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Thrombin active site inhibitors

Bioorganic & Medicinal Chemistry, 1995
Development of small molecule thrombin active site inhibitors has been an area of intense research. A brief review on recent progress and challenges is outlined.
J, Das, S D, Kimball
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Thrombin Active-Site Regions

Seminars in Thrombosis and Hemostasis, 1986
Knowledge is being gained about topographic features of alpha-thrombin and how they may define thrombin specificity and biologic functions. Thrombin is not just an enzyme with moderately restricted proteolytic capabilities, yet with extraordinarily high specificities for certain bonds (such as the A alpha-cleavage site in fibrinogen), but also is a ...
J W, Fenton, D H, Bing
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Superfamily active site templates

Proteins: Structure, Function, and Bioinformatics, 2004
AbstractWe show that three‐dimensional signatures consisting of only a few functionally important residues can be diagnostic of membership in superfamilies of enzymes. Using the enolase superfamily as a model system, we demonstrate that such a signature, or template, can identify superfamily members in structural databases with high sensitivity and ...
Elaine C, Meng   +2 more
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Modulating caspase activity: beyond the active site

Current Opinion in Structural Biology, 2013
Caspases are a family of aspartate-specific cysteine proteases that regulate cellular homeostasis through the mediation of apoptosis and inflammation. Despite keen interest in caspases as therapeutic targets for cancer, inflammatory, and neurodegenerative diseases, no active-site directed small molecule has yet succeeded in navigating human clinical ...
Jeremy, Murray, Adam R, Renslo
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Active-site probes of flavoproteins

Biochemical Society Transactions, 1980
Flavins are very versatile coenzymes, functioning with considerable efficiency in a wide variety of enzymic reactions involving either two-electron or one-electron transfers, with both functions often catalysed by the same enzyme. They are responsible for catalysing the dehydrogenation of many different types of compounds, including dithiols, reduced ...
V, Massey, P, Hemmerich
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Indirect active-site titration of plasminogen activators

Analytical Biochemistry, 1988
A method for the determination of the molar concentration of active tissue plasminogen activator (TPA) and urokinase (UK) has been developed. The method employs the principle of back-titration of a calibrated trypsin standard with a calibrated standard solution of a chloromethyl ketone inhibitor reactive with both trypsin and activator.
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Enzyme Active Sites

1985
Monoclonal antibodies (MAbs) have provided powerful new tools for analysis of enzyme function. MAbs directed at specific subsites of the enzyme active site allow analysis of catalysis at a new level of resolution even for relatively simple, monomeric enzymes.
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Brain and other central nervous system tumor statistics, 2021

Ca-A Cancer Journal for Clinicians, 2021
Kimberly D Miller   +2 more
exaly  

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