Published in J Biomol Screen on December 27, 2013
Biophysics in drug discovery: impact, challenges and opportunities. Nat Rev Drug Discov (2016) 0.81
Refinement of macromolecular structures by the maximum-likelihood method. Acta Crystallogr D Biol Crystallogr (1997) 137.43
Scaling and assessment of data quality. Acta Crystallogr D Biol Crystallogr (2005) 61.38
Molecular replacement with MOLREP. Acta Crystallogr D Biol Crystallogr (2009) 26.26
The integration of macromolecular diffraction data. Acta Crystallogr D Biol Crystallogr (2005) 19.21
Fragment-based drug discovery. J Med Chem (2004) 2.07
Fragment-based lead discovery: leads by design. Drug Discov Today (2005) 1.91
Screening in a spirit haunted world. Drug Discov Today (2006) 1.75
Immunohistochemical localization of PDE10A in the rat brain. Brain Res (2003) 1.61
Immunohistochemical localization of phosphodiesterase 10A in multiple mammalian species. J Histochem Cytochem (2006) 1.60
Preclinical characterization of selective phosphodiesterase 10A inhibitors: a new therapeutic approach to the treatment of schizophrenia. J Pharmacol Exp Ther (2008) 1.60
Enthalpy arrays. Proc Natl Acad Sci U S A (2004) 1.52
Inhibition of the striatum-enriched phosphodiesterase PDE10A: a novel approach to the treatment of psychosis. Neuropharmacology (2006) 1.44
Striatum- and testis-specific phosphodiesterase PDE10A isolation and characterization of a rat PDE10A. Eur J Biochem (1999) 1.41
Cellular and subcellular localization of PDE10A, a striatum-enriched phosphodiesterase. Neuroscience (2006) 1.37
Phosphodiesterase 10A inhibitor activity in preclinical models of the positive, cognitive, and negative symptoms of schizophrenia. J Pharmacol Exp Ther (2009) 1.35
Structural insight into substrate specificity of phosphodiesterase 10. Proc Natl Acad Sci U S A (2007) 1.22
Current landscape of phosphodiesterase 10A (PDE10A) inhibition. J Med Chem (2012) 1.20
PDE10A inhibition reverses subchronic PCP-induced deficits in attentional set-shifting in rats. Eur J Neurosci (2005) 1.13
Inhibition of the striatal specific phosphodiesterase PDE10A ameliorates striatal and cortical pathology in R6/2 mouse model of Huntington's disease. PLoS One (2010) 1.11
Higher throughput calorimetry: opportunities, approaches and challenges. Curr Opin Struct Biol (2010) 1.04
Measurement of enzyme kinetics and inhibitor constants using enthalpy arrays. Anal Biochem (2009) 0.90
The molecular basis for different recognition of substrates by phosphodiesterase families 4 and 10. J Mol Biol (2007) 0.90
Parallel screening of low molecular weight fragment libraries: do differences in methodology affect hit identification? J Biomol Screen (2012) 0.89
A comparative study of fragment screening methods on the p38α kinase: new methods, new insights. J Comput Aided Mol Des (2011) 0.85
Fragment-based screening for inhibitors of PDE4A using enthalpy arrays and X-ray crystallography. J Biomol Screen (2012) 0.84
Start small and stay small. Minimizing attrition in the clinic with a focus on CNS therapeutics. Curr Top Med Chem (2009) 0.78
Structure of a c-kit product complex reveals the basis for kinase transactivation. J Biol Chem (2003) 1.95
A novel mode of Gleevec binding is revealed by the structure of spleen tyrosine kinase. J Biol Chem (2004) 1.55
Structural and kinetic analysis of the substrate specificity of human fibroblast activation protein alpha. J Biol Chem (2005) 1.44
Structural studies of Salmonella typhimurium ArnB (PmrH) aminotransferase: a 4-amino-4-deoxy-L-arabinose lipopolysaccharide-modifying enzyme. Structure (2002) 1.41
SGX523 is an exquisitely selective, ATP-competitive inhibitor of the MET receptor tyrosine kinase with antitumor activity in vivo. Mol Cancer Ther (2009) 1.23
Total synthesis of the ramoplanin A2 and ramoplanose aglycon. J Am Chem Soc (2002) 1.05
Dynamic coupling between the SH2 domain and active site of the COOH terminal Src kinase, Csk. J Mol Biol (2004) 1.02
Total synthesis of the ramoplanin A2 and ramoplanose aglycon. J Am Chem Soc (2003) 0.99
Design, synthesis and structure-activity relationships of novel taxane-based multidrug resistance reversal agents. J Med Chem (2005) 0.98
The 1.59 A resolution crystal structure of TM0096, a flavin mononucleotide binding protein from Thermotoga maritima. Proteins (2004) 0.95
X-ray crystal structures of monomeric and dimeric peptide inhibitors in complex with the human neonatal Fc receptor, FcRn. J Biol Chem (2010) 0.95
Azotobacter vinelandii ferredoxin I: a sequence and structure comparison approach to alteration of [4Fe-4S]2+/+ reduction potential. J Biol Chem (2001) 0.86
Fragment-based screening for inhibitors of PDE4A using enthalpy arrays and X-ray crystallography. J Biomol Screen (2012) 0.84
The structure of LpxD from Pseudomonas aeruginosa at 1.3 Å resolution. Acta Crystallogr Sect F Struct Biol Cryst Commun (2011) 0.84
Analysis of trafficking, stability and function of human connexin 26 gap junction channels with deafness-causing mutations in the fourth transmembrane helix. PLoS One (2013) 0.82
Rapid mixing of sub-microlitre drops by magnetic micro-stirring. Lab Chip (2011) 0.81
Comparative structural analysis of a novel glutathioneS-transferase (ATU5508) from Agrobacterium tumefaciens at 2.0 A resolution. Proteins (2006) 0.79
Structure determination of LpxD from the lipopolysaccharide-synthesis pathway of Acinetobacter baumannii. Acta Crystallogr Sect F Struct Biol Cryst Commun (2012) 0.78
Crystal structures of transhydrogenase domain I with and without bound NADH. Biochemistry (2002) 0.78
Interaction with the S1 beta-pocket of urokinase: 8-heterocycle substituted and 6,8-disubstituted 2-naphthamidine urokinase inhibitors. Bioorg Med Chem Lett (2004) 0.78
Crystal structure of YIGZ, a conserved hypothetical protein from Escherichia coli k12 with a novel fold. Proteins (2004) 0.77
Structure determination of LpxA from the lipopolysaccharide-synthesis pathway of Acinetobacter baumannii. Acta Crystallogr Sect F Struct Biol Cryst Commun (2012) 0.76
Is X-ray crystallography a viable tool for lead discovery? Drug Discov Today (2002) 0.75