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Items: 35


Preparation and biological evaluation of BACE1 inhibitors: Leveraging trans-cyclopropyl moieties as ligand efficient conformational constraints.

Winneroski LL, Erickson JA, Green SJ, Lopez JE, Stout SL, Porter WJ, Timm DE, Audia JE, Barberis M, Beck JP, Boggs LN, Borders AR, Boyer RD, Brier RA, Hembre EJ, Hendle J, Garcia-Losada P, Minguez JM, Mathes BM, May PC, Monk SA, Rankovic Z, Shi Y, Watson BM, Yang Z, Mergott DJ.

Bioorg Med Chem. 2019 Nov 15:115194. doi: 10.1016/j.bmc.2019.115194. [Epub ahead of print]


Merestinib (LY2801653) inhibits neurotrophic receptor kinase (NTRK) and suppresses growth of NTRK fusion bearing tumors.

Konicek BW, Capen AR, Credille KM, Ebert PJ, Falcon BL, Heady GL, Patel BKR, Peek VL, Stephens JR, Stewart JA, Stout SL, Timm DE, Um SL, Willard MD, Wulur IH, Zeng Y, Wang Y, Walgren RA, Betty Yan SC.

Oncotarget. 2018 Feb 13;9(17):13796-13806. doi: 10.18632/oncotarget.24488. eCollection 2018 Mar 2.


Cryo-electron microscopy structure of a human PRMT5:MEP50 complex.

Timm DE, Bowman V, Madsen R, Rauch C.

PLoS One. 2018 Mar 8;13(3):e0193205. doi: 10.1371/journal.pone.0193205. eCollection 2018.


Reconstruction of 3D structures of MET antibodies from electron microscopy 2D class averages.

Chen Q, Vieth M, Timm DE, Humblet C, Schneidman-Duhovny D, Chemmama IE, Sali A, Zeng W, Lu J, Liu L.

PLoS One. 2017 Apr 13;12(4):e0175758. doi: 10.1371/journal.pone.0175758. eCollection 2017.


ESR and X-ray Structure Investigations on the Binding and Mechanism of Inhibition of the Native State of Myeloperoxidase with Low Molecular Weight Fragments.

Chavali B, Masquelin T, Nilges MJ, Timm DE, Stout SL, Matter WF, Jin N, Jadhav PK, Deng GG.

Appl Magn Reson. 2015;46(8):853-873. Epub 2015 May 19.


Preparation and biological evaluation of conformationally constrained BACE1 inhibitors.

Winneroski LL, Schiffler MA, Erickson JA, May PC, Monk SA, Timm DE, Audia JE, Beck JP, Boggs LN, Borders AR, Boyer RD, Brier RA, Hudziak KJ, Klimkowski VJ, Garcia Losada P, Mathes BM, Stout SL, Watson BM, Mergott DJ.

Bioorg Med Chem. 2015 Jul 1;23(13):3260-8. doi: 10.1016/j.bmc.2015.04.062. Epub 2015 May 6.


The potent BACE1 inhibitor LY2886721 elicits robust central Aβ pharmacodynamic responses in mice, dogs, and humans.

May PC, Willis BA, Lowe SL, Dean RA, Monk SA, Cocke PJ, Audia JE, Boggs LN, Borders AR, Brier RA, Calligaro DO, Day TA, Ereshefsky L, Erickson JA, Gevorkyan H, Gonzales CR, James DE, Jhee SS, Komjathy SF, Li L, Lindstrom TD, Mathes BM, Martényi F, Sheehan SM, Stout SL, Timm DE, Vaught GM, Watson BM, Winneroski LL, Yang Z, Mergott DJ.

J Neurosci. 2015 Jan 21;35(3):1199-210. doi: 10.1523/JNEUROSCI.4129-14.2015.


Robust central reduction of amyloid-β in humans with an orally available, non-peptidic β-secretase inhibitor.

May PC, Dean RA, Lowe SL, Martenyi F, Sheehan SM, Boggs LN, Monk SA, Mathes BM, Mergott DJ, Watson BM, Stout SL, Timm DE, Smith Labell E, Gonzales CR, Nakano M, Jhee SS, Yen M, Ereshefsky L, Lindstrom TD, Calligaro DO, Cocke PJ, Greg Hall D, Friedrich S, Citron M, Audia JE.

J Neurosci. 2011 Nov 16;31(46):16507-16. doi: 10.1523/JNEUROSCI.3647-11.2011.


Structural and functional analysis of two new positive allosteric modulators of GluA2 desensitization and deactivation.

Timm DE, Benveniste M, Weeks AM, Nisenbaum ES, Partin KM.

Mol Pharmacol. 2011 Aug;80(2):267-80. doi: 10.1124/mol.110.070243. Epub 2011 May 4.


Discovery of non-covalent dipeptidyl peptidase IV inhibitors which induce a conformational change in the active site.

Sheehan SM, Mest HJ, Watson BM, Klimkowski VJ, Timm DE, Cauvin A, Parsons SH, Shi Q, Canada EJ, Wiley MR, Ruehter G, Evers B, Petersen S, Blaszczak LC, Pulley SR, Margolis BJ, Wishart GN, Renson B, Hankotius D, Mohr M, Zechel JC, Michael Kalbfleisch J, Dingess-Hammond EA, Boelke A, Weichert AG.

Bioorg Med Chem Lett. 2007 Mar 15;17(6):1765-8. Epub 2006 Dec 24.


Slow-onset inhibition of fumarylacetoacetate hydrolase by phosphinate mimics of the tetrahedral intermediate: kinetics, crystal structure and pharmacokinetics.

Bateman RL, Ashworth J, Witte JF, Baker LJ, Bhanumoorthy P, Timm DE, Hurley TD, Grompe M, McClard RW.

Biochem J. 2007 Mar 1;402(2):251-60.


Pyrithiamine as a substrate for thiamine pyrophosphokinase.

Liu JY, Timm DE, Hurley TD.

J Biol Chem. 2006 Mar 10;281(10):6601-7. Epub 2005 Dec 19.


Aminoimidazo[1,2-a]pyridines as a new structural class of cyclin-dependent kinase inhibitors. Part 1: Design, synthesis, and biological evaluation.

Jaramillo C, de Diego JE, Hamdouchi C, Collins E, Keyser H, Sánchez-Martínez C, del Prado M, Norman B, Brooks HB, Watkins SA, Spencer CD, Dempsey JA, Anderson BD, Campbell RM, Leggett T, Patel B, Schultz RM, Espinosa J, Vieth M, Zhang F, Timm DE.

Bioorg Med Chem Lett. 2004 Dec 20;14(24):6095-9.


The discovery of a new structural class of cyclin-dependent kinase inhibitors, aminoimidazo[1,2-a]pyridines.

Hamdouchi C, Keyser H, Collins E, Jaramillo C, De Diego JE, Spencer CD, Dempsey JA, Anderson BD, Leggett T, Stamm NB, Schultz RM, Watkins SA, Cocke K, Lemke S, Burke TF, Beckmann RP, Dixon JT, Gurganus TM, Rankl NB, Houck KA, Zhang F, Vieth M, Espinosa J, Timm DE, Campbell RM, Patel BK, Brooks HB.

Mol Cancer Ther. 2004 Jan;3(1):1-9.


The crystal structure of yeast thiamin pyrophosphokinase.

Baker LJ, Dorocke JA, Harris RA, Timm DE.

Structure. 2001 Jun;9(6):539-46.


Crystal structure of thiamin pyrophosphokinase.

Timm DE, Liu J, Baker LJ, Harris RA.

J Mol Biol. 2001 Jun 29;310(1):195-204.


Structural basis of pheromone binding to mouse major urinary protein (MUP-I).

Timm DE, Baker LJ, Mueller H, Zidek L, Novotny MV.

Protein Sci. 2001 May;10(5):997-1004.


Structural and functional analysis of missense mutations in fumarylacetoacetate hydrolase, the gene deficient in hereditary tyrosinemia type 1.

Bergeron A, D'Astous M, Timm DE, Tanguay RM.

J Biol Chem. 2001 May 4;276(18):15225-31. Epub 2001 Jan 22.


Mechanistic inferences from the crystal structure of fumarylacetoacetate hydrolase with a bound phosphorus-based inhibitor.

Bateman RL, Bhanumoorthy P, Witte JF, McClard RW, Grompe M, Timm DE.

J Biol Chem. 2001 May 4;276(18):15284-91. Epub 2001 Jan 11.


Asymmetries in the nucleosome core particle at 2.5 A resolution.

Harp JM, Hanson BL, Timm DE, Bunick GJ.

Acta Crystallogr D Biol Crystallogr. 2000 Dec;56(Pt 12):1513-34.


Structural and functional analysis of mutations in alkaptonuria.

Rodríguez JM, Timm DE, Titus GP, Beltrán-Valero De Bernabé D, Criado O, Mueller HA, Rodríguez De Córdoba S, Peñalva MA.

Hum Mol Genet. 2000 Sep 22;9(15):2341-50.


Crystal structure of human homogentisate dioxygenase.

Titus GP, Mueller HA, Burgner J, Rodríguez De Córdoba S, Peñalva MA, Timm DE.

Nat Struct Biol. 2000 Jul;7(7):542-6.


Crystal structure and mechanism of a carbon-carbon bond hydrolase.

Timm DE, Mueller HA, Bhanumoorthy P, Harp JM, Bunick GJ.

Structure. 1999 Sep 15;7(9):1023-33.


Macromolecular crystal annealing: evaluation of techniques and variables.

Harp JM, Hanson BL, Timm DE, Bunick GJ.

Acta Crystallogr D Biol Crystallogr. 1999 Jul;55(Pt 7):1329-34.


Macromolecular crystal annealing: overcoming increased mosaicity associated with cryocrystallography.

Harp JM, Timm DE, Bunick GJ.

Acta Crystallogr D Biol Crystallogr. 1998 Jul 1;54(Pt 4):622-8.


Characterization of the lectin from the bulbs of Eranthis hyemalis (winter aconite) as an inhibitor of protein synthesis.

Kumar MA, Timm DE, Neet KE, Owen WG, Peumans WJ, Rao AG.

J Biol Chem. 1993 Nov 25;268(33):25176-83.


Generation and transit pathway of H+ is critical for inhibition of palmar sweating by iontophoresis in water.

Sato K, Timm DE, Sato F, Templeton EA, Meletiou DS, Toyomoto T, Soos G, Sato SK.

J Appl Physiol (1985). 1993 Nov;75(5):2258-64.


Equilibrium denaturation studies of mouse beta-nerve growth factor.

Timm DE, Neet KE.

Protein Sci. 1992 Feb;1(2):236-44.


One-step iodine starch method for direct visualization of sweating.

Sato KT, Richardson A, Timm DE, Sato K.

Am J Med Sci. 1988 Jun;295(6):528-31.


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