RP-3500: a novel, potent, and selective ATR inhibitor that is effective in preclinical models as a monotherapy and in combination with PARP inhibitors
…, A Mulani, V Rimkunas, A Veloso, M Hamel… - Molecular cancer …, 2022 - AACR
Ataxia telangiectasia and Rad3-related (ATR) kinase protects genome integrity during DNA
replication. RP-3500 is a novel, orally bioavailable clinical-stage ATR kinase inhibitor (…
replication. RP-3500 is a novel, orally bioavailable clinical-stage ATR kinase inhibitor (…
Identification of RP-6685, an orally bioavailable compound that inhibits the DNA polymerase activity of Polθ
…, R Papp, MC Mathieu, M Hamel… - Journal of medicinal …, 2022 - ACS Publications
DNA polymerase theta (Polθ) is an attractive synthetic lethal target for drug discovery,
predicted to be efficacious against breast and ovarian cancers harboring BRCA-mutant alleles. …
predicted to be efficacious against breast and ovarian cancers harboring BRCA-mutant alleles. …
The C3a receptor antagonist SB 290157 has agonist activity
MC Mathieu, N Sawyer, GM Greig, M Hamel… - Immunology letters, 2005 - Elsevier
The anaphylatoxin C3a is an important immune regulator with a number of distinct functions
in both innate and adaptive immunity. Many of these roles have been ascribed to C3a based …
in both innate and adaptive immunity. Many of these roles have been ascribed to C3a based …
Discovery of thiophene-2-carboxylic acids as potent inhibitors of HCV NS5B polymerase and HCV subgenomic RNA replication. Part 2: tertiary amides
…, D Nasturica, C Moinet, R Bethell, M Hamel… - Bioorganic & medicinal …, 2004 - Elsevier
Further SAR studies on the thiophene-2-carboxylic acids are reported. These studies led to
the identification of a series of tertiary amides that show inhibition of both HCV NS5B …
the identification of a series of tertiary amides that show inhibition of both HCV NS5B …
Discovery of thiophene-2-carboxylic acids as potent inhibitors of HCV NS5B polymerase and HCV subgenomic RNA replication. Part 1: Sulfonamides
…, D Labrecque, R Bethell, M Hamel… - Bioorganic & medicinal …, 2004 - Elsevier
… Yannopoulos , Nghe Nguyen-Ba , Denis Labrecque , Richard Bethell , Martine Hamel ,
Philippe Courtemanche-Asselin , Lucille L'Heureux , Maud David , Olivier Nicolas …
Philippe Courtemanche-Asselin , Lucille L'Heureux , Maud David , Olivier Nicolas …
Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases
…, RW Friesen, D Guay, FG Gervais, M Hamel… - Bioorganic & medicinal …, 2011 - Elsevier
In this manuscript we wish to report the discovery of MK-7246 (4), a potent and selective
CRTH2 (DP2) antagonist. SAR studies leading to MK-7246 along with two synthetic sequences …
CRTH2 (DP2) antagonist. SAR studies leading to MK-7246 along with two synthetic sequences …
The identification of 4, 7-disubstituted naphthoic acid derivatives as UDP-competitive antagonists of P2Y14
…, JF Fournier, S Gagné, Y Gareau, M Hamel… - Bioorganic & medicinal …, 2011 - Elsevier
A weak, UDP-competitive antagonist of the pyrimidinergic receptor P2RY 14 with a
naphthoic acid core was identified through high-throughput screening. Optimization provided …
naphthoic acid core was identified through high-throughput screening. Optimization provided …
Pharmacological characterization of MK-7246, a potent and selective CRTH2 (chemoattractant receptor-homologous molecule expressed on T-helper type 2 cells) …
FG Gervais, N Sawyer, R Stocco, M Hamel… - Molecular …, 2011 - ASPET
The chemoattractant receptor-homologous molecule expressed on T-helper type 2 cells (CRTH2)
is a G protein-coupled receptor that has been reported to modulate inflammatory …
is a G protein-coupled receptor that has been reported to modulate inflammatory …
Identification of N,N-Disubstituted Phenylalanines as a Novel Class of Inhibitors of Hepatitis C NS5B Polymerase
…, MH Alaoui-Ismaili, R Bethell, M Hamel… - Journal of medicinal …, 2003 - ACS Publications
… Martine Hamel … Das, Carl Poisson, Nghe Nguyen-Ba, Nathalie Turcotte, Melanie Proulx,
Lilianne Halab, Wuyi Wang, Jean Bédard, Nicolas Morin, Martine Hamel, Olivier Nicolas …
Lilianne Halab, Wuyi Wang, Jean Bédard, Nicolas Morin, Martine Hamel, Olivier Nicolas …
Applying the pro-drug approach to afford highly bioavailable antagonists of P2Y14
…, JF Fournier, S Gagné, JY Gauthier, M Hamel… - Bioorganic & medicinal …, 2011 - Elsevier
Our series of competitive antagonists against the G-protein coupled receptor P2Y 14 were
found to be highly shifted in the presence of serum (>99% protein bound). A binding assay …
found to be highly shifted in the presence of serum (>99% protein bound). A binding assay …