Groll M - Search Results

1

Leaving groups prolong the duration of 20S proteasome inhibition and enhance the potency of salinosporamides.

Manam RR, McArthur KA, Chao TH, Weiss J, Ali JA, Palombella VJ, Groll M, Lloyd GK, Palladino MA, Neuteboom ST, Macherla VR, Potts BC. Manam RR, et al. Among authors: groll m. J Med Chem. 2008 Nov 13;51(21):6711-24. doi: 10.1021/jm800548b. Epub 2008 Oct 22. J Med Chem. 2008. PMID: 18939815

2

Crystal structures of Salinosporamide A (NPI-0052) and B (NPI-0047) in complex with the 20S proteasome reveal important consequences of beta-lactone ring opening and a mechanism for irreversible binding.

Groll M, Huber R, Potts BC. Groll M, et al. J Am Chem Soc. 2006 Apr 19;128(15):5136-41. doi: 10.1021/ja058320b. J Am Chem Soc. 2006. PMID: 16608349

3

Snapshots of the fluorosalinosporamide/20S complex offer mechanistic insights for fine tuning proteasome inhibition.

Groll M, McArthur KA, Macherla VR, Manam RR, Potts BC. Groll M, et al. J Med Chem. 2009 Sep 10;52(17):5420-8. doi: 10.1021/jm900559x. J Med Chem. 2009. PMID: 19678642

4

Marizomib, a proteasome inhibitor for all seasons: preclinical profile and a framework for clinical trials.

Potts BC, Albitar MX, Anderson KC, Baritaki S, Berkers C, Bonavida B, Chandra J, Chauhan D, Cusack JC Jr, Fenical W, Ghobrial IM, Groll M, Jensen PR, Lam KS, Lloyd GK, McBride W, McConkey DJ, Miller CP, Neuteboom ST, Oki Y, Ovaa H, Pajonk F, Richardson PG, Roccaro AM, Sloss CM, Spear MA, Valashi E, Younes A, Palladino MA. Potts BC, et al. Among authors: groll m. Curr Cancer Drug Targets. 2011 Mar;11(3):254-84. doi: 10.2174/156800911794519716. Curr Cancer Drug Targets. 2011. PMID: 21247382 Free PMC article. Review.

5

Proteasome structure, function, and lessons learned from beta-lactone inhibitors.

Groll M, Potts BC. Groll M, et al. Curr Top Med Chem. 2011 Dec;11(23):2850-78. doi: 10.2174/156802611798281320. Curr Top Med Chem. 2011. PMID: 21824111 Review.

6

Peptido sulfonyl fluorides as new powerful proteasome inhibitors.

Brouwer AJ, Jonker A, Werkhoven P, Kuo E, Li N, Gallastegui N, Kemmink J, Florea BI, Groll M, Overkleeft HS, Liskamp RM. Brouwer AJ, et al. Among authors: groll m. J Med Chem. 2012 Dec 27;55(24):10995-1003. doi: 10.1021/jm301443r. Epub 2012 Dec 13. J Med Chem. 2012. PMID: 23170994

7

Dimerized linear mimics of a natural cyclopeptide (TMC-95A) are potent noncovalent inhibitors of the eukaryotic 20S proteasome.

Desvergne A, Genin E, Maréchal X, Gallastegui N, Dufau L, Richy N, Groll M, Vidal J, Reboud-Ravaux M. Desvergne A, et al. Among authors: groll m. J Med Chem. 2013 Apr 25;56(8):3367-78. doi: 10.1021/jm4002007. Epub 2013 Apr 17. J Med Chem. 2013. PMID: 23540790

8

Potent proteasome inhibitors derived from the unnatural cis-cyclopropane isomer of Belactosin A: synthesis, biological activity, and mode of action.

Kawamura S, Unno Y, List A, Mizuno A, Tanaka M, Sasaki T, Arisawa M, Asai A, Groll M, Shuto S. Kawamura S, et al. Among authors: groll m. J Med Chem. 2013 May 9;56(9):3689-700. doi: 10.1021/jm4002296. Epub 2013 Apr 22. J Med Chem. 2013. PMID: 23547757

9

Enzyme inhibition by hydroamination: design and mechanism of a hybrid carmaphycin-syringolin enone proteasome inhibitor.

Trivella DB, Pereira AR, Stein ML, Kasai Y, Byrum T, Valeriote FA, Tantillo DJ, Groll M, Gerwick WH, Moore BS. Trivella DB, et al. Among authors: groll m. Chem Biol. 2014 Jun 19;21(6):782-91. doi: 10.1016/j.chembiol.2014.04.010. Epub 2014 Jun 12. Chem Biol. 2014. PMID: 24930969 Free PMC article.

10

Structure-Based Design of β5c Selective Inhibitors of Human Constitutive Proteasomes.

Xin BT, de Bruin G, Huber EM, Besse A, Florea BI, Filippov DV, van der Marel GA, Kisselev AF, van der Stelt M, Driessen C, Groll M, Overkleeft HS. Xin BT, et al. Among authors: groll m. J Med Chem. 2016 Aug 11;59(15):7177-87. doi: 10.1021/acs.jmedchem.6b00705. Epub 2016 Aug 1. J Med Chem. 2016. PMID: 27438186

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