Publications

Our published work.

Research Papers

Small artigo2

Targeting transthyretin amyloidosis in the eye with next-generation stabilizers: AT40 displays potent TTR stabilization in the human vitreous.

Bezerra F, Simões CJV, Beirão JM, Saraiva MJ, Brito RMM, Almeida MR

Amyloid. 2019;26(sup1):73-74
Small artigo 1

Lead optimization of resilient next-generation transthyretin stabilizers for multiple target-product profiles: approaching the CNS

Simões CJV, Almeida ZL, Cardoso AL, Bezerra F, Almeida MR, Beirão J, Pinho e Melo TMVD, Saraiva MJ, Brito RMM

Amyloid. 2019;26(sup1):77-78
Small paper1

A novel bis-furan scaffold transthyretin stabilization and amyloid inhibition.

Simões CJV, Almeida ZL, Costa D, Jesus CSH, Cardoso AL, Almeida MR, Saraiva MJ, Pinho e Melo TMVD, Brito RMM

Eur J Med Chem. 2016 Oct 4;121:823-840
Small paper2

Toward the discovery of functional transthyretin amyloid inhibitors: application of virtual screening methods.

Simões CJ, Mukherjee T, Brito RM, Jackson RM

J Chem Inf Model. 2010 Oct 25;50(10):1806-20
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Potentially amyloidogenic conformational intermediates populate the unfolding landscape of transthyretin: insights from molecular dynamics simulations.

Rodrigues JR, Simões CJ, Silva CG, Brito RM

Protein Sci. 2010 Feb;19(2):202-19
Small paper4

A relational learning approach to Structure-Activity Relationships in drug design toxicity studies.

Camacho R, Pereira M, Costa VS, Fonseca NA, Adriano C, Simões CJ, Brito RM

J Integr Bioinform. 2011 Sep 16;8(3):182
Small paper5

A look into amyloid formation by transthyretin: aggregation pathway and a novel kinetic model.

Faria TQ, Almeida ZL, Cruz PF, Jesus CS, Castanheira P, Brito RM

Phys Chem Chem Phys. 2015 Mar 21;17(11):7255-63
Small paper6

A New Folding Kinetic Mechanism for Human Transthyretin and the Influence of the Amyloidogenic V30M Mutation.

Jesus CS, Almeida ZL, Vaz DC, Faria TQ, Brito RM

Int J Mol Sci. 2016 Aug 31;17(9)
Small paper7

Comparative calorimetric study of non-amyloidogenic and amyloidogenic variants of the homotetrameric protein transthyretin.

Shnyrov VL, Villar E, Zhadan GG, Sanchez-Ruiz JM, Quintas A, Saraiva MJ, Brito RM

Biophys Chem. 2000 Dec 15;88(1-3):61-7
Small paper8

Tetramer dissociation and monomer partial unfolding precedes protofibril formation in amyloidogenic transthyretin variants.

Quintas A, Vaz DC, Cardoso I, Saraiva MJ, Brito RM

J Biol Chem. 2001 Jul 20;276(29):27207-13
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The tetrameric protein transthyretin dissociates to a non-native monomer in solution. A novel model for amyloidogenesis.

Quintas A, Saraiva MJ, Brito RM

J Biol Chem. 1999 Nov 12;274(46):32943-9

Communications

Publication

AT50 Series: 2 - thioxothiazolin - 4 - one derivatives as novel potent transthyretin stabilizers

A.L. Cardoso , B.F.O. Nascimento, Z.L. Almeida, B.L. Victor, C.J.V. Simões, R.M.M. Brito, T.M.V.D Pinho e Melo

Italian-Spanish-Portuguese Joint Meeting in Medicinal Chemistry, July 2018, Palermo, Italy

Publication

Rational design, synthesis and biological evaluation of inhibitors of transthyretin amyloidogenesis: optimization of thiazolidinedione - based derivatives

Z.L. Almeida , C.J.V. Simões, B.F.O . Nascimento, B.L. Víctor; A.L. Cardoso, P.F. Cruz , T.M.V.D. Pinho e Melo , R.M.M. Brito

Italian-Spanish-Portuguese Joint Meeting in Medicinal Chemistry, July 2018, Palermo, Italy

Publication

Classification of corneal permeability of drug-like compounds using data mining and machine learning

Meireles J, Simões CJV, Brito RMM

11th International Conference on Chemical Structures, May 2018, Noordwijkerhout, The Netherlands

Publication

Lead Optimization of Resilient Second-Generation Transthyretin Stabilizers for Multiple Target-Product Profiles: Where Do We Go From Here?

Simões CJV, Almeida ZL, Cardoso AL, Almeida MR, Beirão J, Pinho e Melo TMVD, Saraiva MJ, Brito RMM

XVIth International Symposium on Amyloidosis, March 2018, Kumamoto, Japan

Publication

Targeting transthyretin amyloidosis in the eye with a second-generation stabilizer: AT40X01 displays potent TTR stabilization in the human vitreous.

Bezerra F, Beirão J, Simões CJV, Brito RMM, Saraiva MJ, Almeida MR

XVIth International Symposium on Amyloidosis, March 2018, Kumamoto, Japan

Publication

Highly active 2-thioxothiazolidin-4-one derivatives for transthyretin protein stabilization and amyloid fibril inhibition.

Nascimento BFO, Almeida ZL, Simões CJV, Victor BL, Cardoso AL, Brito RMM, Pinho e Melo TMVD

12th National Organic Chemistry Meeting (12ENQO) and the 5th National Medicinal Chemistry Meeting (5ENQT), January 2018, Coimbra, Portugal

Publication

Discovery of 2-thioxothiazolidin-4-ones as potent transthyretin stabilizers: a story of pride and prejudice in the quest for a better drug.

Simões CJV, Almeida ZL, Victor BL, Nascimento BFO, Cardoso AL, Pinho e Melo TMVD, Brito RMM

12th National Organic Chemistry Meeting (12ENQO) and the 5th National Medicinal Chemistry Meeting (5ENQT), January 2018, Coimbra, Portugal

Patents

Small wipo

Bis-furan derivatives as transthyretin (TTR) stabilizers and amyloid inhibitors for the treatment of familial amyloid polyneuropathy (FAP)

Vieira Simões, Carlos José; Lourenço de Almeida, Zaida Catarina; Vasconcelos Dias de Pinho e Melo, Teresa Margarida; Pontes Meireles Ferreira de Brito, Rui Manuel; Silva Costa, Dora Cristina; Cabral Cardoso Lopes, Ana Lúcia

Patent Application (PCT) no. WO/2016/203402

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Bis-furan derivatives as transthyretin (TTR) stabilizers and amyloid inhibitors for the treatment of familial amyloid polyneuropathy (FAP)

Vieira Simões, Carlos José; Lourenço de Almeida, Zaida Catarina; Vasconcelos Dias de Pinho e Melo, Teresa Margarida; Pontes Meireles Ferreira de Brito, Rui Manuel; Silva Costa, Dora Cristina; Cabral Cardoso Lopes, Ana Lúcia

United States Patent no. 10377729

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Bis-furan derivatives as transthyretin (TTR) stabilizers and amyloid inhibitors for the treatment of familial amyloid polyneuropathy (FAP)

Vieira Simões, Carlos José; Lourenço de Almeida, Zaida Catarina; Vasconcelos Dias de Pinho e Melo, Teresa Margarida; Pontes Meireles Ferreira de Brito, Rui Manuel; Silva Costa, Dora Cristina; Cabral Cardoso Lopes, Ana Lúcia

European Patent no. EP3307723

Small netherlands

Bis-furan derivatives as transthyretin (TTR) stabilizers and amyloid inhibitors for the treatment of familial amyloid polyneuropathy (FAP)

Vieira Simões, Carlos José; Lourenço de Almeida, Zaida Catarina; Vasconcelos Dias de Pinho e Melo, Teresa Margarida; Pontes Meireles Ferreira de Brito, Rui Manuel; Silva Costa, Dora Cristina; Cabral Cardoso Lopes, Ana Lúcia

The Netherlands | EP-NL Patent no. EP3307723

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BIS-FURANDERIVATER SOM TRANSTHYRETIN (TTR)-STABILISERINGSMIDLER OG AMYLOIDHÆMMERE TIL BEHANDLING AF FAMILIÆR AMYLOID POLYNEUROPATI (FAP)

Vieira Simões, Carlos José; Lourenço de Almeida, Zaida Catarina; Vasconcelos Dias de Pinho e Melo, Teresa Margarida; Pontes Meireles Ferreira de Brito, Rui Manuel; Silva Costa, Dora Cristina; Cabral Cardoso Lopes, Ana Lúcia

Denmark | Patent/Reg. no. DK/EP 3307723

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Derivados de bis-furano como estabilizadores de transtirretina (TTR) e inibidores de amilóide para o tratamento de Polineuropatia Amiloidótica Familiar (FAP)

Vieira Simões, Carlos José; Lourenço de Almeida, Zaida Catarina; Vasconcelos Dias de Pinho e Melo, Teresa Margarida; Pontes Meireles Ferreira de Brito, Rui Manuel; Silva Costa, Dora Cristina; Cabral Cardoso Lopes, Ana Lúcia

Portugal | EP-PT Patent no. EP3307723

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Bisfuranderivat som prealbuminstabiliserande medel (TTR-stabiliserande medel) och amyloidhämmare för behandling av familjär amyloid polyneuropati (FAP)

Vieira Simões, Carlos José; Lourenço de Almeida, Zaida Catarina; Vasconcelos Dias de Pinho e Melo, Teresa Margarida; Pontes Meireles Ferreira de Brito, Rui Manuel; Silva Costa, Dora Cristina; Cabral Cardoso Lopes, Ana Lúcia

Sweden | Patent no. SE 3307723 T3

Small teste

Bis-furan derivate als transthyretin (TTR) stabilisatoren und amyloid inhibitoren zur behandlung von familiarer amyloid polyneuropathie (FAP)

Vieira Simões, Carlos José; Lourenço de Almeida, Zaida Catarina; Vasconcelos Dias de Pinho e Melo, Teresa Margarida; Pontes Meireles Ferreira de Brito, Rui Manuel; Silva Costa, Dora Cristina; Cabral Cardoso Lopes, Ana Lúcia

Switzerland/Liechtenstein | EP-CH/LI Patent no. EP3307723

Small germany

Bis-furan derivate als transthyretin (TTR) stabilisatoren und amyloid inhibitoren zur behandlung von familiarer amyloid polyneuropathie (FAP)

Vieira Simões, Carlos José; Lourenço de Almeida, Zaida Catarina; Vasconcelos Dias de Pinho e Melo, Teresa Margarida; Pontes Meireles Ferreira de Brito, Rui Manuel; Silva Costa, Dora Cristina; Cabral Cardoso Lopes, Ana Lúcia

Germany | EP-DE Patent no. EP3307723

Small teste

Dérivés bis-furan en tant que stabilisateurs de la transthyrétine (TTR) et inhibiteurs de l’amyloid pour le traitement de la polyneuropathie amiloide familiale (PAF)

Vieira Simões, Carlos José; Lourenço de Almeida, Zaida Catarina; Vasconcelos Dias de Pinho e Melo, Teresa Margarida; Pontes Meireles Ferreira de Brito, Rui Manuel; Silva Costa, Dora Cristina; Cabral Cardoso Lopes, Ana Lúcia

France | EP-FR Patent no. EP3307723

Small teste

Bis-furan derivatives as transthyretin (ttr) stabilizers and amyloid inhibitors for the treatment of familial amyloid polyneuropathy (fap)

Vieira Simões, Carlos José; Lourenço de Almeida, Zaida Catarina; Vasconcelos Dias de Pinho e Melo, Teresa Margarida; Pontes Meireles Ferreira de Brito, Rui Manuel; Silva Costa, Dora Cristina; Cabral Cardoso Lopes, Ana Lúcia

UK | EP-GB Patent no. EP3307723

Small ireland

Bis-furan derivatives as transthyretin (ttr) stabilizers and amyloid inhibitors for the treatment of familial amyloid polyneuropathy (fap)

Vieira Simões, Carlos José; Lourenço de Almeida, Zaida Catarina; Vasconcelos Dias de Pinho e Melo, Teresa Margarida; Pontes Meireles Ferreira de Brito, Rui Manuel; Silva Costa, Dora Cristina; Cabral Cardoso Lopes, Ana Lúcia

Ireland | EP-IE Patent no. EP3307723

Small wipo

2-thioxothiazolidin-4-one derivatives active as transthyretin ligands and uses thereof

Pontes Meireles Ferreira de Brito, Rui Manuel; Vieira Simões, Carlos José; Vasconcelos Dias de Pinho e Melo, Teresa Margarida; Victor, Bruno Lourenço da Silva; Lourenço de Almeida, Zaida Catarina; Lopes, Ana Lúcia Cabral Cardoso; Nascimento, Bruno Filipe Oliveira

Patent Application (PCT) no. WO/2016/080853

Small uspto

2-thioxothiazolidin-4-one derivatives active as transthyretin ligands and uses thereof

Pontes Meireles Ferreira de Brito, Rui Manuel; Vieira Simões, Carlos José; Vasconcelos Dias de Pinho e Melo, Teresa Margarida; Victor, Bruno Lourenço da Silva; Lourenço de Almeida, Zaida Catarina; Lopes, Ana Lúcia Cabral Cardoso; Nascimento, Bruno Filipe Oliveira

United States Patent no. 11117877

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