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Items: 31

1.

Discovery of Clinical Candidate 1-{[(2S,3S,4S)-3-Ethyl-4-fluoro-5-oxopyrrolidin-2-yl]methoxy}-7-methoxyisoquinoline-6-carboxamide (PF-06650833), a Potent, Selective Inhibitor of Interleukin-1 Receptor Associated Kinase 4 (IRAK4), by Fragment-Based Drug Design.

Lee KL, Ambler CM, Anderson DR, Boscoe BP, Bree AG, Brodfuehrer JI, Chang JS, Choi C, Chung S, Curran KJ, Day JE, Dehnhardt CM, Dower K, Drozda SE, Frisbie RK, Gavrin LK, Goldberg JA, Han S, Hegen M, Hepworth D, Hope HR, Kamtekar S, Kilty IC, Lee A, Lin LL, Lovering FE, Lowe MD, Mathias JP, Morgan HM, Murphy EA, Papaioannou N, Patny A, Pierce BS, Rao VR, Saiah E, Samardjiev IJ, Samas BM, Shen MWH, Shin JH, Soutter HH, Strohbach JW, Symanowicz PT, Thomason JR, Trzupek JD, Vargas R, Vincent F, Yan J, Zapf CW, Wright SW.

J Med Chem. 2017 Jul 13;60(13):5521-5542. doi: 10.1021/acs.jmedchem.7b00231. Epub 2017 Jun 14.

PMID:
28498658
2.

Crystal structure of an intermediate of rotating dimers within the synaptic tetramer of the G-segment invertase.

Ritacco CJ, Kamtekar S, Wang J, Steitz TA.

Nucleic Acids Res. 2013 Feb 1;41(4):2673-82. doi: 10.1093/nar/gks1303. Epub 2012 Dec 28.

3.

Discovery of novel spirocyclic inhibitors of fatty acid amide hydrolase (FAAH). Part 2. Discovery of 7-azaspiro[3.5]nonane urea PF-04862853, an orally efficacious inhibitor of fatty acid amide hydrolase (FAAH) for pain.

Meyers MJ, Long SA, Pelc MJ, Wang JL, Bowen SJ, Schweitzer BA, Wilcox MV, McDonald J, Smith SE, Foltin S, Rumsey J, Yang YS, Walker MC, Kamtekar S, Beidler D, Thorarensen A.

Bioorg Med Chem Lett. 2011 Nov 1;21(21):6545-53. doi: 10.1016/j.bmcl.2011.08.048. Epub 2011 Aug 19.

PMID:
21924613
4.

Structural basis of substrate discrimination and integrin binding by autotaxin.

Hausmann J, Kamtekar S, Christodoulou E, Day JE, Wu T, Fulkerson Z, Albers HM, van Meeteren LA, Houben AJ, van Zeijl L, Jansen S, Andries M, Hall T, Pegg LE, Benson TE, Kasiem M, Harlos K, Kooi CW, Smyth SS, Ovaa H, Bollen M, Morris AJ, Moolenaar WH, Perrakis A.

Nat Struct Mol Biol. 2011 Feb;18(2):198-204. doi: 10.1038/nsmb.1980. Epub 2011 Jan 16.

5.

Crystallization and preliminary X-ray diffraction analysis of rat autotaxin.

Day JE, Hall T, Pegg LE, Benson TE, Hausmann J, Kamtekar S.

Acta Crystallogr Sect F Struct Biol Cryst Commun. 2010 Sep 1;66(Pt 9):1127-9. doi: 10.1107/S1744309110030228. Epub 2010 Aug 31.

6.

Kinetic and structural characterization of caspase-3 and caspase-8 inhibition by a novel class of irreversible inhibitors.

Wang Z, Watt W, Brooks NA, Harris MS, Urban J, Boatman D, McMillan M, Kahn M, Heinrikson RL, Finzel BC, Wittwer AJ, Blinn J, Kamtekar S, Tomasselli AG.

Biochim Biophys Acta. 2010 Sep;1804(9):1817-31. doi: 10.1016/j.bbapap.2010.05.007. Epub 2010 May 24.

PMID:
20580860
7.

Crystal structure of fatty acid amide hydrolase bound to the carbamate inhibitor URB597: discovery of a deacylating water molecule and insight into enzyme inactivation.

Mileni M, Kamtekar S, Wood DC, Benson TE, Cravatt BF, Stevens RC.

J Mol Biol. 2010 Jul 23;400(4):743-54. doi: 10.1016/j.jmb.2010.05.034. Epub 2010 May 21.

8.

Structure-based drug design enables conversion of a DFG-in binding CSF-1R kinase inhibitor to a DFG-out binding mode.

Meyers MJ, Pelc M, Kamtekar S, Day J, Poda GI, Hall MK, Michener ML, Reitz BA, Mathis KJ, Pierce BS, Parikh MD, Mischke DA, Long SA, Parlow JJ, Anderson DR, Thorarensen A.

Bioorg Med Chem Lett. 2010 Mar 1;20(5):1543-7. doi: 10.1016/j.bmcl.2010.01.078. Epub 2010 Jan 21.

PMID:
20137931
9.

Structure of the RAG1 nonamer binding domain with DNA reveals a dimer that mediates DNA synapsis.

Yin FF, Bailey S, Innis CA, Ciubotaru M, Kamtekar S, Steitz TA, Schatz DG.

Nat Struct Mol Biol. 2009 May;16(5):499-508. doi: 10.1038/nsmb.1593. Epub 2009 Apr 26.

10.

Discovery and characterization of a highly selective FAAH inhibitor that reduces inflammatory pain.

Ahn K, Johnson DS, Mileni M, Beidler D, Long JZ, McKinney MK, Weerapana E, Sadagopan N, Liimatta M, Smith SE, Lazerwith S, Stiff C, Kamtekar S, Bhattacharya K, Zhang Y, Swaney S, Van Becelaere K, Stevens RC, Cravatt BF.

Chem Biol. 2009 Apr 24;16(4):411-20. doi: 10.1016/j.chembiol.2009.02.013.

11.

Structure-guided inhibitor design for human FAAH by interspecies active site conversion.

Mileni M, Johnson DS, Wang Z, Everdeen DS, Liimatta M, Pabst B, Bhattacharya K, Nugent RA, Kamtekar S, Cravatt BF, Ahn K, Stevens RC.

Proc Natl Acad Sci U S A. 2008 Sep 2;105(35):12820-4. doi: 10.1073/pnas.0806121105. Epub 2008 Aug 27.

12.

Structures of phi29 DNA polymerase complexed with substrate: the mechanism of translocation in B-family polymerases.

Berman AJ, Kamtekar S, Goodman JL, Lázaro JM, de Vega M, Blanco L, Salas M, Steitz TA.

EMBO J. 2007 Jul 25;26(14):3494-505. Epub 2007 Jul 5.

13.

Toward understanding phosphoseryl-tRNACys formation: the crystal structure of Methanococcus maripaludis phosphoseryl-tRNA synthetase.

Kamtekar S, Hohn MJ, Park HS, Schnitzbauer M, Sauerwald A, Söll D, Steitz TA.

Proc Natl Acad Sci U S A. 2007 Feb 20;104(8):2620-5. Epub 2007 Feb 14.

14.

Implications of structures of synaptic tetramers of gamma delta resolvase for the mechanism of recombination.

Kamtekar S, Ho RS, Cocco MJ, Li W, Wenwieser SV, Boocock MR, Grindley ND, Steitz TA.

Proc Natl Acad Sci U S A. 2006 Jul 11;103(28):10642-7. Epub 2006 Jun 28.

15.

The phi29 DNA polymerase:protein-primer structure suggests a model for the initiation to elongation transition.

Kamtekar S, Berman AJ, Wang J, Lázaro JM, de Vega M, Blanco L, Salas M, Steitz TA.

EMBO J. 2006 Mar 22;25(6):1335-43. Epub 2006 Mar 2.

16.

Asymmetric behavior of archaeal prolyl-tRNA synthetase.

Ambrogelly A, Kamtekar S, Stathopoulos C, Kennedy D, Söll D.

FEBS Lett. 2005 Nov 7;579(27):6017-22. Epub 2005 Oct 5.

17.

Structure of a synaptic gammadelta resolvase tetramer covalently linked to two cleaved DNAs.

Li W, Kamtekar S, Xiong Y, Sarkis GJ, Grindley ND, Steitz TA.

Science. 2005 Aug 19;309(5738):1210-5. Epub 2005 Jun 30.

18.

A specific subdomain in phi29 DNA polymerase confers both processivity and strand-displacement capacity.

Rodríguez I, Lázaro JM, Blanco L, Kamtekar S, Berman AJ, Wang J, Steitz TA, Salas M, de Vega M.

Proc Natl Acad Sci U S A. 2005 May 3;102(18):6407-12. Epub 2005 Apr 21.

19.

Correction of X-ray intensities from single crystals containing lattice-translocation defects.

Wang J, Kamtekar S, Berman AJ, Steitz TA.

Acta Crystallogr D Biol Crystallogr. 2005 Jan;61(Pt 1):67-74. Epub 2004 Dec 17.

PMID:
15608377
20.

Insights into strand displacement and processivity from the crystal structure of the protein-primed DNA polymerase of bacteriophage phi29.

Kamtekar S, Berman AJ, Wang J, Lázaro JM, de Vega M, Blanco L, Salas M, Steitz TA.

Mol Cell. 2004 Nov 19;16(4):609-18. Erratum in: Mol Cell. 2004 Dec 22;16(6):1035-6.

21.

Cys-tRNACys formation and cysteine biosynthesis in methanogenic archaea: two faces of the same problem?

Ambrogelly A, Kamtekar S, Sauerwald A, Ruan B, Tumbula-Hansen D, Kennedy D, Ahel I, Söll D.

Cell Mol Life Sci. 2004 Oct;61(19-20):2437-45. Review.

PMID:
15526152
22.

The structural basis of cysteine aminoacylation of tRNAPro by prolyl-tRNA synthetases.

Kamtekar S, Kennedy WD, Wang J, Stathopoulos C, Söll D, Steitz TA.

Proc Natl Acad Sci U S A. 2003 Feb 18;100(4):1673-8. Epub 2003 Feb 10.

23.

Nucleotide-dependent conformational changes in a protease-associated ATPase HsIU.

Wang J, Song JJ, Seong IS, Franklin MC, Kamtekar S, Eom SH, Chung CH.

Structure. 2001 Nov;9(11):1107-16.

24.

Crystal structures of the HslVU peptidase-ATPase complex reveal an ATP-dependent proteolysis mechanism.

Wang J, Song JJ, Franklin MC, Kamtekar S, Im YJ, Rho SH, Seong IS, Lee CS, Chung CH, Eom SH.

Structure. 2001 Feb 7;9(2):177-84.

25.

De novo heme proteins from designed combinatorial libraries.

Rojas NR, Kamtekar S, Simons CT, McLean JE, Vogel KM, Spiro TG, Farid RS, Hecht MH.

Protein Sci. 1997 Dec;6(12):2512-24.

26.

Trace Analysis of Zn(II), Be(II), and Bi(III) by Enzyme-Catalyzed Chemiluminescence.

Kamtekar SD, Pande R, Ayyagari MS, Marx KA, Kaplan DL, Kumar J, Tripathy S.

Anal Chem. 1996 Jan 1;68(1):216-20. doi: 10.1021/ac950681u.

PMID:
21619238
27.

A biotinylated undecylthiophene copolymer bioconjugate for surface immobilization: creating an alkaline phosphatase chemiluminescence-based biosensor.

Pande R, Kamtekar S, Ayyagari MS, Kamath M, Marx KA, Kumar J, Tripathy SK, Kaplan DL.

Bioconjug Chem. 1996 Jan-Feb;7(1):159-64.

PMID:
8742005
28.

Chemiluminescence-based inhibition kinetics of alkaline phosphatase in the development of a pesticide biosensor.

Ayyagari MS, Kamtekar S, Pande R, Marx KA, Kumar J, Tripathy SK, Akkara J, Kaplan DL.

Biotechnol Prog. 1995 Nov-Dec;11(6):699-703.

PMID:
8541020
29.

Protein Motifs. 7. The four-helix bundle: what determines a fold?

Kamtekar S, Hecht MH.

FASEB J. 1995 Aug;9(11):1013-22. Review.

PMID:
7649401
30.

Molecular assembly of proteins and conjugated polymers: Toward development of biosensors.

Ayyagari MS, Pande R, Kamtekar S, Marx KA, Tripathy SK, Gao H, Kumar J, Akkara JA, Kaplan DL.

Biotechnol Bioeng. 1995 Jan 20;45(2):116-21.

PMID:
18623092
31.

Protein design by binary patterning of polar and nonpolar amino acids.

Kamtekar S, Schiffer JM, Xiong H, Babik JM, Hecht MH.

Science. 1993 Dec 10;262(5140):1680-5.

PMID:
8259512

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