Selective VPS34 inhibitor blocks autophagy and uncovers a role for NCOA4 in ferritin degradation and iron homeostasis in vivo

…, S Menon, Z Wang, A Honda, G Pardee… - Nature cell …, 2014 - nature.com
Cells rely on autophagy to clear misfolded proteins and damaged organelles to maintain
cellular homeostasis. In this study we use the new autophagy inhibitor PIK-III to screen for …

LXH254, a potent and selective ARAF-sparing inhibitor of BRAF and CRAF for the treatment of MAPK-driven tumors

…, M Jaskelioff, J Fuller, K Crawford, G Pardee… - Clinical cancer …, 2021 - AACR
Purpose: Targeting RAF for antitumor therapy in RAS-mutant tumors holds promise. Herein,
we describe in detail novel properties of the type II RAF inhibitor, LXH254. Experimental …

Baculovirus-driven protein expression in insect cells: A benchmarking study

…, A Lehner, R Lemaitre, K Nordén, G Pardee… - Journal of structural …, 2018 - Elsevier
Baculovirus-insect cell expression system has become one of the most widely used
eukaryotic expression systems for heterologous protein production in many laboratories. The …

[HTML][HTML] Structural and biophysical comparisons of the pomalidomide-and CC-220-induced interactions of SALL4 with cereblon

…, E Ornelas, D Dovala, L Tandeske, C Luu, G Pardee… - Scientific reports, 2023 - nature.com
The design of cereblon-binding molecular glues (MGs) that selectively recruit a desired
protein while excluding teratogenic SALL4 is an area of significant interest when designing …

[HTML][HTML] Inhibition of prenylated KRAS in a lipid environment

…, S Ma, A Meyer, Y Mishina, J Narberes, G Pardee… - PLoS …, 2017 - journals.plos.org
RAS mutations lead to a constitutively active oncogenic protein that signals through multiple
effector pathways. In this chemical biology study, we describe a novel coupled biochemical …

[HTML][HTML] Rationally designed PI3Kα mutants to mimic ATR and their use to understand binding specificity of ATR inhibitors

…, R Warne, R Elling, K Yan, M Doyle, G Pardee… - Journal of Molecular …, 2017 - Elsevier
ATR, a protein kinase in the PIKK family, plays a critical role in the cell DNA-damage response
and is an attractive anticancer drug target. Several potent and selective inhibitors of ATR …

Identification of Brain-Penetrant ATP-Competitive mTOR Inhibitors for CNS Syndromes

…, M Knapp, R Elling, J Fuller, G Pardee… - Journal of Medicinal …, 2023 - ACS Publications
The allosteric inhibitor of the mechanistic target of rapamycin (mTOR) everolimus reduces
seizures in tuberous sclerosis complex (TSC) patients through partial inhibition of mTOR …

In-Depth Characterization and Validation in BRG1-Mutant Lung Cancers Define Novel Catalytic Inhibitors of SWI/SNF Chromatin Remodeling

…, F Rago, S Clarkson, R Ge, F Sigoillot, G Pardee… - Biorxiv, 2019 - biorxiv.org
Members of the ATP-dependent SWI/SNF chromatin remodeling complexes are among the
most frequently mutated genes in cancer, suggesting their dysregulation plays a critical role. …

Expression, purification and characterization of inactive and active forms of ERK2 from insect expression system

K Yan, H Merritt, K Crawford, G Pardee… - Protein Expression and …, 2015 - Elsevier
Extracellular signal-regulated kinase 2 (ERK2) is a serine/threonine protein kinase involved
in many cellular programs, such as cell proliferation, differentiation, motility and programed …

Binding Rate Screen–A high-throughput assay in soluble lysate for prioritizing protein expression constructs

J Tian-Yu, S Licht, G Pardee, A Bhat, Y Cao, W Gao… - Analytical …, 2010 - Elsevier
Identification of constructs suitable for the recombinant protein production pipeline is a
bottleneck for structural genomics efforts, as most methods require purified proteins and/or are …