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Items: 25

1.

Discovery of Potent and Selective Periphery-Restricted Quinazoline Inhibitors of the Cyclic Nucleotide Phosphodiesterase PDE1.

Humphrey JM, Movsesian M, Am Ende CW, Becker SL, Chappie TA, Jenkinson S, Liras JL, Liras S, Orozco C, Pandit J, Vajdos FF, Vandeput F, Yang E, Menniti FS.

J Med Chem. 2018 May 10. doi: 10.1021/acs.jmedchem.8b00374. [Epub ahead of print]

PMID:
29718668
2.

Design of a Janus Kinase 3 (JAK3) Specific Inhibitor 1-((2S,5R)-5-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one (PF-06651600) Allowing for the Interrogation of JAK3 Signaling in Humans.

Thorarensen A, Dowty ME, Banker ME, Juba B, Jussif J, Lin T, Vincent F, Czerwinski RM, Casimiro-Garcia A, Unwalla R, Trujillo JI, Liang S, Balbo P, Che Y, Gilbert AM, Brown MF, Hayward M, Montgomery J, Leung L, Yang X, Soucy S, Hegen M, Coe J, Langille J, Vajdos F, Chrencik J, Telliez JB.

J Med Chem. 2017 Mar 9;60(5):1971-1993. doi: 10.1021/acs.jmedchem.6b01694. Epub 2017 Feb 16.

PMID:
28139931
3.

Aminomethyl-Derived Beta Secretase (BACE1) Inhibitors: Engaging Gly230 without an Anilide Functionality.

Butler CR, Ogilvie K, Martinez-Alsina L, Barreiro G, Beck EM, Nolan CE, Atchison K, Benvenuti E, Buzon L, Doran S, Gonzales C, Helal CJ, Hou X, Hsu MH, Johnson EF, Lapham K, Lanyon L, Parris K, O'Neill BT, Riddell D, Robshaw A, Vajdos F, Brodney MA.

J Med Chem. 2017 Jan 12;60(1):386-402. doi: 10.1021/acs.jmedchem.6b01451. Epub 2016 Dec 20.

4.

Discovery of a JAK3-Selective Inhibitor: Functional Differentiation of JAK3-Selective Inhibition over pan-JAK or JAK1-Selective Inhibition.

Telliez JB, Dowty ME, Wang L, Jussif J, Lin T, Li L, Moy E, Balbo P, Li W, Zhao Y, Crouse K, Dickinson C, Symanowicz P, Hegen M, Banker ME, Vincent F, Unwalla R, Liang S, Gilbert AM, Brown MF, Hayward M, Montgomery J, Yang X, Bauman J, Trujillo JI, Casimiro-Garcia A, Vajdos FF, Leung L, Geoghegan KF, Quazi A, Xuan D, Jones L, Hett E, Wright K, Clark JD, Thorarensen A.

ACS Chem Biol. 2016 Dec 16;11(12):3442-3451. Epub 2016 Nov 10.

PMID:
27791347
5.

Discovery of spirocyclic-diamine inhibitors of mammalian acetyl CoA-carboxylase.

Kung DW, Griffith DA, Esler WP, Vajdos FF, Mathiowetz AM, Doran SD, Amor PA, Bagley SW, Banks T, Cabral S, Ford K, Garcia-Irizarry CN, Landis MS, Loomis K, McPherson K, Niosi M, Rockwell KL, Rose C, Smith AC, Southers JA, Tapley S, Tu M, Valentine JJ.

Bioorg Med Chem Lett. 2015 Nov 15;25(22):5352-6. doi: 10.1016/j.bmcl.2015.09.035. Epub 2015 Sep 15.

PMID:
26411795
6.

Discovery of a series of efficient, centrally efficacious BACE1 inhibitors through structure-based drug design.

Butler CR, Brodney MA, Beck EM, Barreiro G, Nolan CE, Pan F, Vajdos F, Parris K, Varghese AH, Helal CJ, Lira R, Doran SD, Riddell DR, Buzon LM, Dutra JK, Martinez-Alsina LA, Ogilvie K, Murray JC, Young JM, Atchison K, Robshaw A, Gonzales C, Wang J, Zhang Y, O'Neill BT.

J Med Chem. 2015 Mar 26;58(6):2678-702. doi: 10.1021/jm501833t. Epub 2015 Mar 9.

PMID:
25695670
7.

Decreasing the rate of metabolic ketone reduction in the discovery of a clinical acetyl-CoA carboxylase inhibitor for the treatment of diabetes.

Griffith DA, Kung DW, Esler WP, Amor PA, Bagley SW, Beysen C, Carvajal-Gonzalez S, Doran SD, Limberakis C, Mathiowetz AM, McPherson K, Price DA, Ravussin E, Sonnenberg GE, Southers JA, Sweet LJ, Turner SM, Vajdos FF.

J Med Chem. 2014 Dec 26;57(24):10512-26. doi: 10.1021/jm5016022. Epub 2014 Dec 11.

8.

Discovery and synthesis of novel 4-aminopyrrolopyrimidine Tie-2 kinase inhibitors for the treatment of solid tumors.

Arcari JT, Beebe JS, Berliner MA, Bernardo V, Boehm M, Borzillo GV, Clark T, Cohen BD, Connell RD, Frost HN, Gordon DA, Hungerford WM, Kakar SM, Kanter A, Keene NF, Knauth EA, Lagreca SD, Lu Y, Martinez-Alsina L, Marx MA, Morris J, Patel NC, Savage D, Soderstrom CI, Thompson C, Tkalcevic G, Tom NJ, Vajdos FF, Valentine JJ, Vincent PW, Wessel MD, Chen JM.

Bioorg Med Chem Lett. 2013 May 15;23(10):3059-63. doi: 10.1016/j.bmcl.2013.03.012. Epub 2013 Mar 21.

PMID:
23566514
9.

Spirocyclic sulfamides as β-secretase 1 (BACE-1) inhibitors for the treatment of Alzheimer's disease: utilization of structure based drug design, WaterMap, and CNS penetration studies to identify centrally efficacious inhibitors.

Brodney MA, Barreiro G, Ogilvie K, Hajos-Korcsok E, Murray J, Vajdos F, Ambroise C, Christoffersen C, Fisher K, Lanyon L, Liu J, Nolan CE, Withka JM, Borzilleri KA, Efremov I, Oborski CE, Varghese A, O'Neill BT.

J Med Chem. 2012 Nov 8;55(21):9224-39. doi: 10.1021/jm3009426. Epub 2012 Oct 8.

PMID:
22984865
10.

Discovery and optimization of a novel spiropyrrolidine inhibitor of β-secretase (BACE1) through fragment-based drug design.

Efremov IV, Vajdos FF, Borzilleri KA, Capetta S, Chen H, Dorff PH, Dutra JK, Goldstein SW, Mansour M, McColl A, Noell S, Oborski CE, O'Connell TN, O'Sullivan TJ, Pandit J, Wang H, Wei B, Withka JM.

J Med Chem. 2012 Nov 8;55(21):9069-88. doi: 10.1021/jm201715d. Epub 2012 May 9.

PMID:
22468999
11.

Deconstruction of activity-dependent covalent modification of heme in human neutrophil myeloperoxidase by multistage mass spectrometry (MS(4)).

Geoghegan KF, Varghese AH, Feng X, Bessire AJ, Conboy JJ, Ruggeri RB, Ahn K, Spath SN, Filippov SV, Conrad SJ, Carpino PA, Guimarães CR, Vajdos FF.

Biochemistry. 2012 Mar 13;51(10):2065-77. doi: 10.1021/bi201872j. Epub 2012 Mar 1.

PMID:
22352991
12.

Structure-guided inhibitor design for human acetyl-coenzyme A carboxylase by interspecies active site conversion.

Rajamohan F, Marr E, Reyes AR, Landro JA, Anderson MD, Corbett JW, Dirico KJ, Harwood JH, Tu M, Vajdos FF.

J Biol Chem. 2011 Dec 2;286(48):41510-9. doi: 10.1074/jbc.M111.275396. Epub 2011 Sep 27.

13.

Discovery of small molecule isozyme non-specific inhibitors of mammalian acetyl-CoA carboxylase 1 and 2.

Corbett JW, Freeman-Cook KD, Elliott R, Vajdos F, Rajamohan F, Kohls D, Marr E, Zhang H, Tong L, Tu M, Murdande S, Doran SD, Houser JA, Song W, Jones CJ, Coffey SB, Buzon L, Minich ML, Dirico KJ, Tapley S, McPherson RK, Sugarman E, Harwood HJ Jr, Esler W.

Bioorg Med Chem Lett. 2010 Apr 1;20(7):2383-8. doi: 10.1016/j.bmcl.2009.04.091. Epub 2009 Apr 24.

PMID:
20219367
14.

Antitumor activity and pharmacology of a selective focal adhesion kinase inhibitor, PF-562,271.

Roberts WG, Ung E, Whalen P, Cooper B, Hulford C, Autry C, Richter D, Emerson E, Lin J, Kath J, Coleman K, Yao L, Martinez-Alsina L, Lorenzen M, Berliner M, Luzzio M, Patel N, Schmitt E, LaGreca S, Jani J, Wessel M, Marr E, Griffor M, Vajdos F.

Cancer Res. 2008 Mar 15;68(6):1935-44. doi: 10.1158/0008-5472.CAN-07-5155.

15.

The 2.0 A crystal structure of the ERalpha ligand-binding domain complexed with lasofoxifene.

Vajdos FF, Hoth LR, Geoghegan KF, Simons SP, LeMotte PK, Danley DE, Ammirati MJ, Pandit J.

Protein Sci. 2007 May;16(5):897-905.

16.

Suppressor of fused regulates Gli activity through a dual binding mechanism.

Merchant M, Vajdos FF, Ultsch M, Maun HR, Wendt U, Cannon J, Desmarais W, Lazarus RA, de Vos AM, de Sauvage FJ.

Mol Cell Biol. 2004 Oct;24(19):8627-41.

17.

Insights into ErbB signaling from the structure of the ErbB2-pertuzumab complex.

Franklin MC, Carey KD, Vajdos FF, Leahy DJ, de Vos AM, Sliwkowski MX.

Cancer Cell. 2004 Apr;5(4):317-28.

18.

Structural insights into the catalytic mechanism of cyclophilin A.

Howard BR, Vajdos FF, Li S, Sundquist WI, Hill CP.

Nat Struct Biol. 2003 Jun;10(6):475-81.

PMID:
12730686
19.

Comprehensive functional maps of the antigen-binding site of an anti-ErbB2 antibody obtained with shotgun scanning mutagenesis.

Vajdos FF, Adams CW, Breece TN, Presta LG, de Vos AM, Sidhu SS.

J Mol Biol. 2002 Jul 5;320(2):415-28.

PMID:
12079396
20.

Crystal structure of human insulin-like growth factor-1: detergent binding inhibits binding protein interactions.

Vajdos FF, Ultsch M, Schaffer ML, Deshayes KD, Liu J, Skelton NJ, de Vos AM.

Biochemistry. 2001 Sep 18;40(37):11022-9.

PMID:
11551198
21.

Crystal structure of cyclophilin A complexed with a binding site peptide from the HIV-1 capsid protein.

Vajdos FF, Yoo S, Houseweart M, Sundquist WI, Hill CP.

Protein Sci. 1997 Nov;6(11):2297-307.

22.

Structure of the carboxyl-terminal dimerization domain of the HIV-1 capsid protein.

Gamble TR, Yoo S, Vajdos FF, von Schwedler UK, Worthylake DK, Wang H, McCutcheon JP, Sundquist WI, Hill CP.

Science. 1997 Oct 31;278(5339):849-53.

23.

Crystal structure of human cyclophilin A bound to the amino-terminal domain of HIV-1 capsid.

Gamble TR, Vajdos FF, Yoo S, Worthylake DK, Houseweart M, Sundquist WI, Hill CP.

Cell. 1996 Dec 27;87(7):1285-94.

24.

How to measure and predict the molar absorption coefficient of a protein.

Pace CN, Vajdos F, Fee L, Grimsley G, Gray T.

Protein Sci. 1995 Nov;4(11):2411-23.

25.

Pseudomonas cepacia 2,2-dialkylglycine decarboxylase. Sequence and expression in Escherichia coli of structural and repressor genes.

Keller JW, Baurick KB, Rutt GC, O'Malley MV, Sonafrank NL, Reynolds RA, Ebbesson LO, Vajdos FF.

J Biol Chem. 1990 Apr 5;265(10):5531-9.

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