Published in J Med Chem on March 26, 2012
Targeting lactate dehydrogenase--a inhibits tumorigenesis and tumor progression in mouse models of lung cancer and impacts tumor-initiating cells. Cell Metab (2014) 1.92
Regulation of pyruvate metabolism and human disease. Cell Mol Life Sci (2013) 1.21
Anticancer agents that counteract tumor glycolysis. ChemMedChem (2012) 1.17
Using a fragment-based approach to target protein-protein interactions. Chembiochem (2013) 1.09
Quinoline 3-sulfonamides inhibit lactate dehydrogenase A and reverse aerobic glycolysis in cancer cells. Cancer Metab (2013) 1.04
Fragment-based screening by protein crystallography: successes and pitfalls. Int J Mol Sci (2012) 0.96
Twenty years on: the impact of fragments on drug discovery. Nat Rev Drug Discov (2016) 0.92
Mapping the protein interaction landscape for fully functionalized small-molecule probes in human cells. J Am Chem Soc (2014) 0.92
Dual targeting of the Warburg effect with a glucose-conjugated lactate dehydrogenase inhibitor. Chembiochem (2013) 0.91
Lactate dehydrogenase-B is silenced by promoter methylation in a high frequency of human breast cancers. PLoS One (2013) 0.88
Pyridomycin bridges the NADH- and substrate-binding pockets of the enoyl reductase InhA. Nat Chem Biol (2013) 0.87
Small-molecule inhibitors of human LDH5. Future Med Chem (2013) 0.86
Assessing the differential action on cancer cells of LDH-A inhibitors based on the N-hydroxyindole-2-carboxylate (NHI) and malonic (Mal) scaffolds. Org Biomol Chem (2013) 0.85
Synergistic inhibitor binding to the papain-like protease of human SARS coronavirus: mechanistic and inhibitor design implications. ChemMedChem (2013) 0.82
Human lactate dehydrogenase a inhibitors: a molecular dynamics investigation. PLoS One (2014) 0.80
Structural characterization of the apo form and NADH binary complex of human lactate dehydrogenase. Acta Crystallogr D Biol Crystallogr (2014) 0.80
Intercepting the Breslow intermediate via Claisen rearrangement: synthesis of complex tertiary alcohols without organometallic reagents. Org Lett (2012) 0.79
Search for Human Lactate Dehydrogenase A Inhibitors Using Structure-Based Modeling. Acta Naturae (2015) 0.77
A Streamlined, Automated Protocol for the Production of Milligram Quantities of Untagged Recombinant Rat Lactate Dehydrogenase A Using ÄKTAxpressTM. PLoS One (2015) 0.76
Identification of New Structural Fragments for the Design of Lactate Dehydrogenase A Inhibitors. Acta Naturae (2016) 0.75
Cell Active Hydroxylactam Inhibitors of Human Lactate Dehydrogenase with Oral Bioavailability in Mice. ACS Med Chem Lett (2016) 0.75
Targeting Metabolic Remodeling in Triple Negative Breast Cancer in a Murine Model. J Cancer (2017) 0.75
Short term outcomes of prostate biopsy in men tested for cancer by prostate specific antigen: prospective evaluation within ProtecT study. BMJ (2012) 4.64
Reduction in critical mortality in urban mass casualty incidents: analysis of triage, surge, and resource use after the London bombings on July 7, 2005. Lancet (2006) 4.60
Consensus statements for management of Barrett's dysplasia and early-stage esophageal adenocarcinoma, based on a Delphi process. Gastroenterology (2012) 2.68
FMD control strategies. Vet Rec (2003) 2.23
FMD control measures. Vet Rec (2007) 2.02
Preclinical anticancer activity of the potent, oral Src inhibitor AZD0530. Mol Oncol (2009) 1.61
Common variants at the MHC locus and at chromosome 16q24.1 predispose to Barrett's esophagus. Nat Genet (2012) 1.52
Journal club: national variability in intracranial pressure monitoring and craniotomy for children with moderate to severe traumatic brain injury. Neurosurgery (2014) 1.39
The presentation and management of victims of chemical and biological agents: a survey of knowledge of UK clinicians. Resuscitation (2003) 1.39
Prehospital thoracostomy. Eur J Emerg Med (2008) 1.38
Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor. J Med Chem (2014) 1.36
The Mycobacterium tuberculosis ino1 gene is essential for growth and virulence. Mol Microbiol (2004) 1.34
Structure-based design of a potent purine-based cyclin-dependent kinase inhibitor. Nat Struct Biol (2002) 1.27
Traumatic cardiac arrest: who are the survivors? Ann Emerg Med (2006) 1.25
Fragment screening to predict druggability (ligandability) and lead discovery success. Drug Discov Today (2011) 1.22
Crystal structures of human ADAMTS-1 reveal a conserved catalytic domain and a disintegrin-like domain with a fold homologous to cysteine-rich domains. J Mol Biol (2007) 1.18
Peptide binding induces large scale changes in inter-domain mobility in human Pin1. J Biol Chem (2003) 1.18
Prevention of MKK6-dependent activation by binding to p38alpha MAP kinase. Biochemistry (2005) 1.11
NMR backbone assignment of a protein kinase catalytic domain by a combination of several approaches: application to the catalytic subunit of cAMP-dependent protein kinase. Chembiochem (2004) 1.10
How tyrosine 15 phosphorylation inhibits the activity of cyclin-dependent kinase 2-cyclin A. J Biol Chem (2006) 1.07
Journal club: Magnetic resonance imaging-guided focused laser interstitial thermal therapy for intracranial lesions: single-institution series. Neurosurgery (2014) 1.07
Cyclin-dependent kinase 4 inhibitors as a treatment for cancer. Part 2: identification and optimisation of substituted 2,4-bis anilino pyrimidines. Bioorg Med Chem Lett (2003) 1.05
Integrin alpha5beta1 and ADAM-17 interact in vitro and co-localize in migrating HeLa cells. J Biol Chem (2004) 1.03
Exploiting structural information in patent specifications for key compound prediction. J Chem Inf Model (2012) 0.97
An integrated approach to fragment-based lead generation: philosophy, strategy and case studies from AstraZeneca's drug discovery programmes. Curr Top Med Chem (2007) 0.96
NMR backbone assignment of the mitogen-activated protein (MAP) kinase p38. J Biomol NMR (2005) 0.93
The development and initial validation of a questionnaire to measure craving for amphetamine. Addiction (2004) 0.93
Structure-based design of protein tyrosine phosphatase-1B inhibitors. Bioorg Med Chem Lett (2005) 0.92
Introduction and use of the ProSeal laryngeal mask airway as a rescue device in a pre-hospital trauma anaesthesia algorithm. Resuscitation (2008) 0.92
Imidazo[1,2-a]pyridines: a potent and selective class of cyclin-dependent kinase inhibitors identified through structure-based hybridisation. Bioorg Med Chem Lett (2003) 0.91
Crystal structure of human thymidine phosphorylase in complex with a small molecule inhibitor. Structure (2004) 0.91
Aminopyrazinamides: novel and specific GyrB inhibitors that kill replicating and nonreplicating Mycobacterium tuberculosis. ACS Chem Biol (2012) 0.90
Probing the ATP ribose-binding domain of cyclin-dependent kinases 1 and 2 with O(6)-substituted guanine derivatives. J Med Chem (2002) 0.90
Small-molecule proteomimetic inhibitors of the HIF-1α-p300 protein-protein interaction. Chembiochem (2014) 0.89
Do interleukin-1 polymorphisms predict the development of periodontitis or the success of dental implants? J Periodontal Res (2002) 0.89
Cyclin-dependent kinase 4 inhibitors as a treatment for cancer. Part 1: identification and optimisation of substituted 4,6-bis anilino pyrimidines. Bioorg Med Chem Lett (2003) 0.89
Biophysical methods in drug discovery from small molecule to pharmaceutical. Methods Mol Biol (2013) 0.88
Transcobalamin polymorphism and serum holo-transcobalamin in relation to Alzheimer's disease. Dement Geriatr Cogn Disord (2004) 0.88
Endovascular coiling of an internal mammary artery pseudoaneurysm following placement of an internal jugular central venous catheter. Mil Med (2010) 0.88
Th1 cytokines are more effective than Th2 cytokines at licensing anti-tumour functions in CD40-activated human macrophages in vitro. Eur J Immunol (2013) 0.88
Methyl-thiazoles: a novel mode of inhibition with the potential to develop novel inhibitors targeting InhA in Mycobacterium tuberculosis. J Med Chem (2013) 0.88
Fragment screening by weak affinity chromatography: comparison with established techniques for screening against HSP90. Anal Chem (2013) 0.87
Structures of the human poly (ADP-ribose) glycohydrolase catalytic domain confirm catalytic mechanism and explain inhibition by ADP-HPD derivatives. PLoS One (2012) 0.87
A novel DYRK1B inhibitor AZ191 demonstrates that DYRK1B acts independently of GSK3β to phosphorylate cyclin D1 at Thr(286), not Thr(288). Biochem J (2014) 0.87
Alzheimer's disease and total plasma aminothiols. Biol Psychiatry (2003) 0.87
Novel 4-anilinoquinazolines with C-6 carbon-linked side chains: synthesis and structure-activity relationship of a series of potent, orally active, EGF receptor tyrosine kinase inhibitors. Bioorg Med Chem Lett (2006) 0.86
Real-time monitoring of New Delhi metallo-β-lactamase activity in living bacterial cells by 1H NMR spectroscopy. Angew Chem Int Ed Engl (2014) 0.86
Discovery of 4-amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide (AZD5363), an orally bioavailable, potent inhibitor of Akt kinases. J Med Chem (2013) 0.86
MDM4 binds ligands via a mechanism in which disordered regions become structured. FEBS Lett (2010) 0.85
Structure-Guided Design of Highly Selective and Potent Covalent Inhibitors of ERK1/2. J Med Chem (2015) 0.85
Body temperature of trauma patients on admission to hospital: a comparison of anaesthetised and non-anaesthetised patients. Emerg Med J (2010) 0.85
Imidazo[1,2-b]pyridazines: a potent and selective class of cyclin-dependent kinase inhibitors. Bioorg Med Chem Lett (2004) 0.85
The emergency control of traumatic maxillofacial haemorrhage. Eur J Emerg Med (2010) 0.84
Serum insulin-like growth factors and mortality in localised and advanced clinically detected prostate cancer. Cancer Causes Control (2011) 0.83
A new series of neutral 5-substituted 4-anilinoquinazolines as potent, orally active inhibitors of erbB2 receptor tyrosine kinase. Bioorg Med Chem Lett (2007) 0.83
Discovery of azabenzimidazole derivatives as potent, selective inhibitors of TBK1/IKKε kinases. Bioorg Med Chem Lett (2012) 0.82
The discovery of AZD5597, a potent imidazole pyrimidine amide CDK inhibitor suitable for intravenous dosing. Bioorg Med Chem Lett (2008) 0.82
Prehospital end-tidal carbon dioxide concentration and outcome in major trauma. J Trauma (2004) 0.82
Restenosis in gold-coated renal artery stents. J Vasc Surg (2005) 0.82
Novel thienopyrimidine and thiazolopyrimidine kinase inhibitors with activity against Tie-2 in vitro and in vivo. Bioorg Med Chem Lett (2009) 0.81
¹H, ¹³C and ¹⁵N resonance assignment for the human K-Ras at physiological pH. Biomol NMR Assign (2012) 0.81
Small molecule binding sites on the Ras:SOS complex can be exploited for inhibition of Ras activation. J Med Chem (2015) 0.81
The challenges of deliberate chemical/biological attack. Resuscitation (2003) 0.80
Exploration of the HIF-1α/p300 interface using peptide and Adhiron phage display technologies. Mol Biosyst (2015) 0.80
Prehospital intranasal evaporative cooling for out-of-hospital cardiac arrest: a pilot, feasibility study. Eur J Emerg Med (2014) 0.80
A study of patients presenting to an emergency department having had a "spiked drink". Emerg Med J (2007) 0.80
Enzymatic characterisation of USP7 deubiquitinating activity and inhibition. Cell Biochem Biophys (2011) 0.80
The Effects of Temperature on Clot Microstructure and Strength in Healthy Volunteers. Anesth Analg (2016) 0.79
Imidazoles: SAR and development of a potent class of cyclin-dependent kinase inhibitors. Bioorg Med Chem Lett (2008) 0.79
NMR backbone assignment of the N-terminal domain of human HSP90. J Biomol NMR (2006) 0.79
Matrix metalloproteinase 17 is necessary for cartilage aggrecan degradation in an inflammatory environment. Ann Rheum Dis (2011) 0.79
Folding and activity of cAMP-dependent protein kinase mutants. FEBS Lett (2005) 0.79
The design and synthesis of novel, potent and orally bioavailable N-aryl piperazine-1-carboxamide CCR2 antagonists with very high hERG selectivity. Bioorg Med Chem Lett (2012) 0.78
Co-administration of N-acetylcysteine, vitamin B12 and folate in cognitively impaired hyperhomocysteinaemic patients. Int J Geriatr Psychiatry (2005) 0.78
Neutral 5-substituted 4-indazolylaminoquinazolines as potent, orally active inhibitors of erbB2 receptor tyrosine kinase. Bioorg Med Chem Lett (2008) 0.78
Enzyme kinetics and binding studies on inhibitors of MEK protein kinase. Biochemistry (2008) 0.78
Structure guided lead generation for M. tuberculosis thymidylate kinase (Mtb TMK): discovery of 3-cyanopyridone and 1,6-naphthyridin-2-one as potent inhibitors. J Med Chem (2014) 0.78
Thiazolopyridine ureas as novel antitubercular agents acting through inhibition of DNA Gyrase B. J Med Chem (2013) 0.78
Backbone NMR assignment of the low-molecular-weight protein tyrosine phosphatase (MPtpA) from Mycobacterium tuberculosis. J Biomol NMR (2005) 0.77
Discovery of AZD3147: a potent, selective dual inhibitor of mTORC1 and mTORC2. J Med Chem (2015) 0.77
Structure-based design of peptidomimetic antagonists of p56(lck) SH2 domain. Bioorg Med Chem Lett (2002) 0.77
Imidazole piperazines: SAR and development of a potent class of cyclin-dependent kinase inhibitors with a novel binding mode. Bioorg Med Chem Lett (2008) 0.77
A pilot evaluation of the use of tissue microarrays for quantitation of target distribution in drug discovery pathology. Exp Toxicol Pathol (2005) 0.77
Target-based whole-cell screening by ¹H NMR spectroscopy. Angew Chem Int Ed Engl (2015) 0.77
Rapid generation of a high quality lead for transforming growth factor-beta (TGF-beta) type I receptor (ALK5). J Med Chem (2009) 0.76
1H, 13C and 15N backbone resonance assignment of the peptidyl-prolyl cis-trans isomerase Pin1. J Biomol NMR (2002) 0.76
Characterization of the complex formed between a potent neutralizing ovine-derived polyclonal anti-TNFα Fab fragment and human TNFα. Biosci Rep (2013) 0.76
How much NMR data is required to determine a protein-ligand complex structure? Chembiochem (2005) 0.76