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Id: biblio-1023795
Autor: Santos, João Henrique Picado Madalena.
Título: PEGylation strategy to the development of analytical and therapeutic proteins / Potencial da PEGuilação para o desenvolvimento de proteínas para fins terapêuticos e analíticos.
Fonte: São Paulo; s.n; 2019. 299 p. tab, graf.
Idioma: en.
Tese: Apresentada a Universidade de São Paulo. Faculdade de Ciências Farmacêuticas para obtenção do grau de Doutor.
Resumo: Protein PEGylation is the covalent bonding of polyethylene glycol (PEG) polymers to amino acid residues of the protein and it is one of the most promising techniques for improving the therapeutic effect of biopharmaceuticals and long-term stability of protein-based biosensors. This chemical modification brings advantages to biopharmaceuticals, such as an increased half-life, enhanced stability, and reduced immunogenicity. Moreover, in the analytical field, PEGylation improves the multiple properties of protein-based biosensors including biocompatibility, thermal and long-term stability, and solubility in organic solvents. However, the use of PEGylated conjugates in the analytical and therapeutic fields has not been widely explored. The limited industrial application of PEGylated bioconjugates can be attributed to the fact that the reaction and separation steps are currently a challenge. The correct selection of the PEGylation reaction design and the purification process are important challenges in the field of bioconjugation. In this sense, the design and optimization of site-specific PEGylation reactions and application of aqueous biphasic systems (ABS) as purification platforms for PEGylated conjugates are the two main objectives of this thesis. Regarding the purification step, the efficient fractionation (i) of the PEGylated conjugates from the native protein and (ii) of the PEGylated conjugates based on their degree of PEGylation was studied. Centrifugal partition chromatography (CPC) was applied as a continuous regime platform based on ABS technology to efficiently purify the PEGylated proteins. The two proteins under study are L-asparaginase, an important biopharmaceutical applied in the treatment of acute lymphoblastic leukemia and cytochrome c, a promising biosensor. The current work developed in this thesis demonstrates the great potential of ABS in the fractionation of PEGylated proteins, under batch and continuous regime. In addition, in situ recovery of the PEGylated products through one-pot bioconjugation and ABS purification was successfully demonstrated for both enzymes studied. Although further research on scale-up is still required, the results presented show the relevance of ABS platforms for the development of separation processes of PEGylated proteins

A PEGuilação de proteínas é a ligação covalente de polímeros de polietilenoglicol (PEG) a resíduos de aminoácidos da proteína e é uma das técnicas mais promissoras para melhorar o efeito terapêutico dos biofármacos e a estabilidade a longo prazo de biossensores proteícos. Esta modificação química traz vantagens aos produtos biofarmacêuticos, como um aumento da meia-vida, maior estabilidade e imunogenicidade reduzida. Além disso, no campo analítico, a PEGuilação melhora as múltiplas propriedades dos biossensores baseados em proteínas, incluindo biocompatibilidade, estabilidade térmica e a longo prazo, e solubilidade em solventes orgânicos. No entanto, o uso de conjugados PEGuilados em campos analíticos e terapêuticos não tem sido amplamente explorado. A aplicação industrial limitada dos bioconjugados PEGuilados pode ser atribuída ao facto de as etapas de reacção e separação serem atualmente um desafio. A seleção correcta do design da reacção de PEGuilação e do processo de purificação são importantes desafios no campo da bioconjugação. Neste sentido, a concepção e otimização de reações de PEGuilação sítio-específicas e aplicação de sistemas aquosos bifásicos (ABS) como plataformas de purificação de conjugados PEGuilados são os dois principais objetivos desta tese. No que concerne à etapa de purificação foi estudado o eficiente fracionamento (i) dos conjugados PEGuilados, da proteína nativa e (ii) dos conjugados PEGuilados baseados no seu grau de PEGuilação. A cromatografia por partição centrífuga (CPC) foi aplicada como uma plataforma de regime contínuo baseada na tecnologia de ABS para purificar eficientemente as proteínas PEGuiladas. As duas proteínas em estudo são a L-asparaginase, importante biofármaco aplicado no tratamento da leucemia linfoblástica aguda e o citocromo c, um potencial biossensor. A partir dos trabalhos desenvolvidos, é possível confirmar o grande potencial dos ABS no fracionamento de proteínas PEGuiladas, em regime contínuo e descontínuo. Além disso, a recuperação in situ dos produtos PEGuilados através da integração em uma única etapa de bioconjugação e purificação por ABS foi comprovada com sucesso para ambas as enzimas estudadas. Embora ainda sejam necessários estudos adicionais sobre a viabilidade destes sistemas em larga escala, os resultados aqui apresentados demonstram a relevância dos ABS para o desenvolvimento de processos de separação de proteínas PEGuiladas
Responsável: BR40.1 - DBD - Divisão de Biblioteca e Documentacão do Conjunto das Químicas
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Id: biblio-967604
Autor: Wiethan, Maria Medianeira Saccol; Bortolin, Gabriel Streck; Pinto, Renata Soares; Sari, Bruno Giacomini; Silva, Antonio Carlos Ferreira da.
Título: Development and multiplication of Eisinea andrei in the manure of cattle subjected to high Trichoderma doses / Desenvolvimento e multiplicação de Eisenia andrei em esterco bovino em altas doses de Trichoderma
Fonte: Biosci. j. (Online);34(6 Supplement 1):1-10, nov./dec. 2018.
Idioma: en.
Resumo: The efficacy of the vermicomposting and products based on the antagonistic fungus and plant growth promoter trichoderma (Trichoderma spp) is well known and studied in organic agriculture. However, for a better methodological efficiency are necessary studies to evaluate the effect of high doses of these bioproducts in the biology and development of earthworms. Thus, the present work aims to test the use of high commercial biocontrol product (ICB Nutrisolo Trichoderma) doses by evaluating the multiplication and development of Eisenia andrei. Changes in the chemical features of the substrate produced by the vermicomposting process using in natura and sterilized organic cattle manure were also assessed. Each experimental unit consisted of 6 kg of substrate (in multipurpose polypropylene box ­ 20 x 40 x 50 cm) containing 48 clitelate adult Eisenia andrei earthworms. ICB Nutrisolo Trichoderma was used as biological agent along with eight strains of the following species: T. koningiopsis, T. asperellum and T. harzianum. The following treatments were applied at doses of 1011 CFU kg-1 of ICB Nutrisolo Trichoderma in the presence of earthworms: T1 (0.5); T2 (1.0); T3 (2.0); T4 (4.0); T5 (8.0) and T6 (0.0). The T7 treatment was herein used in order to evaluate the chemical features of the vermicompost. It was a completely randomized design with four replications per treatment. The temperature was kept at 28°C and humidity ranged between 60 and 70%. After 60 days, the number of young and adult earthworms, and cocoons was counted; then, their dry biomass was assessed. The results found in the lethality test showed decrease in the number of earthworms treated with 4.0x1011 CFU kg-1 of ICB. The biological product doses up to 1.0x1011 CFU kg-1 did not alter the number of adult earthworms and cocoons, or the multiplication index of E. andrei in cattle waste vermicomposts. There was no influence of the tested doses on earthworms' individual development. However, doses above 2.0x1011 CFU kg-1 decreased their total biomass. The C/N ratio for all treatments indicates maturity within acceptable results for organic compounds.

A eficácia da vermicompostagem e de bioprodutos à base do fungo antagonista e promotor de crescimento vegetal trichoderma (Trichoderma spp) é bem conhecida e estudada na agricultura orgânica. Entretanto, para uma melhor eficiência metodológica, são necessários estudos que possam avaliar a interferência de altas doses desses bioprodutos na biologia e desenvolvimento das minhocas. Baseado nesse contexto, o objetivo deste trabalho foi testar altas doses do produto comercial biológico ICB Nutrisolo Trichoderma (ICB), avaliando-se a multiplicação e desenvolvimento de Eisenia andrei, bem como alterações nas características químicas do substrato produzido no processo de vermicompostagem, a partir do resíduo orgânico esterco bovino. O esterco bovino in natura foi autoclavado a 121°C, por duas vezes, em um intervalo de 24 h. A unidade experimental constituiu-se de 6 kg de substrato condicionados em caixa multiuso de polipropileno, com dimensões 20 x 40 x 50 cm, contendo 48 minhocas adultas e cliteladas da espécie E. andrei. Como agente biológico, utilizou-se o produto comercial ICB na forma de fluído, composto por oito cepas das espécies T. koningiopsis, T. asperellum e T. harzianum, com as seguintes doses nos tratamentos a seguir: T1 (0.5); T2 (1.0); T3 (2.0); T4 (4.0); T5 (8.0); e T6 (0.0), sendo todas as concentrações em 1011 UFC kg-1 do produto em vermicomposto, e, para a avaliação das características químicas do vermicomposto em altas doses do produto ICB, foi utilizado também o T7 (somente substrato). O delineamento foi inteiramente casualizado com quatro repetições por tratamento. A temperatura foi mantida a 28ºC e a umidade entre 60 e 70%. Após 60 dias do início da instalação, fez-se a contagem do número de minhocas adultas, jovens e casulos; posteriormente, avaliou-se o seu peso seco total. Os resultados observados no teste de letalidade mostram que, somente a partir de 4.0x1011 UFC kg-1 de ICB, há decréscimo do número de minhocas. Doses altas até 1.0x1011 UFC kg-1 do produto não alteram o número de minhocas adultas e de casulos de E. andrei em vermicompostagem com esterco bovino, entretanto, o índice de multiplicação foi inferior em todos os tratamentos com o produto. Doses acima de 2.0x1011 UFC kg-1 diminuíram o peso seco total. A relação C/N em todos os tratamentos indica maturidade dentro de resultados aceitáveis para compostos orgânicos.
Responsável: BR396.1 - Biblioteca Central


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Id: biblio-1022985
Autor: Schmid, T J; Khalid, S A; Romanha, A J; Alves, T M; Bivatti, M W; Brun, R; Da Costa, F B; de Castro, S L; Ferreira, V F; de Lacerda, M V; Lago, J H; Leon, L L; Lopes, N P; das Neves Amorim, R C; Niehues, M; Ogungbe, IV; Pohlit, A M; Scotti, M T; Setzer, W N; Soeiro, M N C de; Steindel, M; Tempone, A G.
Título: The potential of secondary metabolites from plants as drugs or leads against protozoan neglected diseases - part I
Fonte: Curr Med Chem;19:2128-2175, 2012.
Idioma: en.
Resumo: Infections with protozoan parasites are a major cause of disease and mortality in many tropical countries of the world. Diseases caused by species of the genera Trypanosoma (Human African Trypanosomiasis and Chagas Disease) and Leishmania (various forms of Leishmaniasis) are among the seventeen "Neglected Tropical Diseases" (NTDs) defined as such by WHO due to the neglect of financial investment into research and development of new drugs by a large part of pharmaceutical industry and neglect of public awareness in high income countries. Another major tropical protozoan disease is malaria (caused by various Plasmodium species), which -although not mentioned currently by the WHO as a neglected disease- still represents a major problem, especially to people living under poor circumstances in tropical countries. Malaria causes by far the highest number of deaths of all protozoan infections and is often (as in this review) included in the NTDs. The mentioned diseases threaten many millions of lives world-wide and they are mostly associated with poor socioeconomic and hygienic environment. Existing therapies suffer from various shortcomings, namely, a high degree of toxicity and unwanted effects, lack of availability and/or problematic application under the life conditions of affected populations. Development of new, safe and affordable drugs is therefore an urgent need. Nature has provided an innumerable number of drugs for the treatment of many serious diseases. Among the natural sources for new bioactive chemicals, plants are still predominant. Their secondary metabolism yields an immeasurable wealth of chemical structures which has been and will continue to be a source of new drugs, directly in their native form and after optimization by synthetic medicinal chemistry. The current review, published in two parts, attempts to give an overview on the potential of such plant-derived natural products as antiprotozoal leads and/or drugs in the fight against NTDs.
Responsável: BR91.2 - Centro de Documentação


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Id: lil-772706
Autor: Pérez O, Luis E; Aguilar, María B.
Título: Nivel de información sobre farmacovigilancia en los estudiantes de las carreras de medicina y de farmacia de la Universidad Central de Venezuela en el año 2011 / Level of Information on pharmacovigilance in Students from the medicine and pharmacy schools at Central University of Venezuela in the year 2011
Fonte: Rev. Inst. Nac. Hig;45(1):80-91, jun. 2014. graf, tab.
Idioma: es.
Resumo: Se realizó un estudio de tipo descriptivo transversal cuyo objetivo fue evaluar el nivel de información sobre Farmacovigilancia de los alumnos cursantes de 4º y 5º año de las carreras de Medicina y Farmacia de la Universidad Central de Venezuela durante el año 2011. Se utilizó como instrumento una encuesta dividida en 3 secciones: la primera de 3 preguntas de opinión, la segunda de 8 preguntas de conocimiento general y la tercera de 2 preguntas de interés particular. La encuesta previamente validada, se aplicó a 73 estudiantes de la Facultad de Farmacia de la UCV, comprendidos entre 38 estudiantes de 4to año y 35 de 5to año, y a 212 estudiantes de la Facultad de Medicina de la UCV, comprendidos entre 101 estudiantes de 4to año y 111 de 5to año. El análisis fue descriptivo. Los resultados obtenidos mostraron que el mayor porcentaje que obtuvo un nivel de información alto (16 - 20 puntos) estuvo representado por los estudiantes de 4to año de la Facultad de Medicina con un 43,56%, el mayor porcentaje que obtuvo un nivel de información medio (11-15 puntos) estuvo representado por los estudiantes de 4º año de Farmacia con un 63,15% y el mayor porcentaje que obtuvo un nivel de información bajo (6-10 puntos) estuvo representado por los estudiantes de 5º año de Medicina con un 36,04%. Dado los resultados obtenidos se recomendó la elaboración de una propuesta de Temario de Farmacovigilancia, para incluirla como asignatura dentro de los programas de estudio del último año de las carreras de Medicina y Farmacia, con el fin de suplir los conocimientos necesarios para la práctica profesional futura.

A cross-sectional descriptive research was performed to assess the degree of information on Pharmacovigilance in the 4th and 5th year students from Pharmacy and Medicine Schools of Central University of Venezuela during the June-July 2011 period.The utilized instrument was a questionnaire divided in three sections: the first section containing 3 questions of opinion, the second one had eight general knowledge questions and the third section with two questions of particular interest. We applied a previously validated Test to 73 students from Pharmacy School of UCV, (including 38 and 35 students studying at 4th and 5th year respectively), and to 212 students from the Medicine School of UCV, (101 studiyng at the 4th year and 111 studying at the 5th year). The analysis was descriptive. The results showed that the 4th year students of the Medicine School, adquired the highest percentage of information level (16 - 20 pts), equivalent to a 43.56%. The 4th year students of Pharmacy School, with a 63,15%, the highest in percentage, obtained an average information level (11 -15 pts) and the highest percentage who earned a low level of information (6 - 10 pts) was represented by students of 5th year with 36,04 % , which resulted in recommendations for the development of a proposed agenda for pharmacovigilance, to be included as a subject in the curriculum of the last year of racing surveyed, in order to supply the knowledge necessary for future professional practice.
Responsável: VE9.1 - Biblioteca


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Id: lil-623935
Autor: Gottlieb, Otto R.
Título: The rational search for natural neolignans
Fonte: Mem. Inst. Oswaldo Cruz;86(supl.2):25-29, 1991. ilus.
Idioma: en.
Conferência: Apresentado em: Brazilian-Sino Symposium on Chemistry and Pharmacology of Natural Products, Rio de Janeiro, Dec. 10-14, 1989.
Resumo: A rational method of search for natural neolignans of desired structures is outlined. This involves consultation of a collection of chemical profiles of plant families. The profiles are assembled considering the biosynthetic class (in the present case lignoids), subclass (neolignans), structural types (neolignan skeleta) and relative frequency of substitutional derivatives belonging to each type (known compounds). The method is of course applicable to ani class of natural products. Its use in the case of neolignans is here selected as an exemple in view of the recently discovered antagonism towards PAF of kadsurenone, a representative of this subclass of phytochemicals. Application of the chemical profiles to phylogenetic studies is illustrated.
Responsável: BR1.1 - BIREME


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Id: lil-623930
Autor: Kaplan, Maria Auxiliadora C.
Título: Potential sources of biodynamically active natural products in Brazil
Fonte: Mem. Inst. Oswaldo Cruz;86(supl.2):5-8, 1991. ilus.
Idioma: en.
Conferência: Apresentado em: Brazilian-Sino Symposium on Chemistry and Pharmacology of Natural Products, Rio de Janeiro, Dec. 10-14, 1989.
Resumo: In contrast to China where vegatation is predominantly herbaceous, vegetation in Brazil is commonly arboreous. This fact may explain why Chinese drugs are usually acetate derived, while actual and potential natural therapeutic agents from Brazil are mostly shikimate derived. Only relatively few compounds isolated from Brazilian plants have been submitted to adequate pharmacological testing .
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Id: biblio-1007560
Autor: Tofik, Veridiana de Freitas.
Título: Complexos de cobre com análogos de produtos naturais encontrados em organismos marinhos com atividade antitumoral / Copper complexes with analogues of natural products found in marine organisms with antitumor activity.
Fonte: São Paulo; s.n; 2019. 75 p. graf, tab, ilus.
Idioma: pt.
Tese: Apresentada a Universidade de São Paulo. Instituto de Química para obtenção do grau de Mestre.
Resumo: Neste trabalho foram sintetizados complexos de cobre(II) com derivados imínicos da isatina, incluindo isatinas bromadas semelhantes a compostos encontrados em gastrópodes, a fim de compará-los com o composto já produzido e investigado [Cu(isaepy)], complexo de cobre(II) com base de Schiff feita a partir da isatina e 2-aminoetilpiridina. A isatina é um oxindol produzido em algumas plantas, também encontrado no tecido de mamíferos, com propriedades antitumorais naturais. Isatinas bromadas foram previamente constatadas como mais citotóxicas frente a células tumorais do que a isatina sem substituições. O objetivo principal foi verificar se a presença de bromo nos compostos análogos ao [Cu(isaepy)] levaria a um aumento da atividade antitumoral, assim como maior interação com DNA, alvo usual de metalofármacos. Depois de sintetizados, os compostos foram caracterizados por análise elementar (CHN), espectroscopia no infravermelho, espectroscopia UV/Vis e EPR. Foram feitos testes de citotoxicidade pelo método MTT com células de sarcoma uterino (MES-SA e MES-AS/Dx5, esta última resistente a doxorrubicina), adenocarcinoma cervical (HeLa) e células não cancerosas de fibroblasto humano P4. Adicionalmente, foram feitos testes de interação com DNA por UV/Vis e dicroísmo circular, além de testes de clivagem de DNA plasmidial. De modo geral, foi demonstrado que a simetria tetragonal em torno do cobre, determinada pelo EPR, é importante para a citotoxicidade dos complexos, que dessa forma podem se intercalar ao DNA e impedir sua replicação, por acabar distorcendo a hélice, e pela habilidade de realizarem clivagem oxidativa das fitas. [Cu(isaepy)] e seus análogos bromados demonstraram uma atividade citotóxica muito parecida, assim como grau de interação e clivagem com DNA. Conclui-se que, embora a presença de bromo nos análogos de [Cu(isaepy)] não levem a um aumento de atividade antitumoral, como observado em ligantes correlatos livres, nossos estudos apontam para diferentes fontes naturais (animal ou vegetal) para obtenção de precursores de novos compostos antitumorais

In the present work, copper(II) complexes were synthesized with isatin derived imine ligands, including brominated oxindoles similar to compounds found in gastropods, in order to compare their reactivity with that of [Cu(isaepy)], a Schiff base-copper(II) complex already investigated, obtained with the precursors isatin and 2-aminoethylpyridine. Isatin is a natural oxindole extracted from plants, and also found in mammal tissue, with antitumor properties. Brominated isatins were previously described as much more cytotoxic, towards tumor cells, than unsubstituted isatin. The aim of this work was to verify if the presence of brome in analogue [Cu(isaepy)] compounds would increase their antitumor activity, along with higher DNA interaction, an usual target for metallodrugs. The copper(II) complexes were synthesized and then characterized through elemental analyses (CHN), infrared, UV/Vis and EPR spectroscopies. Cytotoxicity tests were carried out using MTT assay with cells lines MES-SA e MES-SA/Dx5 (uterine sarcome, sensitive and resistent to doxorubicin), HeLa (cervical adenocarcinoma) and non-tumor cells, human fibroblast P4. Additionally, DNA interaction experiments were carried out through UV/Vis spectroscopy and circular dichroism, and at last, DNA cleavage experiments with the studied complexes. In general, it was shown that a tetragonal symmetry around copper, shown by EPR, is very important to the complexes toxicity, since in that way they are able to intercalate DNA, and prevent its replication, as a consequence of double helix distortion, and eventual oxidative cleavage. [Cu(isaepy)] and its brominated analogues demonstrated a very similar cytotoxicity towards cancer cells, as well as quite same level of DNA interaction and cleavage. Although the presence of brome did not increase significantly their antitumor activity, as verified with the free isatin derivatives, our studies pointed to different natural sources to obtain precursors for such new antitumor compounds
Responsável: BR40.1 - DBD - Divisão de Biblioteca e Documentacão do Conjunto das Químicas
BR40.1; T546.6522, T644c. 30100026265-Q


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Id: biblio-1001582
Autor: Wiens, Astrid; Borba, Helena Hiemisch Lobo; Leonart, Letícia Paula; Tonin, Fernanda Stumpf; Steimbach, Laiza Maria; Araújo, Ariane Gonçalves Silva de; Piazza, Thais; Ferreira, Vinicius Lins; Pontarolo, Roberto.
Título: Treatment interruption of biological drugs and tofacitinib in rheumatoid arthritis: A systematic review of case reports
Fonte: Braz. J. Pharm. Sci. (Online);54(4):e17437, 2018. tab, graf.
Idioma: en.
Projeto: Fellow of the Brazilian National Council of Scientific Research-CNPq.
Resumo: The aim of this study was to evaluate interruption of treatment with biological drugs and tofacitinib due to adverse events in patients with rheumatoid arthritis. A systematic review was performed in the electronic databases MEDLINE, Cochrane, Scopus, CRD, IPA, Lilacs and Scielo. Case reports addressing interruption of treatment due to any adverse event related to abatacept (ABA), adalimumab (ADA), anakinra (ANA), certolizumab pegol (CER), etanercept (ETA), golimumab (GOL), infliximab (IFX), rituximab (RTX), secukinumab (SEC), tocilizumab (TCZ), tofacitinib (TOF) or ustekinumab (UST) in rheumatoid arthritis patients were evaluated. Baseline data, patient profile, previous and current treatments, cause of discontinuation and information on reintroduction of treatment were extracted from the case reports. One hundred and fifty-four studies (154 patients) reported 162 discontinuations of rheumatoid arthritis treatment due to adverse events (ETA = 57; IFX = 46; ADA = 32; TCZ = 13; RTX = 5; ANA = 3; GOL = 2; ABA = 2; TOF = 1; CER = 1; SEC = 0 and UST = 0). The mean age of patients was 56 (± 12.1) years and 82% were female. Seventy-four adverse events were confirmed (related to used drug), and 138 were observed in patients using anti-TNF. The most common adverse events were infections (21%), skin disease (15%), autoimmune disease (13%) and hematological disorders (9%). Case reports are important in the detection of rare adverse events and should be considered in the choice of appropriate therapy for patients.
Responsável: BR40.1 - DBD - Divisão de Biblioteca e Documentacão do Conjunto das Químicas


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Id: biblio-974430
Autor: Silva, Daniel Gedder; Emery, Flavio da Silva.
Título: Strategies towards expansion of chemical space of natural product-based compounds to enable drug discovery
Fonte: Braz. J. Pharm. Sci. (Online);54(spe):e01004, 2018. tab, graf.
Idioma: en.
Resumo: Natural products (NPs) are an excellent source of biologically active molecules that provide many biologically biased features that enable innovative designing of synthetic compounds. NPs are characterized by high content of sp3-hybridized carbon atoms; oxygen; spiro, bridged, and linked systems; and stereogenic centers, with high structural diversity. To date, several approaches have been implemented for mapping and navigating into the chemical space of NPs to explore the different aspects of chemical space. The approaches providing novel opportunities to synthesize NP-inspired compound libraries involve NP-based fragments and ring distortion strategies. These methodologies allow access to areas of chemical space that are less explored, and consequently help to overcome the limitations in the use of NPs in drug discovery, such as lack of accessibility and synthetic intractability. In this review, we describe how NPs have recently been used as a platform for the development of diverse compounds with high structural and stereochemical complexity. In addition, we show developed strategies aiming to reengineer NPs toward the expansion of NP-based chemical space by fragment-based approaches and chemical degradation to yield novel compounds to enable drug discovery
Responsável: BR1.1 - BIREME


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Id: biblio-974429
Autor: Santos, João Henrique Picado Madalena; Torres-Obreque, Karin Mariana; Meneguetti, Giovanna Pastore; Amaro, Beatriz Panichi; Rangel-Yagui, Carlota Oliveira.
Título: Protein PEGylation for the design of biobetters: from reaction to purification processes
Fonte: Braz. J. Pharm. Sci. (Online);54(spe):e01009, 2018. tab, graf.
Idioma: en.
Projeto: National Council for Scientific and Technological Development; . Portuguese Foundation for Science and Technology; . CICECO-Aveiro Institute of Materials.
Resumo: The covalent attachment of polyethylene glycol (PEG) to therapeutical proteins is an important route to develop biobetters for biomedical, biotech and pharmaceutical industries. PEG conjugation can shield antigenic epitopes of the protein, reduce degradation by proteolytic enzymes, enhance long-term stability and maintain or even improve pharmacokinetic and pharmacodynamics characteristics of the protein drug. Nonetheless, correct information in terms of the PEGylation process from reaction to downstream processing is of paramount importance for the industrial application and processing scale-up. In this review we present and discuss the main steps in protein PEGylation, namely: PEGylation reaction, separation of the products and final characterization of structure and activity of the resulting species. These steps are not trivial tasks, reason why bioprocessing operations based on PEGylated proteins relies on the use of analytical tools according to the specific pharmaceutical conjugate that is being developed. Therefore, the appropriate selection of the technical and analytical methods may ensure success in implementing a feasible industrial process
Responsável: BR1.1 - BIREME



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