An overview of PROTACs: a promising drug discovery paradigm

Z Liu, M Hu, Y Yang, C Du, H Zhou, C Liu, Y Chen… - Molecular …, 2022 - Springer
Proteolysis targeting chimeras (PROTACs) technology has emerged as a novel therapeutic
paradigm in recent years. PROTACs are heterobifunctional molecules that degrade target …

PI3K signaling in cancer: beyond AKT

EC Lien, CC Dibble, A Toker - Current opinion in cell biology, 2017 - Elsevier
The phosphoinositide 3-kinase (PI3K) signaling pathway is one of the most frequently
altered pathways in human cancer and has a critical role in driving tumor initiation and …

Synthesis of sulfonamide and their synthetic and therapeutic applications: Recent advances

S Mondal, S Malakar - Tetrahedron, 2020 - Elsevier
A sulfonamide is a functional group that is the basis of several sulfa drugs and thereby are
very much important scaffolds in medicinal as well as in synthetic organic chemistry …

PROTACs to address the challenges facing small molecule inhibitors

P Martín-Acosta, X Xiao - European journal of medicinal chemistry, 2021 - Elsevier
Small molecule inhibitors of proteins represent important medicines and critical chemical
tools to investigate the biology of the target proteins. Advances in various-omics …

mTORC2 regulates amino acid metabolism in cancer by phosphorylation of the cystine-glutamate antiporter xCT

Y Gu, CP Albuquerque, D Braas, W Zhang, GR Villa… - Molecular cell, 2017 - cell.com
Mutations in cancer reprogram amino acid metabolism to drive tumor growth, but the
molecular mechanisms are not well understood. Using an unbiased proteomic screen, we …

Ontogeny and Vulnerabilities of Drug-Tolerant Persisters in HER2+ Breast Cancer

CA Chang, J Jen, S Jiang, A Sayad, AS Mer, KR Brown… - Cancer discovery, 2022 - AACR
Resistance to targeted therapies is an important clinical problem in HER2-positive (HER2+)
breast cancer.“Drug-tolerant persisters”(DTP), a subpopulation of cancer cells that survive …

PDK1-SGK1 signaling sustains AKT-independent mTORC1 activation and confers resistance to PI3Kα inhibition

P Castel, H Ellis, R Bago, E Toska, P Razavi… - Cancer cell, 2016 - cell.com
PIK3CA, which encodes the p110α subunit of PI3K, is frequently mutated and oncogenic in
breast cancer. PI3Kα inhibitors are in clinical development and despite promising early …

Design and characterization of SGK3-PROTAC1, an isoform specific SGK3 kinase PROTAC degrader

H Tovell, A Testa, H Zhou, N Shpiro… - ACS Chemical …, 2019 - ACS Publications
SGK3 is a PX domain containing protein kinase activated at endosomes downstream of
class 1 and 3 PI3K family members by growth factors and oncogenic mutations. SGK3 plays …

Rapid and reversible knockdown of endogenously tagged endosomal proteins via an optimized HaloPROTAC degrader

H Tovell, A Testa, C Maniaci, H Zhou… - ACS chemical …, 2019 - ACS Publications
Inducing post-translational protein knockdown is an important approach to probe biology
and validate drug targets. An efficient strategy to achieve this involves expression of a …

SGK1: the dark side of PI3K signaling

A Di Cristofano - Current topics in developmental biology, 2017 - Elsevier
Activation of the PI3K pathway is central to a variety of physiological and pathological
processes. In these contexts, AKT is classically considered the de facto mediator of PI3K …