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Design and therapeutic application of matrix metalloproteinase inhibitors.

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This article is published in Chemical Reviews.The article was published on 1999-09-08. It has received 944 citations till now. The article focuses on the topics: Matrix metalloproteinase inhibitor.

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Glide: a new approach for rapid, accurate docking and scoring. 1. Method and assessment of docking accuracy.

TL;DR: Glide approximates a complete systematic search of the conformational, orientational, and positional space of the docked ligand to find the best docked pose using a model energy function that combines empirical and force-field-based terms.
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Glide: a new approach for rapid, accurate docking and scoring. 2. Enrichment factors in database screening.

TL;DR: Comparisons to results for the thymidine kinase and estrogen receptors published by Rognan and co-workers show that Glide 2.5 performs better than GOLD 1.1, FlexX 1.8, or DOCK 4.01.
Journal ArticleDOI

Matrix Metalloproteinase Inhibitors and Cancer—Trials and Tribulations

TL;DR: The studies that brought MPIs into clinical testing are reviewed and the design and outcome of the trials are discussed in light of new information about the cellular source, substrates, and mode of action of MMPs at different stages of tumor progression.
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Iron-Catalyzed Reactions in Organic Synthesis

TL;DR: A new iron(III) halide-promoted aza-Prins cyclization between γ,δ-unsaturated tosylamines and aldehydes provides six-membered azacycles in good to excellent yields.
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Asymmetric multicomponent reactions (amcrs): the new frontier

TL;DR: Asymmetric multicomponent reactions involve the preparation of chiral compounds by the reaction of three or more reagents added simultaneously and has some advantages over classic divergent reaction strategies, such as lower costs, time, and energy, as well as environmentally friendlier aspects.
References
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Journal ArticleDOI

A metalloproteinase disintegrin that releases tumour-necrosis factor-α from cells

TL;DR: The results should facilitate the development of therapeutically useful inhibitors of TNF-α release, and they indicate that an important function of adamalysins may be to shed cell-surface proteins.
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A matrix metalloproteinase expressed on the surface of invasive tumour cells

TL;DR: The cloning of the complemen-tary DNA encoding a new matrix metalloproteinase with a potential transmembrane domain is reported, which may trigger invasion by tumour cells by activating pro-gelatinase A on the tumour cell surface.
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Discovering High-Affinity Ligands for Proteins: SAR by NMR

TL;DR: A nuclear magnetic resonance (NMR)-based method is described in which small organic molecules that bind to proximal subsites of a protein are identified, optimized, and linked together to produce high-affinity ligands and appears particularly useful in target-directed drug research.
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Mechanism Of Cell Surface Activation Of 72-kDa Type IV Collagenase ISOLATION OF THE ACTIVATED FORM OF THE MEMBRANE METALLOPROTEASE

TL;DR: Activation of 72T4Cl on the cell membrane provides a basic mechanism for spatially regulated extracellular proteolysis and presents a new target for prognosis and treatment of metastatic disease.
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Cloning of a disintegrin metalloproteinase that processes precursor tumour-necrosis factor-alpha.

TL;DR: The expression of recombinant TACE results in the production of functional enzyme that correctly processes precursor TNF-α to the mature form, and provides a readily available source of enzyme to help in the search for new anti-inflammatory agents that target the final processing stage of T NF-α production.
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