Browsing Molecular Pathology by author "Hoelder, Swen"
Now showing items 1-2 of 2
-
Designing Dual Inhibitors of Anaplastic Lymphoma Kinase (ALK) and Bromodomain-4 (BRD4) by Tuning Kinase Selectivity.
Watts, E; Heidenreich, D; Tucker, E; Raab, M; Strebhardt, K; et al. (AMER CHEMICAL SOC, 2019-03)Concomitant inhibition of anaplastic lymphoma kinase (ALK) and bromodomain-4 (BRD4) is a potential therapeutic strategy for targeting two key oncogenic drivers that co-segregate in a significant fraction of high-risk ... -
Novel Quinazolinone Inhibitors of ALK2 Flip between Alternate Binding Modes: Structure-Activity Relationship, Structural Characterization, Kinase Profiling, and Cellular Proof of Concept.
Hudson, L; Mui, J; Vázquez, S; Carvalho, DM; Williams, E; et al. (AMER CHEMICAL SOC, 2018-08-23)Structure-activity relationship and crystallographic data revealed that quinazolinone-containing fragments flip between two distinct modes of binding to activin receptor-like kinase-2 (ALK2). We explored both binding modes ...