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Items: 24

1.

Optimization of 3-Pyrimidin-4-yl-oxazolidin-2-ones as Allosteric and Mutant Specific Inhibitors of IDH1.

Levell JR, Caferro T, Chenail G, Dix I, Dooley J, Firestone B, Fortin PD, Giraldes J, Gould T, Growney JD, Jones MD, Kulathila R, Lin F, Liu G, Mueller A, van der Plas S, Slocum K, Smith T, Terranova R, Touré BB, Tyagi V, Wagner T, Xie X, Xu M, Yang FS, Zhou LX, Pagliarini R, Cho YS.

ACS Med Chem Lett. 2016 Dec 16;8(2):151-156. doi: 10.1021/acsmedchemlett.6b00334. eCollection 2017 Feb 9.

2.

Allosteric inhibition of SHP2 phosphatase inhibits cancers driven by receptor tyrosine kinases.

Chen YN, LaMarche MJ, Chan HM, Fekkes P, Garcia-Fortanet J, Acker MG, Antonakos B, Chen CH, Chen Z, Cooke VG, Dobson JR, Deng Z, Fei F, Firestone B, Fodor M, Fridrich C, Gao H, Grunenfelder D, Hao HX, Jacob J, Ho S, Hsiao K, Kang ZB, Karki R, Kato M, Larrow J, La Bonte LR, Lenoir F, Liu G, Liu S, Majumdar D, Meyer MJ, Palermo M, Perez L, Pu M, Price E, Quinn C, Shakya S, Shultz MD, Slisz J, Venkatesan K, Wang P, Warmuth M, Williams S, Yang G, Yuan J, Zhang JH, Zhu P, Ramsey T, Keen NJ, Sellers WR, Stams T, Fortin PD.

Nature. 2016 Jul 7;535(7610):148-52. Epub 2016 Jun 29.

PMID:
27362227
3.

Allosteric Inhibition of SHP2: Identification of a Potent, Selective, and Orally Efficacious Phosphatase Inhibitor.

Garcia Fortanet J, Chen CH, Chen YN, Chen Z, Deng Z, Firestone B, Fekkes P, Fodor M, Fortin PD, Fridrich C, Grunenfelder D, Ho S, Kang ZB, Karki R, Kato M, Keen N, LaBonte LR, Larrow J, Lenoir F, Liu G, Liu S, Lombardo F, Majumdar D, Meyer MJ, Palermo M, Perez L, Pu M, Ramsey T, Sellers WR, Shultz MD, Stams T, Towler C, Wang P, Williams SL, Zhang JH, LaMarche MJ.

J Med Chem. 2016 Sep 8;59(17):7773-82. doi: 10.1021/acs.jmedchem.6b00680. Epub 2016 Jul 12.

PMID:
27347692
4.

Structural and Functional Consequences of Three Cancer-Associated Mutations of the Oncogenic Phosphatase SHP2.

LaRochelle JR, Fodor M, Xu X, Durzynska I, Fan L, Stams T, Chan HM, LaMarche MJ, Chopra R, Wang P, Fortin PD, Acker MG, Blacklow SC.

Biochemistry. 2016 Apr 19;55(15):2269-77. doi: 10.1021/acs.biochem.5b01287. Epub 2016 Apr 11.

5.

The novolactone natural product disrupts the allosteric regulation of Hsp70.

Hassan AQ, Kirby CA, Zhou W, Schuhmann T, Kityk R, Kipp DR, Baird J, Chen J, Chen Y, Chung F, Hoepfner D, Movva NR, Pagliarini R, Petersen F, Quinn C, Quinn D, Riedl R, Schmitt EK, Schitter A, Stams T, Studer C, Fortin PD, Mayer MP, Sadlish H.

Chem Biol. 2015 Jan 22;22(1):87-97. doi: 10.1016/j.chembiol.2014.11.007. Epub 2014 Dec 24.

6.

Enzyme-dependent lysine deprotonation in EZH2 catalysis.

Kipp DR, Quinn CM, Fortin PD.

Biochemistry. 2013 Oct 1;52(39):6866-78. doi: 10.1021/bi400805w. Epub 2013 Sep 18.

PMID:
24000826
7.

Structure-efficiency relationship of [1,2,4]triazol-3-ylamines as novel nicotinamide isosteres that inhibit tankyrases.

Shultz MD, Majumdar D, Chin DN, Fortin PD, Feng Y, Gould T, Kirby CA, Stams T, Waters NJ, Shao W.

J Med Chem. 2013 Sep 12;56(17):7049-59. doi: 10.1021/jm400826j. Epub 2013 Aug 14.

PMID:
23879431
8.

Identification of NVP-TNKS656: the use of structure-efficiency relationships to generate a highly potent, selective, and orally active tankyrase inhibitor.

Shultz MD, Cheung AK, Kirby CA, Firestone B, Fan J, Chen CH, Chen Z, Chin DN, Dipietro L, Fazal A, Feng Y, Fortin PD, Gould T, Lagu B, Lei H, Lenoir F, Majumdar D, Ochala E, Palermo MG, Pham L, Pu M, Smith T, Stams T, Tomlinson RC, Touré BB, Visser M, Wang RM, Waters NJ, Shao W.

J Med Chem. 2013 Aug 22;56(16):6495-511. doi: 10.1021/jm400807n. Epub 2013 Aug 13.

PMID:
23844574
9.

[1,2,4]triazol-3-ylsulfanylmethyl)-3-phenyl-[1,2,4]oxadiazoles: antagonists of the Wnt pathway that inhibit tankyrases 1 and 2 via novel adenosine pocket binding.

Shultz MD, Kirby CA, Stams T, Chin DN, Blank J, Charlat O, Cheng H, Cheung A, Cong F, Feng Y, Fortin PD, Hood T, Tyagi V, Xu M, Zhang B, Shao W.

J Med Chem. 2012 Feb 9;55(3):1127-36. doi: 10.1021/jm2011222. Epub 2012 Feb 1.

PMID:
22260203
10.

beta-Hydroxylation of the aspartyl residue in the phytotoxin syringomycin E: characterization of two candidate hydroxylases AspH and SyrP in Pseudomonas syringae.

Singh GM, Fortin PD, Koglin A, Walsh CT.

Biochemistry. 2008 Oct 28;47(43):11310-20. doi: 10.1021/bi801322z. Epub 2008 Oct 1.

11.

Andrimid producers encode an acetyl-CoA carboxyltransferase subunit resistant to the action of the antibiotic.

Liu X, Fortin PD, Walsh CT.

Proc Natl Acad Sci U S A. 2008 Sep 9;105(36):13321-6. doi: 10.1073/pnas.0806873105. Epub 2008 Sep 3.

12.

Gatekeeping versus promiscuity in the early stages of the andrimid biosynthetic assembly line.

Magarvey NA, Fortin PD, Thomas PM, Kelleher NL, Walsh CT.

ACS Chem Biol. 2008 Sep 19;3(9):542-54. doi: 10.1021/cb800085g. Epub 2008 Jul 25.

13.

A transglutaminase homologue as a condensation catalyst in antibiotic assembly lines.

Fortin PD, Walsh CT, Magarvey NA.

Nature. 2007 Aug 16;448(7155):824-7. Epub 2007 Jul 25.

PMID:
17653193
14.

Characterization of a C-C bond hydrolase from Sphingomonas wittichii RW1 with novel specificities towards polychlorinated biphenyl metabolites.

Seah SY, Ke J, Denis G, Horsman GP, Fortin PD, Whiting CJ, Eltis LD.

J Bacteriol. 2007 Jun;189(11):4038-45. Epub 2007 Apr 6.

15.

FenF: servicing the Mycosubtilin synthetase assembly line in trans.

Aron ZD, Fortin PD, Calderone CT, Walsh CT.

Chembiochem. 2007 Apr 16;8(6):613-6. No abstract available.

PMID:
17330903
16.

Structures of ternary complexes of BphK, a bacterial glutathione S-transferase that reductively dechlorinates polychlorinated biphenyl metabolites.

Tocheva EI, Fortin PD, Eltis LD, Murphy ME.

J Biol Chem. 2006 Oct 13;281(41):30933-40. Epub 2006 Aug 17.

17.
18.

Directed evolution of a ring-cleaving dioxygenase for polychlorinated biphenyl degradation.

Fortin PD, MacPherson I, Neau DB, Bolin JT, Eltis LD.

J Biol Chem. 2005 Dec 23;280(51):42307-14. Epub 2005 Oct 14.

19.

Molecular basis for the substrate selectivity of bicyclic and monocyclic extradiol dioxygenases.

Vaillancourt FH, Fortin PD, Labbé G, Drouin NM, Karim Z, Agar NY, Eltis LD.

Biochem Biophys Res Commun. 2005 Dec 9;338(1):215-22. Epub 2005 Sep 8.

PMID:
16165093
20.

Evolutionarily divergent extradiol dioxygenases possess higher specificities for polychlorinated biphenyl metabolites.

Fortin PD, Lo AT, Haro MA, Kaschabek SR, Reineke W, Eltis LD.

J Bacteriol. 2005 Jan;187(2):415-21.

21.

Synthesis and evaluation of keto-glutamine analogues as potent inhibitors of severe acute respiratory syndrome 3CLpro.

Jain RP, Pettersson HI, Zhang J, Aull KD, Fortin PD, Huitema C, Eltis LD, Parrish JC, James MN, Wishart DS, Vederas JC.

J Med Chem. 2004 Dec 2;47(25):6113-6.

PMID:
15566280
22.

High-throughput screening identifies inhibitors of the SARS coronavirus main proteinase.

Blanchard JE, Elowe NH, Huitema C, Fortin PD, Cechetto JD, Eltis LD, Brown ED.

Chem Biol. 2004 Oct;11(10):1445-53.

23.

The mechanism-based inactivation of 2,3-dihydroxybiphenyl 1,2-dioxygenase by catecholic substrates.

Vaillancourt FH, Labbe G, Drouin NM, Fortin PD, Eltis LD.

J Biol Chem. 2002 Jan 18;277(3):2019-27. Epub 2001 Nov 13.

24.

Molecular basis for the stabilization and inhibition of 2, 3-dihydroxybiphenyl 1,2-dioxygenase by t-butanol.

Vaillancourt FH, Han S, Fortin PD, Bolin JT, Eltis LD.

J Biol Chem. 1998 Dec 25;273(52):34887-95.

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