Espanhol é um dos principais estudiosos da metodologia da síntese de peptídeos
Ele é um dos mais importantes cientistas na metodologia de síntese de peptídeos. Fundador do Instituto de Pesquisas em Biomedicina de Barcelona, tem mais de 800 artigos publicados e 50 patentes. O espanhol Fernando Albericio, do Departamento de Química Orgânica da Universidade de Barcelona, será um dos conferencistas convidados da 39a Reunião Anual, que será realizada a partir do próximo dia 30, em Goiânia, com o tema "Peptídeos Terapêuticos".
Albericio considera que deu uma guinada em sua carreira ao ir além do ambiente puramente acadêmico em 1991, quando resolveu aceitar o desafio de ser o diretor de pesquisa e desenvolvimento de uma indústria farmacêutica. "Foi lá que aprendi que a verdadeira pesquisa de qualidade é aquela que tem um impacto na sociedade. Pode ser a quebra de um paradigma, mas também um novo produto ou processo", afirmou ao Boletim da SBQ.
Nos últimos dez anos Alberício intensificou suas viagens e pesquisas a países no hemisfério Sul. "Foi uma segunda guinada na minha carreira. Nos países que visitei, percebi que com outra ciência é necessária, e possível. Vi excelentes universidades, mas com raras exceções no Brasil, pouco foco em pesquisa. São países ricos em recursos naturais que acabam exportadores de commodities", observou o professor. "É preciso ter centros de pesquisa disruptiva, baseada nos potenciais da região, com objetivo de mudar paradigmas no setor produtivo."
Albericio irá participar também da Sessão Temática "Criar e Empreender". Ele já mantém colaborações com pesquisadores brasileiros e espera aprofundar os laços com o Brasil. "Espero rever velhos amigos, conhecer novos e, também, realizar um sonho que é ter um laboratório em uma das excelentes universidades brasileiras", declarou.
Leia a íntegra da entrevista do professor Fernando Albericio ao Boletim da SBQ
What achievements have you and your research group recently made, and why are they important?
Four years ago, in our laboratory of South Africa, we have started a medicinal chemistry project focused to fight against infectious diseases. It is important to have in mind that the forecast for 2050 is the death of 50 million people caused by infectious diseases. In our laboratory, we have discovered recently a new family of Ultra Small Antimicrobial Peptides (USAMP) based in a natural product, which shows a "unique" structure and extraordinary biological activities. Thus, the in vitro activity against gram-negative bacteria in the low nanomolar range, is superior to current drugs existing in the market such as Imipenem. They also show excellent in vitro activity against gram-positive bacteria. One member of the family shows in vitro anti-Tuberculosis (TB) activity in the low nanomolar range, which is superior to the current anti-TB drugs existing in the market such as Isoniazid. As they show negligible in vitro cytotoxicity and hemolysis activity as well. It is very likely that a candidate will be able to enter clinical phases very soon under a European industrial consortium sponsored by the EC.
Unfortunately, I will be not able to talk about this research program, because we are filling the corresponding patent to protect the intellectual property and assure that the product can arrive to the market.
Talking about our research programs in cyclic peptides, during the last years, the first total synthesis of three intriguing cyclic peptides (Baringolin, Pipecolidepsin A, and Stellatolide) has been accomplished. All show a great synthetic difficulty and an important and interesting biological activity. Baringolin is a thiopeptide, which shows an important cytotoxic as well as antimicrobial activity. It is constituted for several thiazole moieties in a row. Currently, a medicinal chemistry program has been launched. As first result, a "hit" with improved biological activity and simplified synthetic difficulty has been identified. Pipecolidepsin A constitutes the first example of synthesis of a peptide which contains the non-natural, rare, and much hindered, (2R, 3R, 4R)-2-amine-3-hydroxy-4,5-dimethylhexanoic acid (D-allo-AHDMHA), whose presence has jeopardized its synthesis. All synthetic process has been covered with a patent, has merit publication in Nature Commun., and has had a great impact in the media.
How far (or close) are your achievements from industry?
My research is very close to society and in this sense is very close to the industry. I cannot understand a research that cannot be translated to the society and for that, academicians need connectors, such as the industries.
In 1991, I made a decision that changed my academic life. In that moment, I was Associate Professor at the University of Barcelona when I decided to join the American company Millipore-Waters (Bedford, MA) as Director of Research. While working there, I learned that true quality research is something that has an impact on society. This impact could be a paradigm shift, but also a new product or a new process.
During the Brazilian Chemical Society Conference, I will participate as speaker in two sessions. One during the purely scientific program, but also in the workshop of the last day called "Criar e Emprender". I am really happy to participate in both of them and more in a country such as Brazil. I was founder of the Barcelona Science Park at the University of Barcelona. Brazil and Spain are amongst countries where most science parks have been developed. However, this important fact has not been translated to the academic life.
Coming back to my personal profile, I am co-author of more than 800 scientific articles published in very high index impact journals, but I am very proud of having filled more than 50 patents. In the field of peptide synthesis methodologies, it can be said that almost all of the peptides that are worldwide synthesized at present, both for research as well as for production purposes for the pharmaceutical industry, are performed using methodologies and strategies developed in our research group.
PEG-PS, PAL, BAL, HMPA/HMPP, HFMS, HCTU, PyClock, OxymaPure, COMU, PyOxyma, KOxyma, Oxyma-B, Tmob, Fm, Phacm, DPM, S-Tmp are not a soup of letters, they are the acronyms of compounds developed in our laboratory and that are commercially available from several companies.
In the field of drug discovery, we are working mainly in cancer infective diseases. In cancer and in collaboration with a PharmaMar, a Spanish company, we have studied the marine ecosystem. Thus, from an extensive study of structure-activity around Kahalalide F, which is a cyclic peptide first isolated from a molusc, we identified an analog, Irvalec, that has reached clinical phase II for the treatment of different types of cancers.
In another project, we have developed a family of 1,2-diphenylpyrroles, which have an electron withdrawing substituent in position 3 of the pyrrole, which were transferred to the biotech, ArgoPharma SL. This family of compounds has shown activity for the treatment of several cancers (pancreas, lung, colorectal, breast, and/or prostate carcinoma, and has entered preclinical phase.
You have left one of the higher positions in Spanish science to work in Ecuador and now in South Africa. Could you explain your motivation in sharing your knowledge in the Southern hemisphere?
In the previous question, I was talking about that the decision of joining Millipore-Waters in 1991 changed my scientific life. In this sense, in the last decade, another realization helped change the focus of my academic journey. Until then, all my scientific activity had taken place in Northern countries or the so-called Western world, but then I had started to mainly travel through Latin America and South Africa, where I hold a Research Professor Position.
During my short stays in these parts of the world, I have realized that another kind of academia is necessary and, of course, possible. Thus, in Latin America there are excellent teaching universities, but, with minor exception in Brazil, there is little focus on research. These countries that hold enormous amounts of natural resources are used to export raw materials and import sophisticated ones, therefore resulting in the loss of all value. Furthermore, because the area lacks institutions for developing innovative projects, the best brains of Latin America migrate to worldwide elite universities and companies.
Latin America needs and deserves a large number of Research Universities able to carry out disruptive research. This should not be an imitation of those carried out in Western universities. This should be based on strengths of the region, with the objective of shifting the productive sector paradigm.
Two years ago, I accepted the proposition of the Ecuadorian government to be the Inaugural Rector of Yachay Tech, a new research university. Unfortunately, this project did not work. In a few words: too many politics and a lack of scientific culture.
But my journey continued and I accepted the offer of becoming Research Professor at the University of KwaZulu-Natal in Durban (South Africa). Here, we are developing the program in infectious diseases.
Here in the South, it does not matter where, in Brazil, South Africa, Ecuador, New Zealand, the compromise of the scientist with the society should be different. Here, our research should be objective-driven. It is my personal opinion that while part of the society suffers from threatening diseases such as tuberculosis, biomedicine researchers cannot run curiosity-driven projects. Our duty as human beings and as researchers is to drive our research to alleviate the suffering of an important part of society.
Finally, I would like to remind a poem of the excellent Uruguayan poet Mario Benedetti: El Sur también existe (The South does also exist). Please join me to show that In Ciencia, el Sur también existe.
Why is important that youth study science?
First of all, the really important is that youth studies. It does not matter what, but they have to study. They have to attend the University and if possible to get the maximum degree, a Ph.D. Why? Because they have to return to society what society has given to them. And with a better preparation, they will be able to do that easily.
Science? Because science is the most efficient tool to fight against the inequity that exists in the world. Science makes people free. Science adds value to natural resource in the benefit of the whole society. And Southern countries have these natural resources, but are dependent of the Northern countries for their development.
What do you expect from your visit to Brasil?
First of all, I would like to thank to the Brazilian Chemical Society for the invitation to participate in its annual meeting.
What are my expectations? I have several running collaborations with colleagues at the Brazilian universities. So, the first it will be to meet old friends, but I am expecting to acquire new friends and to start new collaborations.
Finally and if you allow me to share with you and all your readers one of my dreams, I would like to have a stable presence in Brazil. I would like to have a small laboratory in one of the excellent Brazilian universities.
“Two-electron Connection between Tryptophan and Phenylalanine/Tyrosine Residues: Linked, Constrained and Stapled Peptides through C-H Activation Processes”, L. Mendive-Tapia, S. Preciado, J. García, R. Ramón, F. Albericio, R. Lavilla, Nat. Comm. 2015, 6, 7160.
“Multifunctionalized polyurethane–polyurea nanoparticles: hydrophobically driven self-stratification at the o/w interface modulates encapsulation stability”, P. Rocas, Y. Fernández, S. Schwartz Jr, I. Abasolo, J. Rocas, F. Albericio, J. Mat., Chem. B2015, 3, 7604-7613.
“Chemical protein synthesis using a second generation N-acylurea linker for the preparation of peptide-thioester precursors”, JB. Blanco-Canosa, B. Nardone, F. Albericio, PE. Dawson, J. Am. Chem. Soc 2015, 137, 7197.
“Polythiazole Linkers as Functional Rigid Connectors: a New RGD Cyclopeptide with Enhanced Integrin Selectivity”, J. Ruiz-Rodríguez, M. Miguel, S. Preciado, G. Acosta, J. Adan, A. Bidon-Chanal, FJ. Luque, F. Mitjans, R. Lavilla, F. Albericio, Chem. Sci.2015, 5, 3929.
“Stellatolides, a new cyclodepsipeptide family, from the sponge Ecionemia acervus. Isolation, Solid-phase Total Synthesis and Full Structural Assignment of Stellatolide A”, MJ. Martín, R. Rodríguez-Acebes, Y. García-Ramos, V. Martínez, C. Murcia, I. Digón, I. Marco, R. Fernández, F. Reyes, AM. Francesch, S. Munt, M. Pelay-Gimeno, J. Tulla-Puche, F. Albericio, C. Cuevas, J. Am. Chem. Soc. 2014, 136, 6754.
Para saber mais:
A 39ª Reunião Anual da SBQ será no Centro de Convenções de Goiânia, de 30 de maio a 2 de junho de 2016.
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Texto: Mario Henrique Viana, assessor de imprensa da SBQ