A5101711433- Trypanosoma species research and implications
- Research on Leishmaniasis Studies
- Plant biochemistry and biosynthesis
- Esophageal and GI Pathology
- Epilepsy research and treatment
- Signaling Pathways in Disease
- Gastroesophageal reflux and treatments
- Synthesis and biological activity
- Synthesis and Biological Evaluation
- Beetle Biology and Toxicology Studies
- Malaria Research and Control
- Histiocytic Disorders and Treatments
- Tumors and Oncological Cases
- Fungal Plant Pathogen Control
- Pesticide and Herbicide Environmental Studies
- Intestinal Malrotation and Obstruction Disorders
- Peptidase Inhibition and Analysis
- Insect-Plant Interactions and Control
- Nail Diseases and Treatments
- Glycogen Storage Diseases and Myoclonus
- Pneumocystis jirovecii pneumonia detection and treatment
- Biochemical and Molecular Research
- Pharmacological Effects and Toxicity Studies
- Helminth infection and control
- Tuberous Sclerosis Complex Research
Pfizer-University of Granada-Junta de Andalucía Centre for Genomics and Oncological Research
2022
Consejo Superior de Investigaciones Científicas
2011-2014
Instituto de Parasitología y Biomedicina "López - Neyra"
2003-2014
University of Illinois Urbana-Champaign
2009
University of California, San Diego
2009
Instituto Venezolano de Investigaciones Científicas
2003-2008
Cardiff University
2003
Trypanosomatid parasites are the causative agents of many neglected tropical diseases and there is currently considerable interest in targeting endogenous sterol biosynthesis these organisms as a route to development novel anti-infective drugs. Here, we report first x-ray crystallographic structures enzyme squalene synthase (SQS) from trypanosomatid parasite, Trypanosoma cruzi, agent Chagas disease. We obtained five T. cruzi SQS eight human with four classes inhibitors: substrate-analog...
This paper describes the synthesis of some novel azasterols based on (20R,22ξ)-5α-pregnan-20-(piperidin-2-yl)-3β,20-diol. These compounds are potential inhibitors enzyme sterol 24-methyltransferase (24-SMT), which is a vital in biosynthesis ergosterol and related 24-alkyl sterols. Structure−activity studies were undertaken to understand important features for activity against enzyme, with aim increasing selectivity. The evaluated inhibition recombinant Leishmania major 24-SMT effect...
ABSTRACT This paper describes the design and evaluation of novel azasterols as potential compounds for treatment leishmaniasis other diseases caused by trypanosomatid parasites. Azasterols are a known class ( S )-adenosyl- l -methionine: Δ 24 -sterol methyltransferase(24-SMT) inhibitors in fungi, plants, some parasitic protozoa. The prepared showed activity at micromolar nanomolar concentrations when tested against Leishmania spp. Trypanosoma enzymatic sterol composition studies indicated...
ER-119884 and E5700, novel arylquinuclidine derivatives developed as cholesterol-lowering agents, were potent in vitro growth inhibitors of both proliferative stages Leishmania amazonensis, the main causative agent cutaneous leishmaniasis South America, with 50% inhibitory concentrations (IC(50)s) being low-nanomolar to subnanomolar range. The compounds very noncompetitive native L. amazonensis squalene synthase (SQS), inhibition constants also nanomolar Growth was strictly associated...
Staphylococcus aureus produces a golden carotenoid virulence factor called staphyloxanthin (STX), and we report here the inhibition of enzyme, dehydrosqualene synthase (CrtM), responsible for first committed step in STX biosynthesis. The most active compounds are halogen-substituted phosphonosulfonates, with Ki values as low 5 nM against enzyme IC50 S. 11 nM. There is, however, only poor correlation (R2 = 0.27) between cell pIC50 (= −log10 IC50) values. ability to predict from data improves...
There is an urgent need for the development of new drugs treatment tropical parasitic diseases such as Chagas' disease and leishmaniasis. One potential drug target in organisms that cause these sterol biosynthesis. This paper describes design synthesis quinuclidine derivatives inhibitors a key enzyme biosynthesis, squalene synthase (SQS). A number compounds were recombinant Leishmania major SQS at submicromolar concentrations discovered. Some also selective parasite rather than homologous...
ABSTRACT As part of our efforts aimed at searching for new antiparasitic agents, the effect representative 2-alkylaminoethyl-1,1-bisphosphonic acids on Trypanosoma cruzi squalene synthase ( Tc SQS) was investigated. These compounds had proven to be potent inhibitors T. . This cellular activity been associated with an inhibition enzymatic farnesyl diphosphate synthase. 2-Alkylaminoethyl-1,1-bisphosphonic appear have a dual action, since they also inhibit SQS nanomolar range.
Objective. Report a case of Tuberous Sclerosis on childhood. Method. Database research and comparison with the report. Results. (TS) is an autosomal dominant disease that leads to formation hamartomas in multiple organs. From 80 90% individuals affected by TS present seizures during disease, are first clinical sign cases. This female patient, aged 2 years 1 month, presented hypopigmented macules right abdomen, infrapatellar, left inguinal infraoccipital areas, as well little erythematous...
Sleeping sickness or African trypanosomiasis is a serious health concern with an added socio-economic impact in sub-Saharan Africa due to direct infection both humans and their domestic livestock. There no vaccine available against trypanosomes its treatment relies only on chemotherapy. Although the current drugs are effective, most of them far from modern concept drug terms toxicity, specificity therapeutic regime. In search for new molecules trypanocidal activity, high throughput screening...
A Displasia cortical focal, descrita pela primeira vez por Taylor em 1971, constitui uma causa bem conhecida de epilepsia refractaria, susceptivel resposta favoravel ao tratamento cirurgico. Descreve-se o caso crianca oito anos com secundaria a displasia resistente medico. Apos adequada caracterizacao da lesao epileptogenica foi submetida excisao cirurgica, posterior evolucao clinica favoravel. Perante medicamente intratavel localizada e excisao, cirurgia impoe-se como opcao terapeutica...
Apresenta-se um caso clinico de uma crianca 9 anos, com lesoes cutâneas hiperpigmentadas, forma bizarra, em que foi feito o diagnosticode fitofotodermatite. A proposito deste os autores fazem revisao bibliografica desta patologia pouco frequente mas para a qual e necessario estaratento.
Sao apresentados os resultados clinicos, radiograficos, manometricos e terapeuticos em seis doentes com o diagnostico de «Acalasia do Esofago», idades compreendidas entre 4,5 13,5 anos constituindo a casuistica da Unidade Gastroenterologia Pediatrica Hospital Santa Maria 1986 1998. Foram ugurgitacao perda ponderai as formas apresentacao mais frequentes. A forma frequente foi regurgitacao ponderai. O atraso relacao ao inicio sintomatologia 23 meses manometria esofagica diagnostica todos. Dois...