Two-photon small molecule enzymatic probes

L Qian, L Li, SQ Yao - Accounts of Chemical Research, 2016 - ACS Publications
Conspectus Enzymes are essential for life, especially in the development of disease and on
drug effects, but as we cannot yet directly observe the inside interactions and only partially …

Molecular imaging of apoptosis: the case of caspase-3 radiotracers

L Beroske, T Van den Wyngaert, S Stroobants… - International journal of …, 2021 - mdpi.com
The molecular imaging of apoptosis remains an important method for the diagnosis and
monitoring of the progression of certain diseases and the evaluation of the efficacy of …

Proteome-wide covalent ligand discovery in native biological systems

KM Backus, BE Correia, KM Lum, S Forli, BD Horning… - Nature, 2016 - nature.com
Small molecules are powerful tools for investigating protein function and can serve as leads
for new therapeutics. Most human proteins, however, lack small-molecule ligands, and …

Amlexanox-modified platinum (IV) complex triggers apoptotic and autophagic bimodal death of cancer cells

Y Guo, S Jin, D Song, T Yang, J Hu, X Hu, Q Han… - European Journal of …, 2022 - Elsevier
Platinum (IV) prodrugs c, c, t-[PtCl 2 (NH 3) 2 (OH)(amlexanox)](MAP) and c, c, t-[PtCl 2 (NH
3) 2 (amlexanox) 2](DAP) were synthesized by reacting amlexanox with oxoplatin and …

Chemoproteomics Identifies State-Dependent and Proteoform-Selective Caspase-2 Inhibitors

JO Castellón, S Ofori, NR Burton, AR Julio… - Journal of the …, 2024 - ACS Publications
Caspases are a highly conserved family of cysteine-aspartyl proteases known for their
essential roles in regulating apoptosis, inflammation, cell differentiation, and proliferation …

Small molecule active site directed tools for studying human caspases

M Poreba, A Szalek, P Kasperkiewicz, W Rut… - Chemical …, 2015 - ACS Publications
Caspases are proteases of clan CD and were described for the first time more than two
decades ago. They play critical roles in the control of regulated cell death pathways …

Design, synthesis, and anticancer evaluation of novel quinoline derivatives of ursolic acid with hydrazide, oxadiazole, and thiadiazole moieties as potent MEK …

XY Jin, H Chen, DD Li, AL Li, WY Wang… - Journal of enzyme …, 2019 - Taylor & Francis
In this article, a series of novel quinoline derivatives of ursolic acid (UA) bearing hydrazide,
oxadiazole, or thiadiazole moieties were designed, synthesised, and screened for their in …

Synthesis, inverse docking-assisted identification and in vitro biological characterization of Flavonol-based analogs of fisetin as c-Kit, CDK2 and mTOR inhibitors …

T Roy, ST Boateng, S Banang-Mbeumi, PK Singh… - Bioorganic …, 2021 - Elsevier
Due to hurdles, including resistance, adverse effects, and poor bioavailability, among others
linked with existing therapies, there is an urgent unmet need to devise new, safe, and more …

Cyclodextrin-based peptide self-assemblies (Spds) that enhance peptide-based fluorescence imaging and antimicrobial efficacy

JB Jiao, GZ Wang, XL Hu, Y Zang… - Journal of the …, 2019 - ACS Publications
As a result of their high specificity for their corresponding biological targets, peptides have
shown significant potential in a range of diagnostic and therapeutic applications. However …

Emerging challenges in the design of selective substrates, inhibitors and activity‐based probes for indistinguishable proteases

P Kasperkiewicz, M Poreba, K Groborz… - The FEBS …, 2017 - Wiley Online Library
Proteases are enzymes that hydrolyze the peptide bond of peptide substrates and proteins.
Despite significant progress in recent years, one of the greatest challenges in the design …