Expanding the Reach of Precision Oncology by Drugging All KRAS Mutants

MH Hofmann, D Gerlach, S Misale, M Petronczki… - Cancer Discovery, 2022 - AACR
KRAS is the most frequently mutated oncogene, harboring mutations in approximately one
in seven cancers. Allele-specific KRASG12C inhibitors are currently changing the treatment …

[HTML][HTML] Emerging degrader technologies engaging lysosomal pathways

Y Ding, D Xing, Y Fei, B Lu - Chemical Society Reviews, 2022 - pubs.rsc.org
Targeted protein degradation (TPD) provides unprecedented opportunities for drug
discovery. While the proteolysis-targeting chimera (PROTAC) technology has already …

Chemically engineering cells for precision medicine

Y Wang, Z Li, F Mo, TJ Chen-Mayfield, A Saini… - Chemical Society …, 2023 - pubs.rsc.org
Cell-based therapy holds great potential to address unmet medical needs and revolutionize
the healthcare industry, as demonstrated by several therapeutics such as CAR-T cell …

Liquid-liquid phase separation of α-synuclein: a new mechanistic insight for α-synuclein aggregation associated with Parkinson's disease pathogenesis

S Mukherjee, A Sakunthala, L Gadhe… - Journal of molecular …, 2023 - Elsevier
Aberrant aggregation of the misfolded presynaptic protein, α-Synuclein (α-Syn) into Lewy
body (LB) and Lewy neuritis (LN) is a major pathological hallmark of Parkinson's disease …

[HTML][HTML] 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 …

Protein posttranslational modifications in health and diseases: Functions, regulatory mechanisms, and therapeutic implications

Q Zhong, X Xiao, Y Qiu, Z Xu, C Chen, B Chong… - MedComm, 2023 - Wiley Online Library
Protein posttranslational modifications (PTMs) refer to the breaking or generation of covalent
bonds on the backbones or amino acid side chains of proteins and expand the diversity of …

[HTML][HTML] The race to develop oral SERDs and other novel estrogen receptor inhibitors: recent clinical trial results and impact on treatment options

Y Wang, SC Tang - Cancer and Metastasis Reviews, 2022 - Springer
Hormonal therapy plays a vital part in the treatment of estrogen receptor–positive (ER+)
breast cancer. ER can be activated in a ligand-dependent and independent manner …

Proximity-inducing modalities: the past, present, and future

S Singh, W Tian, ZC Severance… - Chemical Society …, 2023 - pubs.rsc.org
Living systems use proximity to regulate biochemical processes. Inspired by this
phenomenon, bifunctional modalities that induce proximity have been developed to redirect …

[HTML][HTML] Protein degradation technology: a strategic paradigm shift in drug discovery

H Li, J Dong, M Cai, Z Xu, XD Cheng, JJ Qin - Journal of Hematology & …, 2021 - Springer
Targeting pathogenic proteins with small-molecule inhibitors (SMIs) has become a widely
used strategy for treating malignant tumors. However, most intracellular proteins have been …

[HTML][HTML] Targeting protein modifications in metabolic diseases: molecular mechanisms and targeted therapies

X Wu, M Xu, M Geng, S Chen, PJ Little, S Xu… - Signal transduction and …, 2023 - nature.com
The ever-increasing prevalence of noncommunicable diseases (NCDs) represents a major
public health burden worldwide. The most common form of NCD is metabolic diseases …