Rational Design Of Therapeutic Drugs
Mostrando 1-8 de 8 artigos, teses e dissertações.
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1. ESTUDOS ESTRUTURAIS DE PROTEÍNAS: INIBIDOR DE ALFA-AMILASE DE Secale cereale, GTPase YchF E ENOLASE DE Trypanosoma cruzi
As proteínas são as biomoléculas mais abundantes nos seres vivos, estando presentes em todas as partes de uma célula. Elas possuem diferentes funções no organismo; seu estudo estrutural é importante, pois traz maior conhecimento sobre suas funções e possibilita entender como interagem entre elas e com outras moléculas. A estrutura de proteínas pod
IBICT - Instituto Brasileiro de Informação em Ciência e Tecnologia. Publicado em: 13/03/2012
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2. Estudos de modelagem molecular e relação estrutura-atividade da acetilcolinesterase e inibidores em Mal de Alzheimer / Molecular modeling studies and structure-activity relationships of acetylcholinesterase inhibitors in Alzheimers disease.
Alzheimers disease is the leading cause of dementia in the elderly. The progression of symptoms is associated with structural changes in cholinergic synapses in specific brain regions and consequentely to decrease the potential of cholinergic neurotransmission. Thus, the increased capacity of cholinergic neurotransmission is the fundamental mechanism of the
Publicado em: 2011
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3. A New Antitumoral Agent: 9-Hydroxyellipticine. Possibility of a Rational Design of Anticancerous Drugs in the Series of DNA Intercalating Drugs
The designing of DNA intercalating drugs with high DNA affinity in the series of ellipticine has led to a new antitumoral agent, 9-hydroxyellipticine, which has a high DNA affinity, a high activity on L 1210 mice leukemia, and a lack of toxicity at therapeutic dose. The possible correlations among chemical structure, DNA reactivity, and pharmacological activ
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4. Rational discovery of novel nuclear hormone receptor antagonists
Nuclear hormone receptors (NRs) are potential targets for therapeutic approaches to many clinical conditions, including cancer, diabetes, and neurological diseases. The crystal structure of the ligand binding domain of agonist-bound NRs enables the design of compounds with agonist activity. However, with the exception of the human estrogen receptor-α, the l
The National Academy of Sciences.
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5. Systematic discovery of multicomponent therapeutics
Multicomponent therapies, originating through deliberate mixing of drugs in a clinical setting, through happenstance, and through rational design, have a successful history in a number of areas of medicine, including cancer, infectious diseases, and CNS disorders. We have developed a high-throughput screening method for identifying effective combinations
National Academy of Sciences.
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6. Mimicking dominant negative inhibition of prion replication through structure-based drug design
Recent progress determining the structure of the host-encoded prion protein (PrPC) and the role of auxiliary molecules in prion replication permits a more rational approach in the development of therapeutic interventions. Our objective is to identify a new class of lead compounds that mimic the dominant negative PrPC mutants, which inhibit an abnormal isofor
The National Academy of Sciences.
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7. Effects of cellular pharmacology on drug distribution in tissues.
The efficacy of targeted therapeutics such as immunotoxins is directly related to both the extent of distribution achievable and the degree of drug internalization by individual cells in the tissue of interest. The factors that influence the tissue distribution of such drugs include drug transport; receptor/drug binding; and cellular pharmacology, the proces
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8. Structure-activity and cross-resistance evaluations of a series of human immunodeficiency virus type-1-specific compounds related to oxathiin carboxanilide.
A series of compounds related to the nonnucleoside reverse transcriptase (RT) inhibitor (NNRTI) oxathiin carboxanilide (UC84) were evaluated for activity against the human immunodeficiency virus (HIV) to determine structural requirements for anti-HIV activity. Twenty-seven compounds representative of the more than 400 Uniroyal Chemical Company (UC) compounds