Research interest of LASSBio
Portuguese version
The main research focus of the Laboratory of Evaluation and Synthesis of Bioactive Substances - LASSBio (Laboratório de Avaliação e Síntese de Substâncias Bioativas) of the Federal University of Rio de Janeiro (Universidade Federal do Rio de Janeiro - UFRJ) is in Medicinal Chemistry.1 This research area aims the rational planning and design of new ligands to attractive targets (e.g. enzymes or bioreceptors), the synthesis of these original compounds and their pharmacological evaluation, in order to identify new drug candidates acting on single or multiple targets to the control and treatment of chronic non transmissible diseases, including inflammatory and neurodegenerative disorders, diabetes, cancer, among others. In addition, the search for novel analgesic prototypes specially designed to control neuropathic pain and for new antiprotozoal drug candidates directed to the treatment of leishmaniasis and other neglected diseases also represent additional challenges to LASSBio research effort.

The in silico and in vitro studies of ADME properties are also performed in LASSBio, ensuring an adequate selection of the lead candidate compounds. The phenotypic evaluation, which allows the identification of the desired pharmacotherapeutic properties, validating the selected therapeutic target, is also performed in-house. Moreover, the in vitro early study of any eventual toxicity of the new discovered lead compounds is also executed in LASSBio.

Additionally, to achieve all goals related to the Drug Discovery (DD) process, LASSBio has several inter-institutional collaborations2, in consonance with the interdisciplinary character of Medicinal Chemistry, aiming to discover innovative drugs candidates. It is the headquarter of the National Institute of Science and Technology in Drugs and Medicines (INCT-INOFAR), a Brazilian network focused on DD which includes several academic laboratories and pharmochemical and pharmaceutical companies.

           Several classic and modern Medicinal Chemistry strategies are successfully employed in the rational design of new molecular frameworks in LASSBio. For instance, the use of molecular simplification, molecular hybridization and bioisosterism strategies,2 alone or combined, have been successfully employed in LASSBio to identify new and original derivatives, planned to present high affinity for one or several elected therapeutic targets, representing valuable and innovative prototypes. The research efforts done in LASSBio3 have been successful in the discovery of several original lead-compounds of real therapeutic interest, which have been object of requests for invention privilege in Brazil and abroad, with ca. 20 patent deposits for new pharmaceuticals taking place from 1999 on. One patent was obtained in 2006 from USPTO, titled “LASSBio-294: A Novel Digitalis-like Compound with Potential Anti-fatigue Activity" (7.091.238, dated August 15, 2006), reporting a new multitarget cardioactive lead-compound, with a novel mechanism of action.4

LASSBio has recently celebrated 22 years of activities, on last April 19th, 2016, and it has consolidated a solid research reputation on Medicinal Chemistry field with a chemical library of nearly 2000 original compounds. The academic contribution of LASSBio has resulted in more than 100 graduate students formed as MSc & PhDs and numerous post-doctorate training. From this work efforts, LASSBio is the source of more than 250 original multi-authors scientific publications, keeping an expressive ratio of more than 10 publications in indexed journals with high impact index each year for the last ten years.

LASSBio also develops an extensive outreach activity with the promotion of the Summer School in Medicinal Chemistry, which has achieved the twenty-second edition last January 2016. Furthermore, LASSBio is also responsible for the “Portal dos Fármacos” website that, together with the “Instituto Virtual de Fármacos” initiative, intends to divulge procedures and guidance to ensure the safe use of medicines by the population. .

The permanent staff of LASSBio are formed by:

Eliezer J. Barreiro
Full-Professor (ICB, UFRJ), Scientific Coordinator
CV-Lattes in:

Carlos Alberto Manssour Fraga
Full-Professor (ICB, UFRJ)
CV-Lattes in:

Lidia Moreira Lima
Associate Professor (ICB, UFRJ)
CV-Lattes in:

Carlos Maurício Rabello Sant’Anna
Associate Professor (ICE-UFRRJ)
CV-Lattes in:

Hélio de Mattos Alves
Adjunct Professor (FF-UFRJ)
CV-Lattes in:

Maria Letícia de Castro Barbosa
Adjunct Professor (FF-UFRJ)
CV-Lattes in:

Rio de Janeiro, July, 2016

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Portuguese version
Últimas Notícias

LASSBio INCT-INOFAR Portal dos FármacosICB - UFRJ
Desenvolvido por: Cúpula Informática