Overview of recent strategic advances in medicinal chemistry

G Wu, T Zhao, D Kang, J Zhang, Y Song… - Journal of medicinal …, 2019 - ACS Publications
Introducing novel strategies, concepts, and technologies that speed up drug discovery and
the drug development cycle is of great importance both in the highly competitive …

Pharmacological targeting of IRE1 in cancer

DP Raymundo, D Doultsinos, X Guillory, A Carlesso… - Trends in cancer, 2020 - cell.com
IRE1α (inositol requiring enzyme 1 alpha) is one of the main transducers of the unfolded
protein response (UPR). IRE1α plays instrumental protumoral roles in several cancers, and …

Targeting ribonucleases with small molecules and bifunctional molecules

L Borgelt, P Wu - ACS Chemical Biology, 2023 - ACS Publications
Ribonucleases (RNases) cleave and process RNAs, thereby regulating the biogenesis,
metabolism, and degradation of coding and noncoding RNAs. Thus, small molecules …

Inhibition of FLT3-ITD Kinase in Acute Myeloid Leukemia by New Imidazo[1,2-b]pyridazine Derivatives Identified by Scaffold Hopping

P Brehova, E Řezníčková, K Skach… - Journal of Medicinal …, 2023 - ACS Publications
FLT3 kinase is a potential drug target in acute myeloid leukemia (AML). Patients with FLT3
mutations typically have higher relapse rates and worse outcomes than patients without …

Recent contributions of pyridazine as a privileged scaffold of anticancer agents in medicinal chemistry: An updated review

ZQ Liu, Q Zhang, YL Liu, XQ Yu, RH Chui… - Bioorganic & Medicinal …, 2024 - Elsevier
Pyridazine, as a privileged scaffold, has been extensively utilized in drug development due
to its multiple biological activities. Especially around its distinctive anticancer property, a …

Dual RNase activity of IRE1 as a target for anticancer therapies

S Bartoszewska, J Sławski, JF Collawn… - Journal of Cell …, 2023 - Springer
The unfolded protein response (UPR) is a cellular mechanism that protects cells during
stress conditions in which there is an accumulation of misfolded proteins in the endoplasmic …

[PDF][PDF] Chemical chaperones to inhibit endoplasmic reticulum stress: implications in diseases

JH Jeon, S Im, HS Kim, D Lee, K Jeong… - Drug Design …, 2022 - Taylor & Francis
The endoplasmic reticulum (ER) is responsible for structural transformation or folding of de
novo proteins for transport to the Golgi. When the folding capacity of the ER is exceeded or …

The functions of IRE1α in neurodegenerative diseases: beyond ER stress

L Chen, M Bi, Z Zhang, X Du, X Chen, Q Jiao… - Ageing research …, 2022 - Elsevier
Inositol-requiring enzyme 1 α (IRE1α) is a type I transmembrane protein that resides in the
endoplasmic reticulum (ER). IRE1α, which is the primary sensor of ER stress, has been …

HEPN RNases–an emerging class of functionally distinct RNA processing and degradation enzymes

MC Pillon, J Gordon, MN Frazier… - Critical reviews in …, 2021 - Taylor & Francis
Abstract HEPN (Higher Eukaryotes and Prokaryotes Nucleotide-binding) RNases are an
emerging class of functionally diverse RNA processing and degradation enzymes. Members …

Conformational heterogeneity of the BTK PHTH domain drives multiple regulatory states

DY Lin, LE Kueffer, P Juneja, TE Wales, JR Engen… - Elife, 2024 - elifesciences.org
Full-length Bruton's tyrosine kinase (BTK) has been refractory to structural analysis. The
nearest full-length structure of BTK to date consists of the autoinhibited SH3–SH2–kinase …