PROTACs: great opportunities for academia and industry (an update from 2020 to 2021)

M He, C Cao, Z Ni, Y Liu, P Song, S Hao, Y He… - … and Targeted Therapy, 2022 - nature.com
Abstract PROteolysis TArgeting Chimeras (PROTACs) technology is a new protein-
degradation strategy that has emerged in recent years. It uses bifunctional small molecules …

Recent advances in targeting the “undruggable” proteins: from drug discovery to clinical trials

X Xie, T Yu, X Li, N Zhang, LJ Foster, C Peng… - Signal transduction and …, 2023 - nature.com
Undruggable proteins are a class of proteins that are often characterized by large, complex
structures or functions that are difficult to interfere with using conventional drug design …

Emerging mechanistic understanding of cilia function in cellular signalling

KI Hilgendorf, BR Myers, JF Reiter - Nature Reviews Molecular Cell …, 2024 - nature.com
Primary cilia are solitary, immotile sensory organelles present on most cells in the body that
participate broadly in human health, physiology and disease. Cilia generate a unique …

Establishing and regulating the composition of cilia for signal transduction

MV Nachury, DU Mick - Nature reviews Molecular cell biology, 2019 - nature.com
The primary cilium is a hair-like surface-exposed organelle of the eukaryotic cell that
decodes a variety of signals—such as odorants, light and Hedgehog morphogens—by …

NBD-based synthetic probes for sensing small molecules and proteins: design, sensing mechanisms and biological applications

C Jiang, H Huang, X Kang, L Yang, Z Xi… - Chemical Society …, 2021 - pubs.rsc.org
Compounds with a nitrobenzoxadiazole (NBD) skeleton exhibit prominent useful properties
including environmental sensitivity, high reactivity toward amines and biothiols (including …

Protein lipidation: occurrence, mechanisms, biological functions, and enabling technologies

H Jiang, X Zhang, X Chen, P Aramsangtienchai… - Chemical …, 2018 - ACS Publications
Protein lipidation, including cysteine prenylation, N-terminal glycine myristoylation, cysteine
palmitoylation, and serine and lysine fatty acylation, occurs in many proteins in eukaryotic …

Protein prenylation: unique fats make their mark on biology

M Wang, PJ Casey - Nature reviews Molecular cell biology, 2016 - nature.com
The modification of eukaryotic proteins by isoprenoid lipids, which is known as prenylation,
controls the localization and activity of a range of proteins that have crucial functions in …

Regulation of small gtpases by gefs, gaps, and gdis

J Cherfils, M Zeghouf - Physiological reviews, 2013 - journals.physiology.org
Small GTPases use GDP/GTP alternation to actuate a variety of functional switches that are
pivotal for cell dynamics. The GTPase switch is turned on by GEFs, which stimulate …

ARF GTPases and their GEFs and GAPs: concepts and challenges

E Sztul, PW Chen, JE Casanova… - Molecular biology of …, 2019 - Am Soc Cell Biol
Detailed structural, biochemical, cell biological, and genetic studies of any gene/protein are
required to develop models of its actions in cells. Studying a protein family in the aggregate …

Small molecule inhibition of the KRAS–PDEδ interaction impairs oncogenic KRAS signalling

G Zimmermann, B Papke, S Ismail, N Vartak… - Nature, 2013 - nature.com
The KRAS oncogene product is considered a major target in anticancer drug discovery,,.
However, direct interference with KRAS signalling has not yet led to clinically useful …