Timothy P Heffron
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Explore the profile of Timothy P Heffron including associated specialties, affiliations and a list of published articles.
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36
Citations
731
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Recent Articles
11.
Chan B, Hanan E, Bowman K, Bryan M, Burdick D, Chan E, et al.
J Med Chem
. 2016 Aug;
59(19):9080-9093.
PMID: 27564586
Inhibitors targeting the activating mutants of the epidermal growth factor receptor (EGFR) have found success in the treatment of EGFR mutant positive non-small-cell lung cancer. A secondary point mutation (T790M)...
12.
Heffron T
J Med Chem
. 2016 Jul;
59(22):10030-10066.
PMID: 27414067
In addition to each of the factors that govern the identification of a successful oncology drug candidate, drug discovery aimed at treating neurological cancer must also consider the presence of...
13.
Heffron T, Ndubaku C, Salphati L, Alicke B, Cheong J, Drobnick J, et al.
ACS Med Chem Lett
. 2016 Apr;
7(4):351-6.
PMID: 27096040
Inhibition of phosphoinositide 3-kinase (PI3K) signaling is an appealing approach to treat brain tumors, especially glioblastoma multiforme (GBM). We previously disclosed our successful approach to prospectively design potent and blood-brain...
14.
Heald R, Bowman K, Bryan M, Burdick D, Chan B, Chan E, et al.
J Med Chem
. 2016 Mar;
59(6):2848.
PMID: 26967667
No abstract available.
15.
Bryan M, Burdick D, Chan B, Chen Y, Clausen S, Dotson J, et al.
ACS Med Chem Lett
. 2016 Jan;
7(1):100-4.
PMID: 26819674
The rapid advancement of a series of noncovalent inhibitors of T790M mutants of EGFR is discussed. The optimization of pyridone 1, a nonselective high-throughput screening hit, to potent molecules with...
16.
Heffron T, Heald R, Ndubaku C, Wei B, Augistin M, Do S, et al.
J Med Chem
. 2016 Jan;
59(3):985-1002.
PMID: 26741947
Inhibitors of the class I phosphoinositide 3-kinase (PI3K) isoform PI3Kα have received substantial attention for their potential use in cancer therapy. Despite the particular attraction of targeting PI3Kα, achieving selectivity...
17.
Hanan E, Baumgardner M, Bryan M, Chen Y, Eigenbrot C, Fan P, et al.
Bioorg Med Chem Lett
. 2015 Dec;
26(2):534-539.
PMID: 26639762
The treatment of epidermal growth factor receptor (EGFR)-driven non-small cell lung cancers with the T790M resistance mutation remains a significant unmet medical need. We report the identification of 4-aminoindazolyl-dihydrofuro[3,4-d]pyrimidines as...
18.
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,...
19.
Levin V, Tonge P, Gallo J, Birtwistle M, Dar A, Iavarone A, et al.
Neuro Oncol
. 2015 Sep;
17 Suppl 6:vi1-26.
PMID: 26403167
Following the first CNS Anticancer Drug Discovery and Development Conference, the speakers from the first 4 sessions and organizers of the conference created this White Paper hoping to stimulate more...
20.
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...