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Items: 41

1.

DPP9's Enzymatic Activity and Not Its Binding to CARD8 Inhibits Inflammasome Activation.

Griswold AR, Ball DP, Bhattacharjee A, Chui AJ, Rao SD, Taabazuing CY, Bachovchin DA.

ACS Chem Biol. 2019 Sep 20. doi: 10.1021/acschembio.9b00462. [Epub ahead of print]

PMID:
31525884
2.

DPP8/9 inhibitors are universal activators of functional NLRP1 alleles.

Gai K, Okondo MC, Rao SD, Chui AJ, Ball DP, Johnson DC, Bachovchin DA.

Cell Death Dis. 2019 Aug 5;10(8):587. doi: 10.1038/s41419-019-1817-5.

3.

A Chemical Strategy for Protease Substrate Profiling.

Griswold AR, Cifani P, Rao SD, Axelrod AJ, Miele MM, Hendrickson RC, Kentsis A, Bachovchin DA.

Cell Chem Biol. 2019 Jun 20;26(6):901-907.e6. doi: 10.1016/j.chembiol.2019.03.007. Epub 2019 Apr 18.

PMID:
31006619
4.

N-terminal degradation activates the NLRP1B inflammasome.

Chui AJ, Okondo MC, Rao SD, Gai K, Griswold AR, Johnson DC, Ball DP, Taabazuing CY, Orth EL, Vittimberga BA, Bachovchin DA.

Science. 2019 Apr 5;364(6435):82-85. doi: 10.1126/science.aau1208. Epub 2019 Mar 14.

PMID:
30872531
5.

6-Substituted Hexamethylene Amiloride (HMA) Derivatives as Potent and Selective Inhibitors of the Human Urokinase Plasminogen Activator for Use in Cancer.

Buckley BJ, Aboelela A, Minaei E, Jiang LX, Xu Z, Ali U, Fildes K, Cheung CY, Cook SM, Johnson DC, Bachovchin DA, Cook GM, Apte M, Huang M, Ranson M, Kelso MJ.

J Med Chem. 2018 Sep 27;61(18):8299-8320. doi: 10.1021/acs.jmedchem.8b00838. Epub 2018 Sep 7.

6.

DPP8/DPP9 inhibitor-induced pyroptosis for treatment of acute myeloid leukemia.

Johnson DC, Taabazuing CY, Okondo MC, Chui AJ, Rao SD, Brown FC, Reed C, Peguero E, de Stanchina E, Kentsis A, Bachovchin DA.

Nat Med. 2018 Aug;24(8):1151-1156. doi: 10.1038/s41591-018-0082-y. Epub 2018 Jul 2.

7.

Inhibition of Dpp8/9 Activates the Nlrp1b Inflammasome.

Okondo MC, Rao SD, Taabazuing CY, Chui AJ, Poplawski SE, Johnson DC, Bachovchin DA.

Cell Chem Biol. 2018 Mar 15;25(3):262-267.e5. doi: 10.1016/j.chembiol.2017.12.013. Epub 2018 Jan 27.

8.

Discovery and Biological Evaluation of Potent and Selective N-Methylene Saccharin-Derived Inhibitors for Rhomboid Intramembrane Proteases.

Goel P, Jumpertz T, Mikles DC, Tichá A, Nguyen MTN, Verhelst S, Hubalek M, Johnson DC, Bachovchin DA, Ogorek I, Pietrzik CU, Strisovsky K, Schmidt B, Weggen S.

Biochemistry. 2017 Dec 26;56(51):6713-6725. doi: 10.1021/acs.biochem.7b01066. Epub 2017 Dec 12.

9.

General and Modular Strategy for Designing Potent, Selective, and Pharmacologically Compliant Inhibitors of Rhomboid Proteases.

Tichá A, Stanchev S, Vinothkumar KR, Mikles DC, Pachl P, Began J, Škerle J, Švehlová K, Nguyen MTN, Verhelst SHL, Johnson DC, Bachovchin DA, Lepšík M, Majer P, Strisovsky K.

Cell Chem Biol. 2017 Dec 21;24(12):1523-1536.e4. doi: 10.1016/j.chembiol.2017.09.007. Epub 2017 Oct 26.

10.

Pyroptosis and Apoptosis Pathways Engage in Bidirectional Crosstalk in Monocytes and Macrophages.

Taabazuing CY, Okondo MC, Bachovchin DA.

Cell Chem Biol. 2017 Apr 20;24(4):507-514.e4. doi: 10.1016/j.chembiol.2017.03.009. Epub 2017 Apr 6.

11.

LACTB is a tumour suppressor that modulates lipid metabolism and cell state.

Keckesova Z, Donaher JL, De Cock J, Freinkman E, Lingrell S, Bachovchin DA, Bierie B, Tischler V, Noske A, Okondo MC, Reinhardt F, Thiru P, Golub TR, Vance JE, Weinberg RA.

Nature. 2017 Mar 30;543(7647):681-686. doi: 10.1038/nature21408. Epub 2017 Mar 22.

12.

DPP8 and DPP9 inhibition induces pro-caspase-1-dependent monocyte and macrophage pyroptosis.

Okondo MC, Johnson DC, Sridharan R, Go EB, Chui AJ, Wang MS, Poplawski SE, Wu W, Liu Y, Lai JH, Sanford DG, Arciprete MO, Golub TR, Bachovchin WW, Bachovchin DA.

Nat Chem Biol. 2017 Jan;13(1):46-53. doi: 10.1038/nchembio.2229. Epub 2016 Nov 7.

13.

Erratum: Chemoproteomic profiling of host and pathogen enzymes active in cholera.

Hatzios SK, Abel S, Martell J, Hubbard T, Sasabe J, Munera D, Clark L, Bachovchin DA, Qadri F, Ryan ET, Davis BM, Weerapana E, Waldor MK.

Nat Chem Biol. 2016 May 18;12(6):466. doi: 10.1038/nchembio0616-466. No abstract available.

PMID:
27191648
14.

Chemoproteomic profiling of host and pathogen enzymes active in cholera.

Hatzios SK, Abel S, Martell J, Hubbard T, Sasabe J, Munera D, Clark L, Bachovchin DA, Qadri F, Ryan ET, Davis BM, Weerapana E, Waldor MK.

Nat Chem Biol. 2016 Apr;12(4):268-274. doi: 10.1038/nchembio.2025. Epub 2016 Feb 22. Erratum in: Nat Chem Biol. 2016 May 18;12(6):466.

15.

Target-based screen against a periplasmic serine protease that regulates intrabacterial pH homeostasis in Mycobacterium tuberculosis.

Zhao N, Darby CM, Small J, Bachovchin DA, Jiang X, Burns-Huang KE, Botella H, Ehrt S, Boger DL, Anderson ED, Cravatt BF, Speers AE, Fernandez-Vega V, Hodder PS, Eberhart C, Rosen H, Spicer TP, Nathan CF.

ACS Chem Biol. 2015 Feb 20;10(2):364-71. doi: 10.1021/cb500746z. Epub 2014 Dec 5.

16.

Characterization of a Selective, Reversible Inhibitor of Lysophospholipase 2 (LYPLA2).

Adibekian A, Martin BR, Chang JW, Hsu KL, Tsuboi K, Bachovchin DA, Speers AE, Brown SJ, Spicer T, Fernandez-Vega V, Ferguson J, Cravatt BF, Hodder P, Rosen H.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2013 Apr 8 [updated 2014 Sep 18].

17.

A high-throughput, multiplexed assay for superfamily-wide profiling of enzyme activity.

Bachovchin DA, Koblan LW, Wu W, Liu Y, Li Y, Zhao P, Woznica I, Shu Y, Lai JH, Poplawski SE, Kiritsy CP, Healey SE, DiMare M, Sanford DG, Munford RS, Bachovchin WW, Golub TR.

Nat Chem Biol. 2014 Aug;10(8):656-63. doi: 10.1038/nchembio.1578. Epub 2014 Jul 6.

18.

Characterization of a Selective, Reversible Inhibitor of Lysophospholipase 1 (LYPLA1).

Adibekian A, Martin BR, Chang JW, Hsu KL, Tsuboi K, Bachovchin DA, Speers AE, Brown SJ, Spicer T, Fernandez-Vega V, Ferguson J, Cravatt BF, Hodder P, Rosen H.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2013 Apr 8 [updated 2014 Jan 13].

19.

Probe Development Efforts to Identify Novel Inhibitors of ABHD10.

Zuhl AM, Mohr JT, Speers AE, Bachovchin DA, Berlin JM, Spicer T, Fernandez-Vega V, Brown SJ, Ferguson J, Fu GC, Cravatt BF, Hodder P, Rosen H.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2011 Dec 6 [updated 2013 Mar 7].

20.

Rapid development of a potent photo-triggered inhibitor of the serine hydrolase RBBP9.

Liu X, Dix M, Speers AE, Bachovchin DA, Zuhl AM, Cravatt BF, Kodadek TJ.

Chembiochem. 2012 Sep 24;13(14):2082-93. doi: 10.1002/cbic.201200445. Epub 2012 Aug 20.

21.

Probe Development Efforts to Identify Novel Inhibitors of Protein Phosphatase Methylesterase-1 (PME-1).

Bachovchin DA, Speers AE, Brown SJ, Spicer TP, Fernandez-Vega V, Ferguson J, Mohr JT, Murphy J, Fu GC, Cravatt BF, Hodder PS, Rosen H.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2010 Aug 31 [updated 2011 Dec 12].

22.

Optimization and Characterization of an Inhibitor for Glutathione S-Tranferase Omega 1 (GSTO1).

Tsuboi K, Bachovchin DA, Speers AE, Brown SJ, Spicer T, Fernandez-Vega V, Ferguson J, Cravatt BF, Hodder P, Rosen H.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2010 Aug 31 [updated 2011 Dec 12].

23.

Confirming target engagement for reversible inhibitors in vivo by kinetically tuned activity-based probes.

Adibekian A, Martin BR, Chang JW, Hsu KL, Tsuboi K, Bachovchin DA, Speers AE, Brown SJ, Spicer T, Fernandez-Vega V, Ferguson J, Hodder PS, Rosen H, Cravatt BF.

J Am Chem Soc. 2012 Jun 27;134(25):10345-8. doi: 10.1021/ja303400u. Epub 2012 Jun 12.

24.

Novel inhibitors for PRMT1 discovered by high-throughput screening using activity-based fluorescence polarization.

Dillon MB, Bachovchin DA, Brown SJ, Finn MG, Rosen H, Cravatt BF, Mowen KA.

ACS Chem Biol. 2012 Jul 20;7(7):1198-204. doi: 10.1021/cb300024c. Epub 2012 Apr 20.

25.

Competitive activity-based protein profiling identifies aza-β-lactams as a versatile chemotype for serine hydrolase inhibition.

Zuhl AM, Mohr JT, Bachovchin DA, Niessen S, Hsu KL, Berlin JM, Dochnahl M, López-Alberca MP, Fu GC, Cravatt BF.

J Am Chem Soc. 2012 Mar 21;134(11):5068-71. doi: 10.1021/ja300799t. Epub 2012 Mar 8.

26.

The pharmacological landscape and therapeutic potential of serine hydrolases.

Bachovchin DA, Cravatt BF.

Nat Rev Drug Discov. 2012 Jan 3;11(1):52-68. doi: 10.1038/nrd3620. Review.

27.

Potent and selective inhibitors of glutathione S-transferase omega 1 that impair cancer drug resistance.

Tsuboi K, Bachovchin DA, Speers AE, Spicer TP, Fernandez-Vega V, Hodder P, Rosen H, Cravatt BF.

J Am Chem Soc. 2011 Oct 19;133(41):16605-16. doi: 10.1021/ja2066972. Epub 2011 Sep 27.

28.

A substrate-free activity-based protein profiling screen for the discovery of selective PREPL inhibitors.

Lone AM, Bachovchin DA, Westwood DB, Speers AE, Spicer TP, Fernandez-Vega V, Chase P, Hodder PS, Rosen H, Cravatt BF, Saghatelian A.

J Am Chem Soc. 2011 Aug 3;133(30):11665-74. doi: 10.1021/ja2036095. Epub 2011 Jul 12.

29.

Discovery and optimization of sulfonyl acrylonitriles as selective, covalent inhibitors of protein phosphatase methylesterase-1.

Bachovchin DA, Zuhl AM, Speers AE, Wolfe MR, Weerapana E, Brown SJ, Rosen H, Cravatt BF.

J Med Chem. 2011 Jul 28;54(14):5229-36. doi: 10.1021/jm200502u. Epub 2011 Jun 30.

30.

Click-generated triazole ureas as ultrapotent in vivo-active serine hydrolase inhibitors.

Adibekian A, Martin BR, Wang C, Hsu KL, Bachovchin DA, Niessen S, Hoover H, Cravatt BF.

Nat Chem Biol. 2011 May 15;7(7):469-78. doi: 10.1038/nchembio.579. Erratum in: Nat Chem Biol. 2012 Mar;8(3):318.

31.

Probe Report for RBBP9 Inhibitors - Probe 2.

Bachovchin DA, Speers AE, Brown SJ, Cravatt BF, V Fernandez-Vega, Spicer T, Mercer BA, Ferguson J, Hodder P, Rosen HR.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2009 Aug 20 [updated 2010 Oct 20].

32.

Probe Report for PME-1 Inhibitors.

Bachovchin DA, Speers AE, Zuhl AM, Brown SJ, Cravatt BF, Fernandez-Vega V, Spicer T, Mercer BA, Ferguson J, Hodder P, Rosen HR.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2010 Feb 26 [updated 2010 Oct 20].

33.

Probe Report for RBBP9 Inhibitors - Probe 1.

Brown SJ, Bachovchin DA, Cravatt BF, Fernandez-Vega V, Spicer T, Mercer BA, Hodder P, Rosen HR.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2009 Mar 13 [updated 2010 Sep 2].

34.

Academic cross-fertilization by public screening yields a remarkable class of protein phosphatase methylesterase-1 inhibitors.

Bachovchin DA, Mohr JT, Speers AE, Wang C, Berlin JM, Spicer TP, Fernandez-Vega V, Chase P, Hodder PS, Schürer SC, Nomura DK, Rosen H, Fu GC, Cravatt BF.

Proc Natl Acad Sci U S A. 2011 Apr 26;108(17):6811-6. doi: 10.1073/pnas.1015248108. Epub 2011 Mar 11.

35.

Quantitative reactivity profiling predicts functional cysteines in proteomes.

Weerapana E, Wang C, Simon GM, Richter F, Khare S, Dillon MB, Bachovchin DA, Mowen K, Baker D, Cravatt BF.

Nature. 2010 Dec 9;468(7325):790-5. doi: 10.1038/nature09472. Epub 2010 Nov 17.

36.

Superfamily-wide portrait of serine hydrolase inhibition achieved by library-versus-library screening.

Bachovchin DA, Ji T, Li W, Simon GM, Blankman JL, Adibekian A, Hoover H, Niessen S, Cravatt BF.

Proc Natl Acad Sci U S A. 2010 Dec 7;107(49):20941-6. doi: 10.1073/pnas.1011663107. Epub 2010 Nov 17.

37.

A fluopol-ABPP HTS assay to identify PAD inhibitors.

Knuckley B, Jones JE, Bachovchin DA, Slack J, Causey CP, Brown SJ, Rosen H, Cravatt BF, Thompson PR.

Chem Commun (Camb). 2010 Oct 14;46(38):7175-7. doi: 10.1039/c0cc02634d. Epub 2010 Aug 25.

38.

Oxime esters as selective, covalent inhibitors of the serine hydrolase retinoblastoma-binding protein 9 (RBBP9).

Bachovchin DA, Wolfe MR, Masuda K, Brown SJ, Spicer TP, Fernandez-Vega V, Chase P, Hodder PS, Rosen H, Cravatt BF.

Bioorg Med Chem Lett. 2010 Apr 1;20(7):2254-8. doi: 10.1016/j.bmcl.2010.02.011. Epub 2010 Feb 6.

39.

Identification of selective inhibitors of uncharacterized enzymes by high-throughput screening with fluorescent activity-based probes.

Bachovchin DA, Brown SJ, Rosen H, Cravatt BF.

Nat Biotechnol. 2009 Apr;27(4):387-94. doi: 10.1038/nbt.1531. Epub 2009 Mar 29. Erratum in: Nat Biotechnol. 2009 May;27(5):485.

40.

alpha-lytic protease can exist in two separately stable conformations with different His57 mobilities and catalytic activities.

Haddad KC, Sudmeier JL, Bachovchin DA, Bachovchin WW.

Proc Natl Acad Sci U S A. 2005 Jan 25;102(4):1006-11. Epub 2005 Jan 18.

41.

Hydrocarbon oxidation vs C-C bond-forming approaches for efficient syntheses of oxygenated molecules.

Fraunhoffer KJ, Bachovchin DA, White MC.

Org Lett. 2005 Jan 20;7(2):223-6.

PMID:
15646963

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