Covalent drug discovery: Progress against key targets, emerging strategies and lessons learnt
Abstract Covalent drug discovery is currently experiencing a boom in industrial and academic interest. To date, at least 75 covalent drugs have received regulatory approval, targeting both traditional target classes and more challenging proteins for which other approaches failed. In many cases, unique aspects of covalent targeting are essential for the
Charles P. Brown +2 more
wiley +1 more source
Distinct impact of PI(4)P flux on PI(4,5)P<sub>2</sub> steady states and oscillations. [PDF]
Xǔ XJ, Tong CS, Wu M.
europepmc +1 more source
Cardiotoxicity of BRAF/MEK inhibitors
Abstract Rapidly accelerated fibrosarcoma type B/B‐Raf proto‐oncogene, serine/threonine kinase (BRAF) and mitogen‐activated protein kinase (MEK) inhibitors have transformed outcomes in cancer therapy, particularly in melanoma. However, cardiovascular toxicities are increasingly recognized in real‐world clinical practice.
Katharina Seuthe +4 more
wiley +1 more source
Toward a molecular logic of lipid droplet heterogeneity? [PDF]
Vanni S.
europepmc +1 more source
Identification of a component of the tubulin poly-glutamylase complex required for phosphoinositide homeostasis and cilium assembly and maintenance [PDF]
Binshad Badarudeen +5 more
openalex +1 more source
Impact of incretin analogues on lipid and lipoprotein metabolism in obesity and diabetes
Abstract Incretin‐based therapies have gained momentum as a key strategy for reducing cardiovascular risk in individuals with obesity and/or type 2 diabetes (T2D). It remains unclear whether the cardiovascular benefits reflect a direct reduction in atherogenic lipoproteins—namely, low‐density lipoproteins (LDL), very low‐density lipoproteins (VLDL) and
Andrea Baragetti, Giuseppe Danilo Norata
wiley +1 more source
Metabolic control of cellular reprogramming: phospholipid remodeling tunes auxin signaling. [PDF]
Wang J, Hu D.
europepmc +1 more source
Lipid transfer proteins and PI4KIIα initiate nuclear p53-phosphoinositide signaling [PDF]
Noah D. Carrillo +8 more
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Targeting KRAS for cancer therapy
In recent years, therapeutics targeted against KRAS proto‐oncogene GTPase (KRAS)‐mutant cancers have seen significant progress. Herein we outline the biology and epidemiology of KRAS alterations at the lineage and allele levels, reviewing the clinical evidence for KRASG12C inhibition from the discovery of the recessive switch pocket to sotorasib ...
Jianlong Jia +4 more
wiley +1 more source

