Procaspase-3 overexpression in cancer: a paradoxical observation with therapeutic potential

MW Boudreau, J Peh, PJ Hergenrother - ACS chemical biology, 2019 - ACS Publications
Many anticancer strategies rely on the promotion of apoptosis in cancer cells as a means to
shrink tumors. Crucial for apoptotic function are executioner caspases, most notably …

Zinc deficiency causes neural tube defects through attenuation of p53 ubiquitylation

H Li, J Zhang, L Niswander - Development, 2018 - journals.biologists.com
Micronutrition is essential for neural tube closure, and zinc deficiency is associated with
human neural tube defects. Here, we modeled zinc deficiency in mouse embryos, and used …

Synthesis and preclinical evaluation of TPA-based zinc chelators as metallo-β-lactamase inhibitors

C Schnaars, G Kildahl-Andersen… - ACS Infectious …, 2018 - ACS Publications
The rise of antimicrobial resistance (AMR) worldwide and the increasing spread of multi-
drug-resistant organisms expressing metallo-β-lactamases (MBL) require the development …

Procaspase-3-activating compound 1 stabilizes hypoxia-inducible factor 1α and induces DNA damage by sequestering ferrous iron

F Li, A Wei, L Bu, L Long, W Chen, C Wang… - Cell death & …, 2018 - nature.com
Abstract Procaspase-3-activating compound 1 (PAC-1) induces procaspase-3 activation via
zinc chelation. However, whether PAC-1 employs other mechanisms remains unknown …

Derivatives of procaspase-activating compound 1 (PAC-1) and their anticancer activities

HS Roth, PJ Hergenrother - Current medicinal chemistry, 2016 - ingentaconnect.com
PAC-1 induces the activation of procaspase-3 in vitro and in cell culture by chelation of
inhibitory labile zinc ions via its ortho-hydroxy-N-acylhydrazone moiety. First reported in …

Removal of metabolic liabilities enables development of derivatives of procaspase-activating compound 1 (PAC-1) with improved pharmacokinetics

HS Roth, RC Botham, SC Schmid, TM Fan… - Journal of medicinal …, 2015 - ACS Publications
Procaspase-activating compound 1 (PAC-1) is an o-hydroxy-N-acylhydrazone that induces
apoptosis in cancer cells by chelation of labile inhibitory zinc from procaspase-3. PAC-1 has …

Synthesis and biological evaluation of new dipicolylamine zinc chelators as metallo-β-lactamase inhibitors

A Prandina, S Radix, M Le Borgne, LP Jordheim… - Tetrahedron, 2019 - Elsevier
Antibiotics are key drugs in modern healthcare, especially in hospitals, where multiresistant
bacteria resides and is a potential threat to human health. In the present work, a new series …

Targeting procaspase‐3 with WF‐208, a novel PAC‐1 derivative, causes selective cancer cell apoptosis

F Wang, Y Liu, L Wang, J Yang, Y Zhao… - Journal of Cellular …, 2015 - Wiley Online Library
Caspase‐3 is a critical effector caspase in apoptosis cascade, and is often over‐expressed
in many cancer tissues. The first synthesized procaspase‐3 activator, PAC‐1, induces …

Toward a rational design of polyamine-based zinc-chelating agents for cancer therapies

C Galiana-Rosello, C Aceves-Luquero… - Journal of Medicinal …, 2020 - ACS Publications
In vitro viability assays against a representative panel of human cancer cell lines revealed
that polyamines L1a and L5a displayed remarkable activity with IC50 values in the …

SM-1, a novel PAC-1 derivative, activates procaspase-3 and causes cancer cell apoptosis

Y Chen, M Sun, J Ding, Q Zhu - Cancer chemotherapy and pharmacology, 2016 - Springer
Purpose To develop more potent procaspase-3 activator, 7 novel derivatives of PAC-1 were
synthesized and evaluated. Among them, SM-1 stood out for its promising activity and good …