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Author Details

David E Timm
Lilly Research Laboratories
1988
45
27
Andrej Sali (CM4AI)
PMIDPaper TitleJournal TitlePublished Year
34081466Discovery and Early Clinical Development of LY3202626, a Low-Dose, CNS-Penetrant BACE Inhibitor.J Med Chem2021
34342224Discovery of a First-in-Class Inhibitor of the PRMT5-Substrate Adaptor Interaction.J Med Chem2021
31786008Preparation and biological evaluation of BACE1 inhibitors: Leveraging trans-cyclopropyl moieties as ligand efficient conformational constraints.Bioorg Med Chem2020
29568395Merestinib (LY2801653) inhibits neurotrophic receptor kinase (NTRK) and suppresses growth of NTRK fusion bearing tumors.Oncotarget2018
29518110Cryo-electron microscopy structure of a human PRMT5:MEP50 complex.PLoS One2018
29088532Optimization of Hydroxyethylamine Transition State Isosteres as Aspartic Protease Inhibitors by Exploiting Conformational Preferences.J Med Chem2017
28406969Reconstruction of 3D structures of MET antibodies from electron microscopy 2D class averages.PLoS One2017
25609634The potent BACE1 inhibitor LY2886721 elicits robust central Aβ pharmacodynamic responses in mice, dogs, and humans.J Neurosci2015
26224994ESR and X-ray Structure Investigations on the Binding and Mechanism of Inhibition of the Native State of Myeloperoxidase with Low Molecular Weight Fragments.Appl Magn Reson2015
26001341Preparation and biological evaluation of conformationally constrained BACE1 inhibitors.Bioorg Med Chem2015
21543522Structural and functional analysis of two new positive allosteric modulators of GluA2 desensitization and deactivation.Mol Pharmacol2011
22090477Robust central reduction of amyloid-β in humans with an orally available, non-peptidic β-secretase inhibitor.J Neurosci2011
17239592Discovery of non-covalent dipeptidyl peptidase IV inhibitors which induce a conformational change in the active site.Bioorg Med Chem Lett2007
17064256Slow-onset inhibition of fumarylacetoacetate hydrolase by phosphinate mimics of the tetrahedral intermediate: kinetics, crystal structure and pharmacokinetics.Biochem J2007
16365036Pyrithiamine as a substrate for thiamine pyrophosphokinase.J Biol Chem2006
16249081Macrocyclic peptidomimetic inhibitors of beta-secretase (BACE): first X-ray structure of a macrocyclic peptidomimetic-BACE complex.Bioorg Med Chem Lett2006
16302802Preorganization of the hydroxyethylene dipeptide isostere: the preferred conformation in solution resembles the conformation bound to BACE.J Med Chem2005
14684335Phe*-Ala-based pentapeptide mimetics are BACE inhibitors: P2 and P3 SAR.Bioorg Med Chem Lett2004
15546737Aminoimidazo[1,2-a]pyridines as a new structural class of cyclin-dependent kinase inhibitors. Part 1: Design, synthesis, and biological evaluation.Bioorg Med Chem Lett2004
14749470The discovery of a new structural class of cyclin-dependent kinase inhibitors, aminoimidazo[1,2-a]pyridines.Mol Cancer Ther2004
14684336P3 cap modified Phe*-Ala series BACE inhibitors.Bioorg Med Chem Lett2004
14643321Design and synthesis of statine-containing BACE inhibitors.Bioorg Med Chem Lett2003
11154690Mechanistic inferences from the crystal structure of fumarylacetoacetate hydrolase with a bound phosphorus-based inhibitor.J Biol Chem2001
11278491Structural and functional analysis of missense mutations in fumarylacetoacetate hydrolase, the gene deficient in hereditary tyrosinemia type 1.J Biol Chem2001
11316880Structural basis of pheromone binding to mouse major urinary protein (MUP-I).Protein Sci2001
11435118The crystal structure of yeast thiamin pyrophosphokinase.Structure2001
11419946Crystal structure of thiamin pyrophosphokinase.J Mol Biol2001
11092917Asymmetries in the nucleosome core particle at 2.5 A resolution.Acta Crystallogr D Biol Crystallogr2000
11001939Structural and functional analysis of mutations in alkaptonuria.Hum Mol Genet2000
10876237Crystal structure of human homogentisate dioxygenase.Nat Struct Biol2000
10508789Crystal structure and mechanism of a carbon-carbon bond hydrolase.Structure1999
10393299Macromolecular crystal annealing: evaluation of techniques and variables.Acta Crystallogr D Biol Crystallogr1999
9761858Macromolecular crystal annealing: overcoming increased mosaicity associated with cryocrystallography.Acta Crystallogr D Biol Crystallogr1998
9232643The crystal structure of the mouse glandular kallikrein-13 (prorenin converting enzyme).Protein Sci1997
7752246The crystal structure of the N-terminal SH3 domain of Grb2.J Mol Biol1995
7890765Alteration of NH2-terminal residues of nerve growth factor affects activity and Trk binding without affecting stability or conformation.J Biol Chem1995
7634088Crystal structure of the pleckstrin homology domain from dynamin.Nat Struct Biol1994
8019416Circular dichroism and crosslinking studies of the interaction between four neurotrophins and the extracellular domain of the low-affinity neurotrophin receptor.Protein Sci1994
8161524Comparative equilibrium denaturation studies of the neurotrophins: nerve growth factor, brain-derived neurotrophic factor, neurotrophin 3, and neurotrophin 4/5.Biochemistry1994
7756976Conformational stability of dimeric proteins: quantitative studies by equilibrium denaturation.Protein Sci1994
8227081Characterization of the lectin from the bulbs of Eranthis hyemalis (winter aconite) as an inhibitor of protein synthesis.J Biol Chem1993
8307885Generation and transit pathway of H+ is critical for inhibition of palmar sweating by iontophoresis in water.J Appl Physiol (1985)1993
1304381Spectroscopic and chemical studies of the interaction between nerve growth factor (NGF) and the extracellular domain of the low affinity NGF receptor.Protein Sci1992
1304906Equilibrium denaturation studies of mouse beta-nerve growth factor.Protein Sci1992
3389391One-step iodine starch method for direct visualization of sweating.Am J Med Sci1988
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Collaborators

Institute of Pathology, Friedrich-Alexander-University Erlangen-Nuremberg
Co-authored papers 3
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Co-authored papers 3
Heartand Lung Research Institute, University of Cambridge
Co-authored papers 2
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Co-authored papers 1
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Co-authored papers 1
University of California San Francisco
Co-authored papers 1
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Co-authored papers 1
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Co-authored papers 1
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University of California san francisco
Co-authored papers 1
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Co-authored papers 1
The Hebrew University of Jerusalem
Co-authored papers 1
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Co-authored papers 1