Peter Kovar
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Explore the profile of Peter Kovar including associated specialties, affiliations and a list of published articles.
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32
Citations
542
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Recent Articles
1.
Kovar P, Richardson P, Korepanova A, Afanador G, Stojkovic V, Li T, et al.
SLAS Discov
. 2024 Aug;
29(6):100179.
PMID: 39151824
The SARS-CoV-2 main protease (Mpro) is essential for viral replication because it is responsible for the processing of most of the non-structural proteins encoded by the virus. Inhibition of Mpro...
2.
Wang L, Doherty G, Judd A, Tao Z, Hansen T, Frey R, et al.
ACS Med Chem Lett
. 2020 Oct;
11(10):1829-1836.
PMID: 33062160
Herein we describe the discovery of A-1331852, a first-in-class orally active BCL-X inhibitor that selectively and potently induces apoptosis in BCL-X-dependent tumor cells. This molecule was generated by re-engineering our...
3.
Fidanze S, Liu D, Mantei R, Hasvold L, Pratt J, Sheppard G, et al.
Bioorg Med Chem Lett
. 2018 Apr;
28(10):1804-1810.
PMID: 29678460
Novel conformationally constrained BET bromodomain inhibitors have been developed. These inhibitors were optimized in two similar, yet distinct chemical series, the 6-methyl-1H-pyrrolo[2,3-c]pyridin-7(6H)-ones (A) and the 1-methyl-1H-pyrrolo[2,3-c]pyridin-7(6H)-ones (B). Each series demonstrated...
4.
Wang L, Pratt J, Soltwedel T, Sheppard G, Fidanze S, Liu D, et al.
J Med Chem
. 2017 Apr;
60(9):3828-3850.
PMID: 28368119
Members of the BET family of bromodomain containing proteins have been identified as potential targets for blocking proliferation in a variety of cancer cell lines. A two-dimensional NMR fragment screen...
5.
Hasvold L, Sheppard G, Wang L, Fidanze S, Liu D, Pratt J, et al.
Bioorg Med Chem Lett
. 2017 Mar;
27(10):2225-2233.
PMID: 28268136
An NMR fragment screen for binders to the bromodomains of BRD4 identified 2-methyl-3-ketopyrroles 1 and 2. Elaboration of these fragments guided by structure-based design provided lead molecules with significant activity...
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7.
Gullich A, Kovar P, Zart S, Reimann A
J Sports Sci
. 2016 Mar;
35(3):207-215.
PMID: 27018979
This study examined contributions of different types of sport activities to the development of elite youth soccer performance. Match-play performance of 44 German male players was assessed by expert coaches...
8.
Leverson J, Phillips D, Mitten M, Boghaert E, Diaz D, Tahir S, et al.
Sci Transl Med
. 2015 Mar;
7(279):279ra40.
PMID: 25787766
The BCL-2/BCL-XL/BCL-W inhibitor ABT-263 (navitoclax) has shown promising clinical activity in lymphoid malignancies such as chronic lymphocytic leukemia. However, its efficacy in these settings is limited by thrombocytopenia caused by...
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10.
Akritopoulou-Zanze I, Wakefield B, Gasiecki A, Kalvin D, Johnson E, Kovar P, et al.
Bioorg Med Chem Lett
. 2011 Feb;
21(5):1480-3.
PMID: 21288717
We report the synthesis and biological evaluation of 5-substituted indazoles as kinase inhibitors. The compounds were synthesized in a parallel synthesis fashion from readily available starting materials employing heterocycle forming...