Development of a lead inhibitor for the A16V+S108T mutant of dihydrofolate reductase from the cycloguanil-resistant strain (T9/94) of Plasmodium falciparum.

PubWeight™: 0.83‹?›

🔗 View Article (PMID 10893311)

Published in J Med Chem on July 13, 2000

Authors

Y Yuthavong1, T Vilaivan, N Chareonsethakul, S Kamchonwongpaisan, W Sirawaraporn, R Quarrell, G Lowe

Author Affiliations

1: National Center for Genetic Engineering and Biotechnology, National Science and Technology Development Agency, Bangkok 10400, Thailand.

Articles by these authors

Artemisinin and the antimalarial endoperoxides: from herbal remedy to targeted chemotherapy. Microbiol Rev (1996) 3.26

Primary prevention for alcohol misuse in young people. Cochrane Database Syst Rev (2002) 2.80

Disruption of the type III adenylyl cyclase gene leads to peripheral and behavioral anosmia in transgenic mice. Neuron (2000) 2.73

Longer-term primary prevention for alcohol misuse in young people: a systematic review. Addiction (2003) 2.67

The proton flux through the bacterial flagellar motor. Cell (1987) 2.56

Evidence for histidine in the active site of papain. Biochem J (1968) 2.16

Increased susceptibility of malaria-infected variant erythrocytes to the mononuclear phagocyte system. Blood Cells (1990) 2.06

Tanning with ultraviolet A sunbeds. BMJ (1990) 1.93

Influence of age-related maculopathy on visual functioning and health-related quality of life. Am J Ophthalmol (1999) 1.86

A comparison of the associations between seven hemostatic or inflammatory variables and coronary heart disease. J Thromb Haemost (2007) 1.69

Kinetic specificity in papain-catalysed hydrolyses. Biochem J (1971) 1.60

Formation of precise connections in the olfactory bulb occurs in the absence of odorant-evoked neuronal activity. Neuron (2000) 1.52

Iron-dependent free radical generation from the antimalarial agent artemisinin (qinghaosu). Antimicrob Agents Chemother (1993) 1.50

Delayed progression to AIDS in volunteers treated with long-term HIV-1 Immunogen (REMUNE) therapy in Thailand. HIV Med (2004) 1.45

The location of the active-site histidine residue in the primary sequence of papain. Biochem J (1968) 1.44

A systematic review of drug-induced subacute cutaneous lupus erythematosus. Br J Dermatol (2011) 1.42

Malarial (Plasmodium falciparum) dihydrofolate reductase-thymidylate synthase: structural basis for antifolate resistance and development of effective inhibitors. Parasitology (2005) 1.35

Crystal structure of Mycobacterium tuberculosis 7,8-dihydropteroate synthase in complex with pterin monophosphate: new insight into the enzymatic mechanism and sulfa-drug action. J Mol Biol (2000) 1.32

Investigation of the active site of papain with fluorescent probes. Biochem J (1973) 1.30

Beta-lactamase inhibitors. The inhibition of serine beta-lactamases by specific boronic acids. Biochem J (1988) 1.29

Association of IL-10 polymorphism with severity of illness in community acquired pneumonia. Thorax (2003) 1.28

Three-dimensional structure of M. tuberculosis dihydrofolate reductase reveals opportunities for the design of novel tuberculosis drugs. J Mol Biol (2000) 1.27

The amino acid sequence around the active-site cysteine and histidine residues, and the buried cysteine residue in ficin. Biochem J (1970) 1.26

Completion of the amino acid sequence of papain. Biochem J (1969) 1.24

Human Dermo-1 has attributes similar to twist in early bone development. Bone (2000) 1.20

pH-dependence and structure-activity relationships in the papain-catalysed hydrolysis of anilides. Biochem J (1971) 1.19

Expression of human thymidylate synthase in Escherichia coli. J Biol Chem (1989) 1.18

Adolescent drinking behaviour and family socialization factors: a meta-analysis. J Adolesc (1991) 1.17

Kinetic and molecular properties of dihydrofolate reductase from pyrimethamine-sensitive and pyrimethamine-resistant Plasmodium chabaudi. Mol Biochem Parasitol (1984) 1.13

Phosphatidylinositol synthase and phosphatidylinositol/inositol exchange reactions in turkey erythrocyte membranes. Biochem J (1991) 1.13

Hen egg white lysozyme expressed in, and secreted from, Aspergillus niger is correctly processed and folded. Biotechnology (N Y) (1990) 1.09

The amino acid sequence around the active-site cysteine and histidine residues of stem bromelain. Biochem J (1970) 1.07

Interaction of pyrimethamine, cycloguanil, WR99210 and their analogues with Plasmodium falciparum dihydrofolate reductase: structural basis of antifolate resistance. Bioorg Med Chem (2000) 1.07

Alcohol misuse prevention for young people: a systematic review reveals methodological concerns and lack of reliable evidence of effectiveness. Addiction (1997) 1.06

A reinvestigation of residues 64-68 and 175 in papain. Evidence that residues 64 and 175 are asparagine. Biochem J (1970) 1.05

Suppression of odorant responses by odorants in olfactory receptor cells. Science (1994) 1.04

Cloning and expression of Mycobacterium tuberculosis and Mycobacterium leprae dihydropteroate synthase in Escherichia coli. J Bacteriol (1999) 1.03

A kinetic and fluorimetric investigation of papain modified at tryptophan-69 and -177 by N-bromosuccinimide. Biochem J (1974) 1.01

The structure and mechanism of action of papain. Philos Trans R Soc Lond B Biol Sci (1970) 1.00

Stereochemistry of phosphoryl transfer. Philos Trans R Soc Lond B Biol Sci (1981) 1.00

An international multicenter randomized study of computer-assisted oral anticoagulant dosage vs. medical staff dosage. J Thromb Haemost (2008) 1.00

The stereochemical course of phosphoryl transfer catalysed by polynucleotide kinase (bacteriophage-T4-infected Escherichia coli B). Biochem J (1981) 0.99

Co-operative ionisation of aspartic-acid-158 and histidine-159 in papain. Evidence from 19F nuclear-magnetic-resonance and fluorescence spectroscopy. Eur J Biochem (1976) 0.97

Presence of t(8;21)(q22;q22) in myeloperoxidase-positive, myeloid surface antigen-negative acute myeloid leukemia. Am J Clin Pathol (1997) 0.96

Lysozyme-catalysed hydrolysis of some beta-aryl di-N-acetylchitobiosides. Biochem J (1967) 0.96

The stereochemical course of yeast hexokinase-catalysed phosphoryl transfer by using adenosine 5'[gamma(S)-16O,17O,18O]triphosphate as substrate. Biochem J (1981) 0.96

Catalytic mechanism of phosphorylase kinase probed by mutational studies. Biochemistry (1999) 0.95

Socioeconomic inequalities in coronary heart disease risk in older age: contribution of established and novel coronary risk factors. J Thromb Haemost (2009) 0.95

A three-disulphide derivative of hen lysozyme. Structure, dynamics and stability. Biochem J (1991) 0.94

Bayesian methods for meta-analysis of causal relationships estimated using genetic instrumental variables. Stat Med (2010) 0.93

Heterologous expression of the bifunctional thymidylate synthase-dihydrofolate reductase from Leishmania major. Biochemistry (1988) 0.93

Calcium permeable AMPA receptors and autoreceptors in external tufted cells of rat olfactory bulb. Neuroscience (2006) 0.92

Evaluation of resins for on-bead screening: a study of papain and chymotrypsin specificity using PEGA-bound combinatorial peptide libraries. Bioorg Med Chem Lett (1998) 0.92

Possible hydrolytic mechanisms. Proc R Soc Lond B Biol Sci (1967) 0.91

Inhibition of papain by N-acyl-aminoacetaldehydes and N-acyl-aminopropanones. Evidence for hemithioacetal formation by a cross-saturation technique in nuclear-magnetic resonance spectroscopy. Eur J Biochem (1977) 0.90

Peripheral vascular disease. Rheologic variables during controlled ischemia. Circulation (1989) 0.90

Rational drug design approach for overcoming drug resistance: application to pyrimethamine resistance in malaria. J Med Chem (1998) 0.90

Chemical synthesis of the Plasmodium falciparum dihydrofolate reductase-thymidylate synthase gene. Mol Biochem Parasitol (1996) 0.90

Human thioredoxin reductase is efficiently inhibited by (2,2':6',2' '-terpyridine)platinum(II) complexes. Possible implications for a novel antitumor strategy. J Med Chem (2001) 0.90

Characteristics and risk factors of Plasmodium falciparum malaria in Eastern and Central Nepal. Kathmandu Univ Med J (KUMJ) (2010) 0.88

Hypocalcemic tetany and metabolic alkalosis in a dialysis patient: an unusual event. Am J Kidney Dis (1997) 0.88

Natural acetylenes. XXII. Trans-Dehydromatricaria ester as a biosynthetic precursor of some fungal polyacetylenes. J Chem Soc Perkin 1 (1966) 0.88

Scottish Intercollegiate Guidelines Network: the first 15 years (1993-2008). J R Coll Physicians Edinb (2011) 0.88

(2,2':6',2"-Terpyridine)platinum(II) complexes are irreversible inhibitors of Trypanosoma cruzi trypanothione reductase but not of human glutathione reductase. J Med Chem (2000) 0.88

Inhibition of human leukocyte and porcine pancreatic elastase by homologues of bovine pancreatic trypsin inhibitor. Biochemistry (1996) 0.87

The specificity of the S1' subsite of papain. Biochem J (1974) 0.87

The stereochemical course of phosphoryl transfer catalysed by Bacillus stearothermophilus and rabbit skeletal-muscle phosphofructokinase with a chiral [16O,17O,18O]phosphate ester. Biochem J (1981) 0.86

The prevalence and analysis of risk factors for age-related macular degeneration: 18-year follow-up data from the Speedwell eye study, United Kingdom. Eye (Lond) (2011) 0.86

Cytotoxicity of 2,2':6',2' '-terpyridineplatinum(II) complexes against human ovarian carcinoma. J Med Chem (1999) 0.86

Crystal structure of the mutant D52S hen egg white lysozyme with an oligosaccharide product. J Mol Biol (1994) 0.85

A double-blind, adjuvant-controlled trial of human immunodeficiency virus type 1 (HIV-1) immunogen (Remune) monotherapy in asymptomatic, HIV-1-infected thai subjects with CD4-cell counts of >300. Clin Diagn Lab Immunol (2000) 0.85

Cytotoxic labdane diterpenoids from Croton oblongifolius. Phytochemistry (2001) 0.85

Diffusion through narrow pores: movement of ions, water and nonelectrolytes through track-etched PETP membranes. J Membr Biol (1996) 0.84

Academic stress and secretory immunoglobulin A. Psychol Rep (2000) 0.84

Safety and immunogenicity of REMUNE in HIV-infected Thai subjects. Vaccine (1998) 0.84

Studies of inositol analogues as inhibitors of the phosphoinositide pathway, and incorporation of 2-deoxy-2-fluoro-myo-inositol to give analogues of phosphatidylinositol intermediates. Biochem J (1991) 0.84

Evidence for hemiacetal formation between N-acyl-L-phenylalaninals and alpha-chymotrypsin by cross-saturation nuclear magnetic resonance spectroscopy. Biochemistry (1979) 0.84

D.D.A.V.P. in haemophilia. Lancet (1977) 0.83

Single odorant molecules? Nature (1995) 0.83

Sarcoidosis and coeliac disease. Lancet (1984) 0.83

Correlated firing in tufted cells of mouse olfactory bulb. Neuroscience (2010) 0.82

4-Picoline-2,2':6',2"-terpyridine-platinum(II) - a potent intercalator of DNA. FEBS Lett (1996) 0.82

Bioxanthracenes from the insect pathogenic fungus. Cordyceps pseudomilitaris BCC 1620. I. Taxonomy, fermentation, isolation and antimalarial activity. J Antibiot (Tokyo) (2001) 0.82

Conversion of the active-site cysteine residue of papain into a dehydro-serine, a serine and a glycine residue. Eur J Biochem (1978) 0.82

The pKa value of the active site histidine in photo-oxidised papain. FEBS Lett (1976) 0.82

Inactivation of artemisinin by thalassemic erythrocytes. Biochem Pharmacol (2000) 0.82

Clear-cell carcinoma of the ovary in a 19-year-old woman. Aust N Z J Obstet Gynaecol (1998) 0.81

Evidence for cross-linking DNA by bis-intercalators with rigid and extended linkers is provided by knotting and catenation. Nucleic Acids Res (1992) 0.81

Structure and properties of TentaGel resin beads: implications for combinatorial library chemistry. Mol Divers (1996) 0.81

Inhibition of fructose-1,6-bisphosphate aldolase from rabbit muscle and Bacillus stearothermophilus. Eur J Biochem (1977) 0.81

Synthesis of (Rp,Rp)-P1,P4-Bis(5'-adenosyl)-1[17O,18O2],4[17O,18O2] tetraphosphate from (Sp,Sp)-P1,P4-Bis(5'-adenosyl)-1[thio-18O2], 4[thio-18O2]tetraphosphate with retention at phosphorus and the stereochemical course of hydrolysis by the unsymmetrical Ap4A phosphodiesterase from lupin seeds. J Biol Chem (1989) 0.81

A stereochemical investigation of the hydrolysis of cyclic AMP and the (Sp)-and (Rp)-diastereoisomers of adenosine cyclic 3':5'-phosphorothioate by bovine heart and baker's-yeast cyclic AMP phosphodiesterases. Biochem J (1982) 0.81

Cytotoxicity of (2,2':6',2''-terpyridine)platinum(II) complexes to Leishmania donovani, Trypanosoma cruzi, and Trypanosoma brucei. J Med Chem (1999) 0.81

The stereochemical course of nucleotidyl transfer catalyzed by ATP sulfurylase. J Biol Chem (1982) 0.80