Emerging and Re-emerging Warheads for Targeted Covalent Inhibitors: An Update

L Hillebrand, XJ Liang, RAM Serafim… - Journal of Medicinal …, 2024 - ACS Publications
Covalent inhibitors and other types of covalent modalities have seen a revival in the past two
decades, with a variety of new targeted covalent drugs having been approved in recent …

Technologies for Direct Detection of Covalent Protein–Drug Adducts

E Mons, RQ Kim, MPC Mulder - Pharmaceuticals, 2023 - mdpi.com
In the past two decades, drug candidates with a covalent binding mode have gained the
interest of medicinal chemists, as several covalent anticancer drugs have successfully …

Targeting the Labile Iron Pool with Engineered DFO Nanosheets to Inhibit Ferroptosis for Parkinson's Disease Therapy

L Lei, J Yuan, Z Dai, S Xiang, Q Tu, X Cui… - Advanced …, 2024 - Wiley Online Library
Ferroptosis in neurons is considered one of the key factors that induces Parkinson's disease
(PD), which is caused by excessive iron accumulation in the intracellular labile iron pool …

Cannabidiol Protects Dopaminergic-like Neurons against Paraquat- and Maneb-Induced Cell Death through Safeguarding DJ-1CYS106 and Caspase 3 …

M Mendivil-Perez, AA Felizardo-Otalvaro… - ACS Chemical …, 2023 - ACS Publications
Parkinson's disease (PD), a progressive neurodegenerative movement disorder, has
reached pandemic status worldwide. This neurologic disorder is caused primarily by the …

N‐Cyanopiperazines as Specific Covalent Inhibitors of the Deubiquitinating Enzyme UCHL1

M Schmidt, C Grethe, S Recknagel… - Angewandte Chemie …, 2024 - Wiley Online Library
Cyanamides have emerged as privileged scaffolds in covalent inhibitors of deubiquitinating
enzymes (DUBs). However, many compounds with a cyanopyrrolidine warhead show cross …

Profiling nuclear cysteine ligandability and effects on nuclear localization using proximity labeling-coupled chemoproteomics

Q Peng, E Weerapana - Cell Chemical Biology, 2024 - cell.com
The nucleus controls cell growth and division through coordinated interactions between
nuclear proteins and chromatin. Mutations that impair nuclear protein association with …

Development of Inhibitors, Probes, and PROTAC Provides a Complete Toolbox to Study PARK7 in the Living Cell

Y Jia, M Oyken, RQ Kim, RTN Tjokrodirijo… - Journal of Medicinal …, 2024 - ACS Publications
The integration of diverse chemical tools like small-molecule inhibitors, activity-based
probes (ABPs), and proteolysis targeting chimeras (PROTACs) advances clinical drug …

Practical Three-Component Regioselective Synthesis of Drug-Like 3-Aryl(or heteroaryl)-5,6-dihydrobenzo[h]cinnolines as Potential Non-Covalent Multi-Targeting …

H Mousavi, M Rimaz, B Zeynizadeh - ACS Chemical …, 2024 - ACS Publications
Neurodegenerative diseases (NDs) are one of the prominent health challenges facing
contemporary society, and many efforts have been made to overcome and (or) control it. In …

Identification of DOT1L inhibitor in a screen for factors that promote dopaminergic neuron survival

J Cui, J Carey, RA Reijo Pera - Frontiers in Aging Neuroscience, 2022 - frontiersin.org
Parkinson's disease (PD) is a common neurodegenerative disorder characterized by the
progressive loss of dopaminergic (DA) neurons in the substantia nigra region of the …

[HTML][HTML] Celastrus orbiculatus Thunb. extract targeting DJ-1 inhibits non-small cell lung cancer invasion and metastasis through mitochondrial-induced ROS …

X Ni, S Yu, X Jiang, F Wu, J Zhou, D Mao… - Journal of …, 2024 - Elsevier
Abstract Ethnopharmacological relevance Celastrus orbiculatus Thunb. is an ancient
traditional Chinese herb with a long history of medicinal use. The ethyl acetate extract of …