Rino Stocco
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Explore the profile of Rino Stocco including associated specialties, affiliations and a list of published articles.
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20
Citations
316
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Recent Articles
1.
Xu H, George E, Gallo D, Medvedev S, Wang X, Kryczka R, et al.
Res Sq
. 2024 Feb;
PMID: 38410486
Ovarian cancers (OVCAs) and endometrial cancers (EMCAs) with amplification are often resistant to standard of care treatment and represent an unmet clinical need. Previously, synthetic-lethal screening identified loss of the...
2.
Black W, Abdoli A, An X, Auger A, Beaulieu P, Bernatchez M, et al.
J Med Chem
. 2024 Feb;
67(4):2349-2368.
PMID: 38299539
ATR is a key kinase in the DNA-damage response (DDR) that is synthetic lethal with several other DDR proteins, making it an attractive target for the treatment of genetically selected...
3.
Bubenik M, Mader P, Mochirian P, Vallee F, Clark J, Truchon J, et al.
J Med Chem
. 2022 Sep;
65(19):13198-13215.
PMID: 36126059
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. Here, we describe our hit-to-lead...
4.
Szychowski J, Papp R, Dietrich E, Liu B, Vallee F, Leclaire M, et al.
J Med Chem
. 2022 Jul;
65(15):10251-10284.
PMID: 35880755
PKMYT1 is a regulator of CDK1 phosphorylation and is a compelling therapeutic target for the treatment of certain types of DNA damage response cancers due to its established synthetic lethal...
5.
Gallo D, Young J, Fourtounis J, Martino G, Alvarez-Quilon A, Bernier C, et al.
Nature
. 2022 Apr;
604(7907):749-756.
PMID: 35444283
Amplification of the CCNE1 locus on chromosome 19q12 is prevalent in multiple tumour types, particularly in high-grade serous ovarian cancer, uterine tumours and gastro-oesophageal cancers, where high cyclin E levels...
6.
Roulston A, Zimmermann M, Papp R, Skeldon A, Pellerin C, Dumas-Berube E, et al.
Mol Cancer Ther
. 2021 Dec;
21(2):245-256.
PMID: 34911817
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 (NCT04497116). RP-3500 is highly potent with IC values...
7.
Zaghdane H, Boyd M, Colucci J, Simard D, Berthelette C, LeBlanc Y, et al.
Bioorg Med Chem Lett
. 2011 Apr;
21(11):3471-4.
PMID: 21515053
A new series of indole amide acting as hCRTH2 receptor ligands had been explored and are described herein. Several amide derivatives displaying low nanomolar activity in hCRTH2 binding and whole...
8.
Simard D, LeBlanc Y, Berthelette C, Zaghdane M, Molinaro C, Wang Z, et al.
Bioorg Med Chem Lett
. 2010 Dec;
21(2):841-5.
PMID: 21185722
A new class of 7-azaindole analogs of MK-7246 as potent and selective CRTH2 antagonists is reported. The SAR leading to the identification of the optimal azaindole regioisomer as well as...
9.
Boyd M, Berthelette C, Chiasson J, Clark P, Colucci J, Denis D, et al.
Bioorg Med Chem Lett
. 2010 Dec;
21(1):484-7.
PMID: 21126875
A novel series of EP(4) ligands, based on a benzyl indoline scaffold, has been discovered. It was found that agonism and antagonism in this series can be easily modulated by...
10.
Gallant M, Beaulieu C, Berthelette C, Colucci J, A Crackower M, Dalton C, et al.
Bioorg Med Chem Lett
. 2010 Nov;
21(1):288-93.
PMID: 21106375
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 enabling...