List of works - Luca Settimo

Design and optimization of selective protein kinase C θ (PKCθ) inhibitors for the treatment of autoimmune diseases

scientific article

Determinants of antagonist binding at the alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor subunit, GluR-D. Role of the conserved arginine 507 and glutamate 727 residues

scientific article published in December 2002

Determination of binding site residues responsible for the subunit selectivity of novel marine-derived compounds on kainate receptors

scientific article published on 14 March 2006

Discovery of Selective, Orally Bioavailable Pyrazolopyridine Inhibitors of Protein Kinase Cθ (PKCθ) That Ameliorate Symptoms of Experimental Autoimmune Encephalomyelitis

scientific article published on 27 June 2019

Discrimination between agonists and antagonists by the alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid-selective glutamate receptor. A mutation analysis of the ligand-binding domain of GluR-D subunit

scientific article published on 7 August 2002

Divergent pharmacological activity of novel marine-derived excitatory amino acids on glutamate receptors

scientific article published on 24 May 2005

Evolutionary genomics of epidemic visceral leishmaniasis in the Indian subcontinent

scientific article

Functional analysis of drug resistance-associated mutations in the Trypanosoma brucei adenosine transporter 1 (TbAT1) and the proposal of a structural model for the protein

scientific article published on 21 March 2015

Model structures of the N-methyl-D-aspartate receptor subunit NR1 explain the molecular recognition of agonist and antagonist ligands

scientific article published in March 2004

Positively selected modifications in the pore of TbAQP2 allow pentamidine to enter Trypanosoma brucei

scientific article published on 07 August 2020

Repurposing human PDE4 inhibitors for neglected tropical diseases. Evaluation of analogs of the human PDE4 inhibitor GSK-256066 as inhibitors of PDEB1 of Trypanosoma brucei

scientific article

Repurposing human PDE4 inhibitors for neglected tropical diseases: design, synthesis and evaluation of cilomilast analogues as Trypanosoma brucei PDEB1 inhibitors

scientific article

Selective agonist binding of (S)-2-amino-3-(3-hydroxy-5-methyl-4-isoxazolyl)propionic acid (AMPA) and 2S-(2alpha,3beta,4beta)-2-carboxy-4-(1-methylethenyl)-3-pyrrolidineacetic acid (kainate) receptors: a molecular modeling study

scientific article published in December 2003

Structure-based optimization of aminopyridines as PKCθ inhibitors.

scientific article

Subtype selectivity and flexibility of ionotropic glutamate receptors upon antagonist ligand binding

scientific article published on 26 January 2006

Transport proteins determine drug sensitivity and resistance in a protozoan parasite, Trypanosoma brucei

scientific article

List of works by Luca Settimo

Design and optimization of selective protein kinase C θ (PKCθ) inhibitors for the treatment of autoimmune diseases

Determinants of antagonist binding at the alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor subunit, GluR-D. Role of the conserved arginine 507 and glutamate 727 residues

Determination of binding site residues responsible for the subunit selectivity of novel marine-derived compounds on kainate receptors

Discovery of Selective, Orally Bioavailable Pyrazolopyridine Inhibitors of Protein Kinase Cθ (PKCθ) That Ameliorate Symptoms of Experimental Autoimmune Encephalomyelitis

Discrimination between agonists and antagonists by the alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid-selective glutamate receptor. A mutation analysis of the ligand-binding domain of GluR-D subunit

Divergent pharmacological activity of novel marine-derived excitatory amino acids on glutamate receptors

Evolutionary genomics of epidemic visceral leishmaniasis in the Indian subcontinent

Functional analysis of drug resistance-associated mutations in the Trypanosoma brucei adenosine transporter 1 (TbAT1) and the proposal of a structural model for the protein

Model structures of the N-methyl-D-aspartate receptor subunit NR1 explain the molecular recognition of agonist and antagonist ligands

Positively selected modifications in the pore of TbAQP2 allow pentamidine to enter Trypanosoma brucei

Repurposing human PDE4 inhibitors for neglected tropical diseases. Evaluation of analogs of the human PDE4 inhibitor GSK-256066 as inhibitors of PDEB1 of Trypanosoma brucei

Repurposing human PDE4 inhibitors for neglected tropical diseases: design, synthesis and evaluation of cilomilast analogues as Trypanosoma brucei PDEB1 inhibitors

Selective agonist binding of (S)-2-amino-3-(3-hydroxy-5-methyl-4-isoxazolyl)propionic acid (AMPA) and 2S-(2alpha,3beta,4beta)-2-carboxy-4-(1-methylethenyl)-3-pyrrolidineacetic acid (kainate) receptors: a molecular modeling study

Structure-based optimization of aminopyridines as PKCθ inhibitors.

Subtype selectivity and flexibility of ionotropic glutamate receptors upon antagonist ligand binding

Transport proteins determine drug sensitivity and resistance in a protozoan parasite, Trypanosoma brucei