Publications

Our published work.

Research Papers

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
Small abstract3

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
Small paper9a

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

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

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

Patents

Small patent1a

Bis-furan derivatives as transthyretin (TTR) stabilizers and amyloid inhibitors for the treatment of Familial Amyloid Polyneuropathy (FAP).

Simões CJV, Almeida ZL, Cardoso AL, Pinho e Melo TMVD, Brito RMM, Costa D

WO/2016/203402

Small patente2

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

Brito RMM, Simões CJV, Pinho e Melo TMVD, Victor BLS, Almeida ZL, Cardoso AL, Nascimento BF, Ferreira MS

WO/2016/080853

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