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Items: 16

1.

Dual Inhibition of TYK2 and JAK1 for the Treatment of Autoimmune Diseases: Discovery of (( S)-2,2-Difluorocyclopropyl)((1 R,5 S)-3-(2-((1-methyl-1 H-pyrazol-4-yl)amino)pyrimidin-4-yl)-3,8-diazabicyclo[3.2.1]octan-8-yl)methanone (PF-06700841).

Fensome A, Ambler CM, Arnold E, Banker ME, Brown MF, Chrencik J, Clark JD, Dowty ME, Efremov IV, Flick A, Gerstenberger BS, Gopalsamy A, Hayward MM, Hegen M, Hollingshead BD, Jussif J, Knafels JD, Limburg DC, Lin D, Lin TH, Pierce BS, Saiah E, Sharma R, Symanowicz PT, Telliez JB, Trujillo JI, Vajdos FF, Vincent F, Wan ZK, Xing L, Yang X, Yang X, Zhang L.

J Med Chem. 2018 Oct 11;61(19):8597-8612. doi: 10.1021/acs.jmedchem.8b00917. Epub 2018 Aug 16.

PMID:
30113844
2.

Selective Targeting of Bromodomains of the Bromodomain-PHD Fingers Family Impairs Osteoclast Differentiation.

Meier JC, Tallant C, Fedorov O, Witwicka H, Hwang SY, van Stiphout RG, Lambert JP, Rogers C, Yapp C, Gerstenberger BS, Fedele V, Savitsky P, Heidenreich D, Daniels DL, Owen DR, Fish PV, Igoe NM, Bayle ED, Haendler B, Oppermann UCT, Buffa F, Brennan PE, Müller S, Gingras AC, Odgren PR, Birnbaum MJ, Knapp S.

ACS Chem Biol. 2017 Oct 20;12(10):2619-2630. doi: 10.1021/acschembio.7b00481. Epub 2017 Sep 12.

3.

Synthesis of Chiral Azabicycles from Pyroglutaminols.

Choi C, Nuhant P, Mousseau JJ, Yang X, Gerstenberger BS, Williams JM, Wright SW.

Org Lett. 2016 Nov 4;18(21):5748-5751. Epub 2016 Oct 27.

PMID:
27786487
4.

Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit.

Gerstenberger BS, Trzupek JD, Tallant C, Fedorov O, Filippakopoulos P, Brennan PE, Fedele V, Martin S, Picaud S, Rogers C, Parikh M, Taylor A, Samas B, O'Mahony A, Berg E, Pallares G, Torrey AD, Treiber DK, Samardjiev IJ, Nasipak BT, Padilla-Benavides T, Wu Q, Imbalzano AN, Nickerson JA, Bunnage ME, Müller S, Knapp S, Owen DR.

J Med Chem. 2016 May 26;59(10):4800-11. doi: 10.1021/acs.jmedchem.6b00012. Epub 2016 May 3.

5.

Selective targeting of the BRG/PB1 bromodomains impairs embryonic and trophoblast stem cell maintenance.

Fedorov O, Castex J, Tallant C, Owen DR, Martin S, Aldeghi M, Monteiro O, Filippakopoulos P, Picaud S, Trzupek JD, Gerstenberger BS, Bountra C, Willmann D, Wells C, Philpott M, Rogers C, Biggin PC, Brennan PE, Bunnage ME, Schüle R, Günther T, Knapp S, Müller S.

Sci Adv. 2015 Nov 13;1(10):e1500723. doi: 10.1126/sciadv.1500723. eCollection 2015 Nov.

6.

(R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells.

Barsyte-Lovejoy D, Li F, Oudhoff MJ, Tatlock JH, Dong A, Zeng H, Wu H, Freeman SA, Schapira M, Senisterra GA, Kuznetsova E, Marcellus R, Allali-Hassani A, Kennedy S, Lambert JP, Couzens AL, Aman A, Gingras AC, Al-Awar R, Fish PV, Gerstenberger BS, Roberts L, Benn CL, Grimley RL, Braam MJ, Rossi FM, Sudol M, Brown PJ, Bunnage ME, Owen DR, Zaph C, Vedadi M, Arrowsmith CH.

Proc Natl Acad Sci U S A. 2014 Sep 2;111(35):12853-8. doi: 10.1073/pnas.1407358111. Epub 2014 Aug 18.

7.

Siderophore receptor-mediated uptake of lactivicin analogues in gram-negative bacteria.

Starr J, Brown MF, Aschenbrenner L, Caspers N, Che Y, Gerstenberger BS, Huband M, Knafels JD, Lemmon MM, Li C, McCurdy SP, McElroy E, Rauckhorst MR, Tomaras AP, Young JA, Zaniewski RP, Shanmugasundaram V, Han S.

J Med Chem. 2014 May 8;57(9):3845-55. doi: 10.1021/jm500219c. Epub 2014 Apr 21.

PMID:
24694215
8.

Pyridone-conjugated monobactam antibiotics with gram-negative activity.

Brown MF, Mitton-Fry MJ, Arcari JT, Barham R, Casavant J, Gerstenberger BS, Han S, Hardink JR, Harris TM, Hoang T, Huband MD, Lall MS, Lemmon MM, Li C, Lin J, McCurdy SP, McElroy E, McPherson C, Marr ES, Mueller JP, Mullins L, Nikitenko AA, Noe MC, Penzien J, Plummer MS, Schuff BP, Shanmugasundaram V, Starr JT, Sun J, Tomaras A, Young JA, Zaniewski RP.

J Med Chem. 2013 Jul 11;56(13):5541-52. doi: 10.1021/jm400560z. Epub 2013 Jun 27.

PMID:
23755848
9.

Covalent inhibitors of interleukin-2 inducible T cell kinase (itk) with nanomolar potency in a whole-blood assay.

Zapf CW, Gerstenberger BS, Xing L, Limburg DC, Anderson DR, Caspers N, Han S, Aulabaugh A, Kurumbail R, Shakya S, Li X, Spaulding V, Czerwinski RM, Seth N, Medley QG.

J Med Chem. 2012 Nov 26;55(22):10047-63. doi: 10.1021/jm301190s. Epub 2012 Nov 12.

PMID:
23098091
10.

Identification of a chemical probe for bromo and extra C-terminal bromodomain inhibition through optimization of a fragment-derived hit.

Fish PV, Filippakopoulos P, Bish G, Brennan PE, Bunnage ME, Cook AS, Federov O, Gerstenberger BS, Jones H, Knapp S, Marsden B, Nocka K, Owen DR, Philpott M, Picaud S, Primiano MJ, Ralph MJ, Sciammetta N, Trzupek JD.

J Med Chem. 2012 Nov 26;55(22):9831-7. doi: 10.1021/jm3010515. Epub 2012 Nov 8.

11.

Novel monobactams utilizing a siderophore uptake mechanism for the treatment of gram-negative infections.

Mitton-Fry MJ, Arcari JT, Brown MF, Casavant JM, Finegan SM, Flanagan ME, Gao H, George DM, Gerstenberger BS, Han S, Hardink JR, Harris TM, Hoang T, Huband MD, Irvine R, Lall MS, Megan Lemmon M, Li C, Lin J, McCurdy SP, Mueller JP, Mullins L, Niosi M, Noe MC, Pattavina D, Penzien J, Plummer MS, Risley H, Schuff BP, Shanmugasundaram V, Starr JT, Sun J, Winton J, Young JA.

Bioorg Med Chem Lett. 2012 Sep 15;22(18):5989-94. doi: 10.1016/j.bmcl.2012.07.005. Epub 2012 Jul 20. Erratum in: Bioorg Med Chem Lett. 2015 Sep 15;25(18):4029.

PMID:
22892121
12.

One-pot synthesis of N-arylpyrazoles from arylhalides.

Gerstenberger BS, Rauckhorst MR, Starr JT.

Org Lett. 2009 May 21;11(10):2097-100. doi: 10.1021/ol900515a.

PMID:
19385606
13.

Diazonamide support studies: stereoselective formation of the C10 chiral center in both the CDEFG and AEFG fragments.

Lin J, Gerstenberger BS, Stessman NY, Konopelski JP.

Org Lett. 2008 Sep 18;10(18):3969-72. doi: 10.1021/ol8014336. Epub 2008 Aug 15.

14.

Structural characterization of an enantiomerically pure amino acid imidazolide and direct formation of the beta-lactam nucleus from an alpha-amino acid.

Gerstenberger BS, Lin J, Mimieux YS, Brown LE, Oliver AG, Konopelski JP.

Org Lett. 2008 Feb 7;10(3):369-72. doi: 10.1021/ol7025922. Epub 2008 Jan 9.

15.

tert-Buyldiphenylsilylethyl ("TBDPSE"): a practical protecting group for phenols.

Gerstenberger BS, Konopelski JP.

J Org Chem. 2005 Feb 18;70(4):1467-70.

PMID:
15704987
16.

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