Human Platelet 12-Lipoxygenase, New Findings about Its Activity, Membrane Binding and Low-resolution Structure

التفاصيل البيبلوغرافية
العنوان: Human Platelet 12-Lipoxygenase, New Findings about Its Activity, Membrane Binding and Low-resolution Structure
المؤلفون: Hartmut Kühn, John David Dignam, Ansari M. Aleem, Jerzy Jankun, Dmitri I. Svergun, Matthias Walther, Ewa Skrzypczak-Jankun
المصدر: Journal of Molecular Biology. 376:193-209
بيانات النشر: Elsevier BV, 2008.
سنة النشر: 2008
مصطلحات موضوعية: Blood Platelets, Models, Molecular, PLAT domain, Stereochemistry, Dimer, Arachidonate 12-Lipoxygenase, Cofactor, Substrate Specificity, chemistry.chemical_compound, Stereospecificity, Protein structure, Structural Biology, Humans, Protein Structure, Quaternary, Molecular Biology, Sequence Deletion, chemistry.chemical_classification, Arachidonic Acid, biology, Membrane Proteins, Monomer, Enzyme, chemistry, biology.protein, Dimerization, Protein Binding, Cysteine
الوصف: Human platelet 12-lipoxygenase (hp-12LOX, 662 residues+iron nonheme cofactor) and its major metabolite 12S-hydroxyeicosatetraenoic acid have been implicated in cardiovascular and renal diseases, many types of cancer and inflammatory responses. However, drug development is slow due to a lack of structural information. The major hurdle in obtaining a high-resolution X-ray structure is growing crystals, a process that requires the preparation of highly homogenous, reproducible and stable protein samples. To understand the properties of hp-12LOX, we have expressed and studied the behavior, function and low-resolution structure of the hp-12LOX His-tagged recombinant enzyme and its mutants in solution. We have found that it is a dimer easily converted into bigger aggregates, which are soluble/covalent-noncovalent/reversible. The heavier oligomers show a higher activity at pH 8, in contrast to dimers with lower activity showing two maxima at pH 7 and pH 8, indicating the existence of two different conformers. In the seven-point C-->S mutant, aggregation is diminished, activity has one broad peak at pH 8 and there is no change in specificity. Truncation of the N(t)-beta-barrel domain (PLAT, residues 1-116) reduces activity to approximately 20% of that shown by the whole enzyme, does not affect regio- or stereospecificity and lowers membrane binding by a factor of approximately 2. "NoPLAT" mutants show strong aggregation into oligomers containing six or more catalytic domains regardless of the status of the seven cysteine residues tested. Time-of-flight mass spectrometry suggests two arachidonic acid molecules bound to one molecule of enzyme. Small angle X-ray scattering studies (16 A resolution, chi approximately 1) suggest that two hp-12LOX monomers are joined by the catalytic domains, with the PLAT domains floating on the flexible linkers away from the main body of the dimer.
تدمد: 0022-2836
DOI: 10.1016/j.jmb.2007.11.086
URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5d47d0a662a95bb2c2cab8045da7114c
https://doi.org/10.1016/j.jmb.2007.11.086
Rights: CLOSED
رقم الانضمام: edsair.doi.dedup.....5d47d0a662a95bb2c2cab8045da7114c
قاعدة البيانات: OpenAIRE
الوصف
تدمد:00222836
DOI:10.1016/j.jmb.2007.11.086