, J.; Hubbard, T.; Sasabe, J.; Munera, D.; Clark, L.; Bachovchin, D. A.; Qadri, F.; Ryan,  E. T.; Davis , B. M.; Weerapana, E.; Waldor, M. K. “Chemoproteomic profiling of host and pathogen enzymes active in cholera.” Nat Chem Biol. 2016, 12, 268-274.

19.  Zhao, N.; Darby, C.; Small, J.; Bachovchin, D. A.; Jiang, X.; Burns-Huang, K.; Botella, H.; Ehrt, S.; Boger, D.; Anderson, E.; Cravatt, B. F.; Speers, A.; Fernandez-Vega, V.; Rosen, H.; Spicer, T.; Nathan, C. “A target-based screen against mycobacterial acid resistance protease implicates an additional periplasmic serine protease in regulation of intrabacterial pH homeostasis in Mycobacterium tuberculosis.” ACS Chem Biol. 2015, 10, 364-371.

18.  Bachovchin, D. A.; Koblan, L. W.; Wu, W.; Liu, Y.; Li, Y.; Zhao, P.; Woznica, I.; Shu, Y.; Lai, J. H.; Poplawski, S. E.; Kiritsy, C. P.; Healey, S. E.; DiMare, M.; Sanford, D. G.; Munford, R. S.; Bachovchin, W. W.; Golub, T. R. “A high-throughput, multiplexed assay for superfamily-wide profiling of enzyme activity.” Nat Chem Biol. 2014, 10, 656-663.

17.  Liu, X.; Dix, M.; Speers, A.; Bachovchin, D. A.; Zuhl, A. M.; Cravatt, B. F.; Kodadek, T. “Rapid development of a potent photo-triggered inhibitor of the serine hydrolase RBBP9.” ChemBioChem. 2012, 13, 2082-2093.

16.  Adibekian, A.; Martin, B.; Chang, J. W.; Hsu, K. L.; Tsuboi, K.; Bachovchin, D. A.; Speers, A. E.; Brown, S. J.; Spicer, T.; Fernandez-Vega, V.; Rosen, H.; Cravatt, B. F. “Confirming target engagement of reversible inhibitors in vivo by kinetically tuned activity-based probes.” J Am Chem Soc. 2012, 134, 10345-10348.

15.  Dillon, M. B.; Bachovchin, D. A.; Brown, S. J.; Finn, M. J.; Rosen, H.; Cravatt, B. F.; Mowen, K. A. “Novel inhibitors for PRMT1 discovered by high-throughput screening using activity-based fluorescence polarization.” ACS Chem Biol. 2012, 7, 1198-1204.

14.  Zuhl, A. M.; Mohr, J. T.; Bachovchin, D. A.; Niessen, S.; Hsu, K. L.; Berlin, J. M.; Dochnahl, M.; Lopez-Alberca, M. P.; Fu, G. C.; Cravatt, B. F. “Competitive activity-based protein profiling identifies aza-b-lactams as a versatile chemotype for serine hydrolase inhibition.” J Am Chem Soc. 2012, 134, 5068-5071.

13.  Bachovchin, D. A.; Cravatt, B. F. “The pharmacological landscape and therapeutic potential of serine hydrolases.” Nat Rev Drug Discov. 2012, 11, 52-68.

12.  Tsuboi, K.; Bachovchin, D. A.; Speers, A. E.; Spicer, T. P.; Fernandez-Vega, V.; Hodder, P.; Rosen, H.; Cravatt, B. F. “Potent and selective inhibitors of glutathione S-transferase omega 1 that impair cancer drug resistance.” J Am Chem Soc. 2011, 133, 16605-16616.

11.  Lone, A. M.; Bachovchin, D. A.; Westwood, D.; Speers, A. E.; Spicer, T. P.; Fernandez-Vega, V.; Chase, P.; Hodder, P. S.; Rosen, H.; Cravatt, B. F.; Saghatelian, A. “A substrate-free activity-based protein profiling screen for the discovery of selective PREPL inhibitors.” J Am Chem Soc. 2011, 133, 11665-11674.

10.  Bachovchin, D. A.*; Zuhl, A. M.*; Speers, A. E.; Wolfe, M. R.; Weerapana, E.; Brown, S. J.; Rosen, H.; Cravatt, B. F. “Discovery and optimization of sulfonyl acrylonitriles as selective, covalent inhibitors of protein phosphatase methylesterase-1.J Med Chem. 2011, 54, 5229-5226.

9.  Adibekian, A.; Martin, B. R.; Wang, C.; Hsu, K.; Bachovchin, D. A.; Niessen, S.; Hoover, H.; Cravatt, B. F. “Click-generated triazole ureas as a versatile scaffold for ultrapotent in vivo-active serine hydrolase inhibitors.” Nat Chem Biol. 2011, 7, 469-478.

8.  Bachovchin, D. A.; Mohr, J. T.; Speers, A. E.; Wang, C.; Berlin, J. M.; Spicer, T. P.; Fernandez-Vega, V.; Chase, P.; Hodder, P. S.; Schürer, S. C.; Nomura, D. K.; Rosen, H.; Fu, G. C.; Cravatt, B. F. “Academic cross-fertilization by public screening yields a remarkable class of protein phosphatase methylesterase-1 inhibitors.” Proc Natl Acad Sci. 2011, 108, 6811-6816.

7.  Weerapana, E.*; Wang, C.*; Simon, G. M.; Khare, S.; Richter, F.; Dillon, M. B.; Bachovchin, D. A.; Mowen, K.; Baker, D.; Cravatt, B. F. “Quantitative reactivity profiling predicts functional cysteines in native and designed proteins.” Nature. 2010, 468, 790-795.

6.  Bachovchin, D. A.*;  Ji, T.*; Li, W.*; Simon, G. M.; Hoover, H.; Niessen, S.; Cravatt, B. F. “A superfamily-wide portrait of serine hydrolase inhibition achieved by library-versus-library screening.” Proc Natl Acad Sci. 2010, 107, 20941-20946. 

5.  Knuckley, B.; Jones, J. E.; Bachovchin, D. A.; Slack, J.; Causey, C. P.; Brown, S. J.; Rosen, H.; Cravatt, B. F.; Thompson, P. R. “A Fluopol-ABPP HTS Assay to Identify PAD Inhibitors.” Chem Comm. 2010, 46, 7175-7177.

4.  Bachovchin, D. A.; Wolfe, M. R.; Masuda, K.; Brown, S. J.; Spicer, T. P.; Fernandez-Vega, V.; Chase, P.; Hodder, P.S.; Rosen, H.; Cravatt, B. F. “Oxime esters as selective, covalent inhibitors of the serine hydrolase retinoblastoma-binding protein 9 (RBBP9).” Bioorg Med Chem Lett. 2010, 20, 2254-2258.

3.  Bachovchin, D. A.; Brown, S. J.; Rosen, H.; Cravatt, B. F.; “Identification of selective inhibitors of uncharacterized enzymes by high-throughput screening with fluorescent activity-based probes.” Nat. Biotechnol. 2009, 27, 387-394.

2.  Fraunhoffer, K. J.; Bachovchin, D. A.; White, M.C. “Hydrocarbon oxidation vs. C-C Bond forming approaches for efficient syntheses of oxygenated molecules.” Org Lett. 2005, 7, 223-226.

1.  Haddad, K. C.; Sudmeier, J. L.; Bachovchin, D. A.; Bachovchin, W.W.; “a-lytic protease can exist in two separately stable conformations with different His57 mobilities and catalytic activities.” Proc Natl Acad Sci. 2005, 102, 1006-1011.

 

*Equal contribution

# Corresponding author