Shape shifting leads to small-molecule allosteric drug discovery.

No abstract is available for this paper.

• Publication year

  2008

• Venue

  Chemistry and Biology

• Publication date

  2008-06-23

• Fields of study

  Biology, Medicine, Chemistry

• Identifiers
  DOI 10.1016/j.chembiol.2008.04.012PMID 18559269PMCID PMC2703447
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• Adapting Proteostasis for Disease Intervention

  2008cited by this paper
• Kinetics and thermodynamics of the interchange of the morpheein forms of human porphobilinogen synthase.

  2008cited by this paper
• ALAD porphyria is a conformational disease.

  2007cited by this paper
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  2007cited by this paper
• Synergistic Substrate Inhibition of ent-Copalyl Diphosphate Synthase: A Potential Feed-Forward Inhibition Mechanism Limiting Gibberellin Metabolism1[OA]

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  2006cited by this paper
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  2006cited by this paper
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  2006cited by this paper
• A detergent-based assay for the detection of promiscuous inhibitors

  2006cited by this paper
• Small-molecule inhibition of TNF-alpha.

  2005cited by this paper
• Small-Molecule Inhibition of TNF-α

  2005cited by this paper
• Morpheeins--a new structural paradigm for allosteric regulation.

  2005cited by this paper
• Substrate-induced Interconversion of Protein Quaternary Structure Isoforms*

  2005cited by this paper
• MollDE: a homology modeling framework you can click with

  2005cited by this paper
• Rhodobacter capsulatus porphobilinogen synthase, a high activity metal ion independent hexamer

  2004cited by this paper
• Glide: a new approach for rapid, accurate docking and scoring. 2. Enrichment factors in database screening.

  2004cited by this paper
• The porphobilinogen synthase catalyzed reaction mechanism.

  2004cited by this paper
• Searching for new allosteric sites in enzymes.

  2004cited by this paper
• Control of tetrapyrrole biosynthesis by alternate quaternary forms of porphobilinogen synthase

  2003cited by this paper
• Conformational diversity and protein evolution--a 60-year-old hypothesis revisited.

  2003cited by this paper
• An unusual phylogenetic variation in the metal ion binding sites of porphobilinogen synthase.

  2003cited by this paper
• Structure of porphobilinogen synthase from Pseudomonas aeruginosa in complex with 5-fluorolevulinic acid suggests a double Schiff base mechanism.

  2002cited by this paper
• Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings.

  2001cited by this paper
• Tetrapyrroles: the pigments of life.

  2000cited by this paper
• Porphobilinogen synthase from pea: expression from an artificial gene, kinetic characterization, and novel implications for subunit interactions.

  2000cited by this paper
• Prediction of drug solubility from Monte Carlo simulations.

  2000cited by this paper
• The structure of mouse tumour-necrosis factor at 1.4 A resolution: towards modulation of its selectivity and trimerization.

  1999cited by this paper
• High resolution crystal structure of a Mg2+-dependent porphobilinogen synthase.

  1999cited by this paper
• 5-Aminolevulinic acid dehydratase deficiency porphyria: a twenty-year clinical and biochemical follow-up.

  1998cited by this paper
• Empirical scoring functions: I. The development of a fast empirical scoring function to estimate the binding affinity of ligands in receptor complexes

  1997cited by this paper
• Characterization of the role of the stimulatory magnesium of Escherichia coli porphobilinogen synthase.

  1995cited by this paper
• Dissociation of enzyme oligomers: a mechanism for allosteric regulation.

  1994cited by this paper
• Aminolevulinic acid dehydratase in pea (Pisum sativum L.). Identification of an unusual metal-binding domain in the plant enzyme.

  1991cited by this paper
• Regulatory mechanisms in photosynthetic carbon metabolism.

  1976influential reference
• Comparison of experimental binding data and theoretical models in proteins containing subunits.

  1966cited by this paper
• ON THE NATURE OF ALLOSTERIC TRANSITIONS: A PLAUSIBLE MODEL.

  1965cited by this paper
• Allosteric proteins and cellular control systems.

  1963influential reference

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  2022cites this paper
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  2022cites this paper
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  2021cites this paper
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  2020cites this paper
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  2020cites this paper
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  2019cites this paper
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  2019cites this paper
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  2019cites this paper
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  2019cites this paper
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  2018cites this paper
• Learner characteristics, behaviour, technology use and adoption of mobile learning among community health care trainees, Amref Health Africa, Kenya.

  2017cites this paper
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  2015cites this paper
• Interactions of HIV-1 proteins as targets for developing anti-HIV-1 peptides.

  2015cites this paper
• wALADin Benzimidazoles Differentially Modulate the Function of Porphobilinogen Synthase Orthologs

  2014cites this paper
• Allosteric modulation of protein oligomerization: an emerging approach to drug design

  2014influential citation
• Discovery of highly potent TNFα inhibitors using virtual screen.

  2014cites this paper
• Concentration-dependent oligomerization of cross-linked complexes between ferredoxin and ferredoxin-NADP+ reductase.

  2013cites this paper
• Environmental contaminants perturb fragile protein assemblies and inhibit normal protein function.

  2013cites this paper
• A selective inhibitor of heme biosynthesis in endosymbiotic bacteria elicits antifilarial activity in vitro.

  2013influential citation
• Impact of quaternary structure dynamics on allosteric drug discovery.

  2013cites this paper
• Structural systems pharmacology: the role of 3D structures in next-generation drug development.

  2013cites this paper
• A new model for allosteric regulation of phenylalanine hydroxylase: implications for disease and therapeutics.

  2013cites this paper
• Pharmacogenomics and Personalized Medicine for Infectious Diseases

  2013cites this paper
• Protein–Protein Interactions in the Solid State: The Troubles of Crystallizing Protein–Protein Complexes

  2013cites this paper
• A generalized model and high throughput data analysis system for functional modulation of receptor-agonist systems suitable for use in drug discovery.

  2013cites this paper
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  2013cites this paper
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  2012cites this paper
• 3.8 Protein and Nucleic Acid Folding: Domain Swapping in Proteins

  2012cites this paper
• The morpheein model of allostery: evaluating proteins as potential morpheeins.

  2012cites this paper
• Structural Basis for Morpheein-type Allosteric Regulation of Escherichia coli Glucosamine-6-phosphate Synthase

  2012cites this paper
• Allostery and the dynamic oligomerization of porphobilinogen synthase.

  2012cites this paper
• Dynamic dissociating homo-oligomers and the control of protein function.

  2012cites this paper
• Fine-tuning multiprotein complexes using small molecules.

  2012cites this paper
• Biophysical and computational fragment-based approaches to targeting protein–protein interactions: applications in structure-guided drug discovery

  2012cites this paper
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  2011cites this paper
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  2010cites this paper
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  2010cites this paper
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  2010cites this paper
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  2010cites this paper
• Literature Search and Review

  2010cites this paper
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  2009cites this paper
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  2009cites this paper
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  2009cites this paper
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  2009cites this paper
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  2009cites this paper
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  2009cites this paper
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