Steve Sideris
Overview
Explore the profile of Steve Sideris including associated specialties, affiliations and a list of published articles.
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35
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1512
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Recent Articles
11.
Heald R, Bowman K, Bryan M, Burdick D, Chan B, Chan E, et al.
J Med Chem
. 2015 Oct;
58(22):8877-95.
PMID: 26455919
Because of their increased activity against activating mutants, first-generation epidermal growth factor receptor (EGFR) kinase inhibitors have had remarkable success in treating non-small-cell lung cancer (NSCLC) patients, but acquired resistance,...
12.
Fauber B, Dragovich P, Chen J, Corson L, Ding C, Eigenbrot C, et al.
Bioorg Med Chem Lett
. 2014 Dec;
24(24):5683-5687.
PMID: 25467161
A series of 3,6-disubstituted dihydropyrones were identified as inhibitors of human lactate dehydrogenase (LDH)-A. Structure activity relationships were explored and a series of 6,6-spiro analogs led to improvements in LDHA...
13.
Gazzard L, Appleton B, Chapman K, Chen H, Clark K, Drobnick J, et al.
Bioorg Med Chem Lett
. 2014 Dec;
24(24):5704-5709.
PMID: 25453805
Checkpoint kinase 1 (ChK1) is activated in response to DNA damage, acting to temporarily block cell cycle progression and allow for DNA repair. It is envisaged that inhibition of ChK1...
14.
Hanan E, Eigenbrot C, Bryan M, Burdick D, Chan B, Chen Y, et al.
J Med Chem
. 2014 Nov;
57(23):10176-91.
PMID: 25383627
Activating mutations within the epidermal growth factor receptor (EGFR) kinase domain, commonly L858R or deletions within exon 19, increase EGFR-driven cell proliferation and survival and are correlated with impressive responses...
15.
Haling J, Sudhamsu J, Yen I, Sideris S, Sandoval W, Phung W, et al.
Cancer Cell
. 2014 Aug;
26(3):402-413.
PMID: 25155755
Numerous oncogenic mutations occur within the BRAF kinase domain (BRAF(KD)). Here we show that stable BRAF-MEK1 complexes are enriched in BRAF(WT) and KRAS mutant (MT) cells but not in BRAF(MT)...
16.
Dragovich P, Fauber B, Boggs J, Chen J, Corson L, Ding C, et al.
Bioorg Med Chem Lett
. 2014 Jul;
24(16):3764-71.
PMID: 25037916
A novel class of 3-hydroxy-2-mercaptocyclohex-2-enone-containing inhibitors of human lactate dehydrogenase (LDH) was identified through a high-throughput screening approach. Biochemical and surface plasmon resonance experiments performed with a screening hit (LDHA...
17.
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....
18.
Fauber B, Dragovich P, Chen J, Corson L, Ding C, Eigenbrot C, et al.
Bioorg Med Chem Lett
. 2013 Sep;
23(20):5533-9.
PMID: 24012183
A 2-amino-5-aryl-pyrazine was identified as an inhibitor of human lactate dehydrogenase A (LDHA) via a biochemical screening campaign. Biochemical and biophysical experiments demonstrated that the compound specifically interacted with human...
19.
Lee W, Ortwine D, Bergeron P, Lau K, Lin L, Malek S, et al.
Bioorg Med Chem Lett
. 2013 Aug;
23(18):5097-104.
PMID: 23932790
A series of N-7-methyl-imidazolopyrimidine inhibitors of the mTOR kinase have been designed and prepared, based on the hypothesis that the N-7-methyl substituent on imidazolopyrimidine would impart selectivity for mTOR over...
20.
Ndubaku C, Heffron T, Staben S, Baumgardner M, Blaquiere N, Bradley E, et al.
J Med Chem
. 2013 May;
56(11):4597-610.
PMID: 23662903
Dysfunctional signaling through the phosphoinositide 3-kinase (PI3K)/AKT/mTOR pathway leads to uncontrolled tumor proliferation. In the course of the discovery of novel benzoxepin PI3K inhibitors, we observed a strong dependency of...