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A 2D-QSPR approach to predict blood-brain barrier penetration of drugs acting on the central nervous system BJPS
Sá,Matheus Malta de; Pasqualoto,Kerly Fernanda Mesquita; Rangel-Yagui,Carlota de Oliveira.
Drugs acting on the central nervous system (CNS) have to cross the blood-brain barrier (BBB) in order to perform their pharmacological actions. Passive BBB diffusion can be partially expressed by the blood/brain partition coefficient (logBB). As the experimental evaluation of logBB is time and cost consuming, theoretical methods such as quantitative structure-property relationships (QSPR) can be useful to predict logBB values. In this study, a 2D-QSPR approach was applied to a set of 28 drugs acting on the CNS, using the logBB property as biological data. The best QSPR model [n = 21, r = 0.94 (r² = 0.88), s = 0.28, and Q² = 0.82] presented three molecular descriptors: calculated n-octanol/water partition coefficient (ClogP), polar surface area (PSA), and...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Two-dimensional quantitative structure-property relationships (2D-QSPR); Calculated n-octanol/water partition coefficient (ClogP); Blood-brain barrier; Benzodiazepines.
Ano: 2010 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502010000400016
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Biopharmaceuticals from microorganisms: from production to purification BJM
Jozala,Angela Faustino; Geraldes,Danilo Costa; Tundisi,Louise Lacalendola; Feitosa,Valker de Araújo; Breyer,Carlos Alexandre; Cardoso,Samuel Leite; Mazzola,Priscila Gava; Oliveira-Nascimento,Laura de; Rangel-Yagui,Carlota de Oliveira; Magalhães,Pérola de Oliveira; Oliveira,Marcos Antonio de; Pessoa Jr,Adalberto.
ABSTRACT The use of biopharmaceuticals dates from the 19th century and within 5-10 years, up to 50% of all drugs in development will be biopharmaceuticals. In the 1980s, the biopharmaceutical industry experienced a significant growth in the production and approval of recombinant proteins such as interferons (IFN α, β, and γ) and growth hormones. The production of biopharmaceuticals, known as bioprocess, involves a wide range of techniques. In this review, we discuss the technology involved in the bioprocess and describe the available strategies and main advances in microbial fermentation and purification process to obtain biopharmaceuticals.
Tipo: Info:eu-repo/semantics/article Palavras-chave: Biopharmaceuticals; Fermentation process; Biotechnology; Upstream process; Downstream process.
Ano: 2016 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1517-83822016000500051
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Polymeric micelles and molecular modeling applied to the development of radiopharmaceuticals BJPS
Grallert,Sibila Roberta Marques; Rangel-Yagui,Carlota de Oliveira; Pasqualoto,Kerly Fernanda Mesquita; Tavares,Leoberto Costa.
Micelles composed of amphiphilic copolymers linked to a radioactive element are used in nuclear medicine predominantly as a diagnostic application. A relevant advantage of polymeric micelles in aqueous solution is their resulting particle size, which can vary from 10 to 100 nm in diameter. In this review, polymeric micelles labeled with radioisotopes including technetium (99mTc) and indium (111In), and their clinical applications for several diagnostic techniques, such as single photon emission computed tomography (SPECT), gamma-scintigraphy, and nuclear magnetic resonance (NMR), were discussed. Also, micelle use primarily for the diagnosis of lymphatic ducts and sentinel lymph nodes received special attention. Notably, the employment of these diagnostic...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Radiopharmaceuticals/development; Polymeric micelles/diagnostic application; Radioisotopes; Imaging diagnostic agents; Diagnostic techniques.
Ano: 2012 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502012000100002
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