Fibroblast growth factor (FGF) and FGF receptor-mediated autocrine signaling in non-small-cell lung cancer cells

…, P Hercule, WR Helton, JE Smith, LA McDermott… - Molecular …, 2009 - ASPET
Despite widespread expression of epidermal growth factor (EGF) receptors (EGFRs) and
EGF family ligands in non-small-cell lung cancer (NSCLC), EGFR-specific tyrosine kinase …

[HTML][HTML] Novel combination of mitochondrial division inhibitor 1 (mdivi-1) and platinum agents produces synergistic pro-apoptotic effect in drug resistant tumor cells

W Qian, J Wang, V Roginskaya, LA McDermott… - Oncotarget, 2014 - ncbi.nlm.nih.gov
Overcoming platinum drug resistance represents a major clinical challenge in cancer
treatment. We discovered a novel drug combination using cisplatin and a class of …

[HTML][HTML] Characterization of the interactions of potent allosteric inhibitors with glutaminase C, a key enzyme in cancer cell glutamine metabolism

Q Huang, C Stalnecker, C Zhang, LA McDermott… - Journal of Biological …, 2018 - ASBMB
Altered glycolytic flux in cancer cells (the "Warburg effect") causes their proliferation to rely
upon elevated glutamine metabolism ("glutamine addiction"). This requirement is met by the …

Design and evaluation of novel glutaminase inhibitors

LA McDermott, P Iyer, L Vernetti, S Rimer, J Sun… - Bioorganic & medicinal …, 2016 - Elsevier
… Author links open overlay panel Lee A. McDermott a b , Prema Iyer a b , Larry Vernetti b ,
Shawn Rimer a , Jingran Sun a , Melissa Boby a , Tianyi Yang a , Michael Fioravanti a , Jason O…

[HTML][HTML] New insights into the molecular mechanisms of glutaminase C inhibitors in cancer cells using serial room temperature crystallography

…, DM Szebenyi, E Arenholz, LA McDermott… - Journal of Biological …, 2022 - ASBMB
Cancer cells frequently exhibit uncoupling of the glycolytic pathway from the TCA cycle (ie,
the "Warburg effect") and as a result, often become dependent on their ability to increase …

Screening and in vitro testing of antifolate inhibitors of human cytosolic serine hydroxymethyltransferase

…, G Montini, M Marani, A Paone, LA McDermott… - …, 2015 - Wiley Online Library
Metabolic reprogramming of tumor cells toward serine catabolism is now recognized as a
hallmark of cancer. Serine hydroxymethyltransferase (SHMT), the enzyme providing one‐…

Pharmacological optimization for successful traumatic brain injury drug development

SM Poloyac, RJ Bertz, LA McDermott… - Journal of …, 2020 - liebertpub.com
The purpose of this review is to highlight the pharmacological barrier to drug development
for traumatic brain injury (TBI) and to discuss best practice strategies to overcome such …

Development of high-content assays for kidney progenitor cell expansion in transgenic zebrafish

…, ND Goldberg, LA McDermott… - Journal of …, 2013 - journals.sagepub.com
Reactivation of genes normally expressed during organogenesis is a characteristic of
kidney regeneration. Enhancing this reactivation could potentially be a therapeutic target to …

[HTML][HTML] Characterization of allosteric modulators that disrupt androgen receptor co-activator protein-protein interactions to alter transactivation–Drug leads for …

AT Fancher, Y Hua, DA Close, W Xu, LA McDermott… - SLAS Discovery, 2023 - Elsevier
Three series of compounds were prioritized from a high content screening campaign that
identified molecules that blocked dihydrotestosterone (DHT) induced formation of Androgen …

RO4383596, an orally active KDR, FGFR, and PDGFR inhibitor: synthesis and biological evaluation

LA McDermott, M Simcox, B Higgins, T Nevins… - Bioorganic & medicinal …, 2005 - Elsevier
(±)-1-(anti-3-Hydroxy-cyclopentyl)-3-(4-methoxy-phenyl)-7-phenylamino-3,4-dihydro-1H-pyrimido[4,5-d]pyrimidin-2-one
(RO4383596) is a potent and selective inhibitor of the pro-…