[HTML][HTML] Structural basis of Keap1 interactions with Nrf2

P Canning, FJ Sorrell, AN Bullock - Free Radical Biology and Medicine, 2015 - Elsevier
Keap1 is a highly redox-sensitive member of the BTB-Kelch family that assembles with the
Cul3 protein to form a Cullin–RING E3 ligase complex for the degradation of Nrf2. Oxidative …

[PDF][PDF] Family-wide structural analysis of human numb-associated protein kinases

FJ Sorrell, M Szklarz, KRA Azeez, JM Elkins, S Knapp - Structure, 2016 - cell.com
The highly diverse Numb-associated kinase (NAK) family has been linked to broad cellular
functions including receptor-mediated endocytosis, Notch pathway modulation, osteoblast …

Systematic potency and property assessment of VHL ligands and implications on PROTAC design

J Krieger, FJ Sorrell, AA Wegener, B Leuthner… - …, 2023 - Wiley Online Library
Herein, we describe a systematic SAR‐ and SPR‐investigation of the peptidomimetic
hydroxy‐proline based VHL‐ligand VH032, from which most to‐date published VHL‐targeting …

Structural complexity in the KCTD family of Cullin3-dependent E3 ubiquitin ligases

…, CE Sanvitale, JC Bufton, FJ Sorrell… - Biochemical …, 2017 - portlandpress.com
Members of the potassium channel tetramerization domain (KCTD) family are soluble non-channel
proteins that commonly function as Cullin3 (Cul3)-dependent E3 ligases. Solution …

[PDF][PDF] WNT activates the AAK1 kinase to promote clathrin-mediated endocytosis of LRP6 and establish a negative feedback loop

…, N Kapadia, S Müller, AS Santiago, FJ Sorrell… - Cell reports, 2019 - cell.com
β-Catenin-dependent WNT signal transduction governs development, tissue homeostasis,
and a vast array of human diseases. Signal propagation through a WNT-Frizzled/LRP …

Structural and biochemical characterization of the KLHL3–WNK kinase interaction important in blood pressure regulation

FR Schumacher, FJ Sorrell, DR Alessi… - Biochemical …, 2014 - portlandpress.com
WNK1 [with no lysine (K)] and WNK4 regulate blood pressure by controlling the activity of
ion co-transporters in the kidney. Groundbreaking work has revealed that the ubiquitylation …

Synthesis and Structure–Activity Relationships of 3,5-Disubstituted-pyrrolo[2,3-b]pyridines as Inhibitors of Adaptor-Associated Kinase 1 with Antiviral Activity

S Verdonck, SY Pu, FJ Sorrell, JM Elkins… - Journal of medicinal …, 2019 - ACS Publications
There are currently no approved drugs for the treatment of emerging viral infections, such as
dengue and Ebola. Adaptor-associated kinase 1 (AAK1) is a cellular serine–threonine …

Development of a differential scanning fluorimetry based high throughput screening assay for the discovery of affinity binders against an anthrax protein

FJ Sorrell, GK Greenwood, K Birchall, B Chen - Journal of pharmaceutical …, 2010 - Elsevier
The anthrax protein protective antigen (PA) is responsible for cell-surface recognition and
aids the delivery of the toxic anthrax enzymes into host cells. By targeting PA and preventing it …

Discovery of Highly Selective Inhibitors of Calmodulin-Dependent Kinases That Restore Insulin Sensitivity in the Diet-Induced Obesity in Vivo Mouse Model

…, V Novitskaya, J Morgan, FJ Sorrell… - Journal of medicinal …, 2020 - ACS Publications
Polymorphisms in the region of the calmodulin-dependent kinase isoform D (CaMK1D) gene
are associated with increased incidence of diabetes, with the most common polymorphism …

Structure–Activity Relationship Refinement and Further Assessment of Indole‐3‐glyoxylamides as a Lead Series against Prion Disease

MJ Thompson, JC Louth, S Ferrara, FJ Sorrell… - …, 2011 - Wiley Online Library
Abstract Structure–activity relationships within the indole‐3‐glyoxylamide series of antiprion
agents have been explored further, resulting in discovery of several new compounds …