John Lesnick
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Explore the profile of John Lesnick including associated specialties, affiliations and a list of published articles.
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Articles
12
Citations
164
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Recent Articles
1.
Miniaturization of High-Throughput Epigenetic Methyltransferase Assays with Acoustic Liquid Handling
Edwards B, Lesnick J, Wang J, Tang N, Peters C
J Lab Autom
. 2015 Oct;
21(1):208-16.
PMID: 26450876
Epigenetics continues to emerge as an important target class for drug discovery and cancer research. As programs scale to evaluate many new targets related to epigenetic expression, new tools and...
2.
Pei Z, Blackwood E, Liu L, Malek S, Belvin M, Koehler M, et al.
ACS Med Chem Lett
. 2014 Jun;
4(1):103-7.
PMID: 24900569
Aberrant activation of the PI3K-Akt-mTOR signaling pathway has been observed in human tumors and tumor cell lines, indicating that these protein kinases may be attractive therapeutic targets for treating cancer....
3.
Staben S, Ndubaku C, Blaquiere N, Belvin M, Bull R, Dudley D, et al.
Bioorg Med Chem Lett
. 2013 Apr;
23(9):2606-13.
PMID: 23540645
A series of suitable five-membered heterocyclic alternatives to thiophenes within a thienobenzoxepin class of PI3-kinase (PI3K) inhibitors was discovered. Specific thiazolobenzoxepin 8-substitution was identified that increased selectivity over PI3Kβ. PI3Kβ-sparing...
4.
Staben S, Blaquiere N, Tsui V, Kolesnikov A, Do S, Bradley E, et al.
Bioorg Med Chem Lett
. 2012 Dec;
23(3):897-901.
PMID: 23265894
Substructural class effects surrounding replacement of a 'cis' N-methyl aniline amide within potent and selective thienobenzoxepin PI3-kinase inhibitors are disclosed. While a simple aryl to alkyl switch was not tolerated...
5.
Murray J, Sweeney Z, Chan B, Balazs M, Bradley E, Castanedo G, et al.
J Med Chem
. 2012 Aug;
55(17):7686-95.
PMID: 22877085
Inhibition of PI3Kδ is considered to be an attractive mechanism for the treatment of inflammatory diseases and leukocyte malignancies. Using a structure-based design approach, we have identified a series of...
6.
Sutherlin D, Baker S, Bisconte A, Blaney P, Brown A, Chan B, et al.
Bioorg Med Chem Lett
. 2012 Jun;
22(13):4296-302.
PMID: 22672799
A potent inhibitor of PI3Kδ that is ≥ 200 fold selective for the remaining three Class I PI3K isoforms and additional kinases is described. The hypothesis for selectivity is illustrated...
7.
Safina B, Baker S, Baumgardner M, Blaney P, Chan B, Chen Y, et al.
J Med Chem
. 2012 May;
55(12):5887-900.
PMID: 22626259
PI3Kδ is a lipid kinase and a member of a larger family of enzymes, PI3K class IA(α, β, δ) and IB (γ), which catalyze the phosphorylation of PIP2 to PIP3....
8.
Heffron T, Wei B, Olivero A, Staben S, Tsui V, Do S, et al.
J Med Chem
. 2011 Oct;
54(22):7815-33.
PMID: 21985639
Of the four class I phosphoinositide 3-kinase (PI3K) isoforms, PI3Kα has justly received the most attention for its potential in cancer therapy. Herein we report our successful approaches to achieve...
9.
Sutherlin D, Bao L, Berry M, Castanedo G, Chuckowree I, Dotson J, et al.
J Med Chem
. 2011 Oct;
54(21):7579-87.
PMID: 21981714
The discovery of 2 (GDC-0980), a class I PI3K and mTOR kinase inhibitor for oncology indications, is described. mTOR inhibition was added to the class I PI3K inhibitor 1 (GDC-0941)...
10.
Staben S, Siu M, Goldsmith R, Olivero A, Do S, Burdick D, et al.
Bioorg Med Chem Lett
. 2011 Jun;
21(13):4054-8.
PMID: 21636270
Starting from thienobenzopyran HTS hit 1, co-crystallization, molecular modeling and metabolic analysis were used to design potent and metabolically stable inhibitors of PI3-kinase. Compound 15 demonstrated PI3K pathway suppression in...