[HTML][HTML] Polyphosphate coated nanoparticles: Enzyme-activated charge-reversal gene delivery systems
Aim The current study aimed to develop enzyme-activated charge-reversal lipid
nanoparticles (LNPs) as novel gene delivery systems. Methods Palmitic acid was covalently …
nanoparticles (LNPs) as novel gene delivery systems. Methods Palmitic acid was covalently …
Development and application of novel electrophilic warheads in target identification and drug discovery
Nucleophilic amino acids play important roles in maintenance of protein structure and
function, covalent modification of such amino acid residues by therapeutic agents is an …
function, covalent modification of such amino acid residues by therapeutic agents is an …
Proteome‐Wide Fragment‐Based Ligand and Target Discovery
Chemical probes are invaluable tools to investigate biological processes and can serve as
lead molecules for the development of new therapies. However, despite their utility, only a …
lead molecules for the development of new therapies. However, despite their utility, only a …
Context‐Dependence of the Reactivity of Cysteine and Lysine Residues
The S‐alkylation of Cys residues with a maleimide and the Nϵ‐acylation of Lys residues
with an N‐hydroxysuccinimide (NHS) ester are common methods for bioconjugation. Using …
with an N‐hydroxysuccinimide (NHS) ester are common methods for bioconjugation. Using …
Fluorescent cellulose nanocrystals for the detection of lead ions in complete aqueous solution
A fluorescent probe for the detection of lead ions in complete aqueous solution was
synthesized by covalently combining a fluorescent 1, 8-naphthalimide dye with cellulose …
synthesized by covalently combining a fluorescent 1, 8-naphthalimide dye with cellulose …
Novel electrophilic warhead targeting a triple-negative breast cancer driver in live cells revealed by “inverse drug discovery”
Y Fan, H Si, Z Zhang, L Zhong, H Sun… - Journal of Medicinal …, 2021 - ACS Publications
The “inverse drug discovery” strategy is a potent means of exploring the cellular targets of
latent electrophiles not typically used in medicinal chemistry. Cyclopropenone, a powerful …
latent electrophiles not typically used in medicinal chemistry. Cyclopropenone, a powerful …
Chemoproteomics-enabled covalent ligand screening reveals ALDH3A1 as a lung cancer therapy target
JL Counihan, AL Wiggenhorn, KE Anderson… - ACS chemical …, 2018 - ACS Publications
Chemical genetics is a powerful approach for identifying therapeutically active small
molecules, but identifying the mechanisms of action underlying hit compounds remains …
molecules, but identifying the mechanisms of action underlying hit compounds remains …
Cellular exposure to chloroacetanilide herbicides induces distinct protein destabilization profiles
GM Quanrud, Z Lyu, SV Balamurugan… - ACS Chemical …, 2023 - ACS Publications
Herbicides in the widely used chloroacetanilide class harbor a potent electrophilic moiety,
which can damage proteins through nucleophilic substitution. In general, damaged proteins …
which can damage proteins through nucleophilic substitution. In general, damaged proteins …
[HTML][HTML] The power of sulfhydryl groups: Thiolated lipid-based nanoparticles enhance cellular uptake of nucleic acids
D Stengel, AM Jörgensen, I Polidori, P Kapitza… - Journal of Colloid and …, 2024 - Elsevier
Aim The aim of the study was to evaluate the effect of thiolation of lipid-based nanoparticles
(LNPs) on cellular uptake of nucleic acids. Methods A thiolated surfactant was synthesized …
(LNPs) on cellular uptake of nucleic acids. Methods A thiolated surfactant was synthesized …
Targeting the ubiquitin system by fragment-based drug discovery
C Kennedy, K McPhie, K Rittinger - Frontiers in Molecular …, 2022 - frontiersin.org
The ubiquitin system contains a wealth of potential drug targets for many diseases and
conditions, including neurodegenerative, immune, metabolic and developmental diseases …
conditions, including neurodegenerative, immune, metabolic and developmental diseases …