Olivier Geneste
Overview
Explore the profile of Olivier Geneste including associated specialties, affiliations and a list of published articles.
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Articles
22
Citations
2044
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Recent Articles
1.
Sipos S, Balazs B, Gati T, Csekei M, Kovaacs M, Kovacs M, et al.
ChemMedChem
. 2025 Feb;
:e202400970.
PMID: 39895364
Atropisomersm is an emerging feature in recent drug candidates due to the increasing complexity of the targeted protein surfaces. The developability of the drug candidates requires that their atropisomer interconversion...
2.
Vasas A, Ivanschitz L, Molnar B, Kiss A, Baker L, Fiumana A, et al.
J Med Chem
. 2024 Oct;
67(21):18993-19009.
PMID: 39441669
Inhibition of ubiquitin-specific protease 7, USP7, has been proposed as a mechanism to affect many disease processes, primarily those implicated in oncology. The bound crystal structure of a published high-throughput...
3.
Sipos S, Balint B, Szabo Z, Ondi L, Csekei M, Szlavik Z, et al.
ACS Omega
. 2021 Sep;
6(34):22073-22102.
PMID: 34497901
Following the identification of thieno[2,3-]pyrimidine-based selective and potent inhibitors of MCL-1, we explored the effect of core swapping at different levels of advancement. During hit-to-lead optimization, X-ray-guided S-N replacement in...
4.
Szlavik Z, Csekei M, Paczal A, Szabo Z, Sipos S, Radics G, et al.
J Med Chem
. 2020 Nov;
63(22):13762-13795.
PMID: 33146521
Myeloid cell leukemia 1 (Mcl-1) has emerged as an attractive target for cancer therapy. It is an antiapoptotic member of the Bcl-2 family of proteins, whose upregulation in human cancers...
5.
Moujalled D, Hanna D, Hediyeh-Zadeh S, Pomilio G, Brown L, Litalien V, et al.
Blood Adv
. 2020 Jun;
4(12):2762-2767.
PMID: 32569380
Improving survival outcomes in adult B-cell acute lymphoblastic leukemia (B-ALL) remains a clinical challenge. Relapsed disease has a poor prognosis despite the use of tyrosine kinase inhibitors (TKIs) for Philadelphia...
6.
Murray J, Davidson J, Chen I, Davis B, Dokurno P, Graham C, et al.
ACS Omega
. 2019 Aug;
4(5):8892-8906.
PMID: 31459977
We describe our work to establish structure- and fragment-based drug discovery to identify small molecules that inhibit the anti-apoptotic activity of the proteins Mcl-1 and Bcl-2. This identified hit series...
7.
Szlavik Z, Ondi L, Csekei M, Paczal A, Szabo Z, Radics G, et al.
J Med Chem
. 2019 Jul;
62(15):6913-6924.
PMID: 31339316
Myeloid cell leukemia 1 (Mcl-1), an antiapoptotic member of the Bcl-2 family of proteins, whose upregulation when observed in human cancers is associated with high tumor grade, poor survival, and...
8.
Moujalled D, Pomilio G, Ghiurau C, Ivey A, Salmon J, Rijal S, et al.
Leukemia
. 2018 Sep;
33(4):905-917.
PMID: 30214012
Improving outcomes in acute myeloid leukemia (AML) remains a major clinical challenge. Overexpression of pro-survival BCL-2 family members rendering transformed cells resistant to cytotoxic drugs is a common theme in...
9.
Casara P, Davidson J, Claperon A, Le Toumelin-Braizat G, Vogler M, Bruno A, et al.
Oncotarget
. 2018 May;
9(28):20075-20088.
PMID: 29732004
Escape from apoptosis is one of the major hallmarks of cancer cells. The B-cell Lymphoma 2 (BCL-2) gene family encodes pro-apoptotic and anti-apoptotic proteins that are key regulators of the...
10.
Merino D, Whittle J, Vaillant F, Serrano A, Gong J, Giner G, et al.
Sci Transl Med
. 2017 Aug;
9(401).
PMID: 28768804
The development of BH3 mimetics, which antagonize prosurvival proteins of the BCL-2 family, represents a potential breakthrough in cancer therapy. Targeting the prosurvival member MCL-1 has been an area of...