An overview of PROTACs: a promising drug discovery paradigm
Proteolysis targeting chimeras (PROTACs) technology has emerged as a novel therapeutic
paradigm in recent years. PROTACs are heterobifunctional molecules that degrade target …
paradigm in recent years. PROTACs are heterobifunctional molecules that degrade target …
PI3K signaling in cancer: beyond AKT
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 …
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 …
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 …
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
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 …
molecular mechanisms are not well understood. Using an unbiased proteomic screen, we …
Ontogeny and Vulnerabilities of Drug-Tolerant Persisters in HER2+ Breast Cancer
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 …
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
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 …
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 …
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 …
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 …
processes. In these contexts, AKT is classically considered the de facto mediator of PI3K …