Sulfopin is a covalent inhibitor of Pin1 that blocks Myc-driven tumors in vivo

C Dubiella, BJ Pinch, K Koikawa, D Zaidman… - Nature chemical …, 2021 - nature.com
The peptidyl-prolyl isomerase, Pin1, is exploited in cancer to activate oncogenes and inactivate
tumor suppressors. However, despite considerable efforts, Pin1 has remained an elusive …

Identification of a potent and selective covalent Pin1 inhibitor

BJ Pinch, ZM Doctor, B Nabet, CM Browne… - Nature chemical …, 2020 - nature.com
Peptidyl-prolyl cis/trans isomerase NIMA-interacting 1 (Pin1) is commonly overexpressed in
human cancers, including pancreatic ductal adenocarcinoma (PDAC). While Pin1 is …

[PDF][PDF] Targeting Pin1 renders pancreatic cancer eradicable by synergizing with immunochemotherapy

…, S Kibe, F Suizu, N Sekino, N Kim, TD Manz, BJ Pinch… - Cell, 2021 - cell.com
Pancreatic ductal adenocarcinoma (PDAC) is characterized by notorious resistance to
current therapies attributed to inherent tumor heterogeneity and highly desmoplastic and …

[PDF][PDF] Development and characterization of a Wee1 kinase degrader

Z Li, BJ Pinch, CM Olson, KA Donovan, RP Nowak… - Cell chemical …, 2020 - cell.com
The G1/S cell cycle checkpoint is frequently dysregulated in cancer, leaving cancer cells reliant
on a functional G2/M checkpoint to prevent excessive DNA damage. Wee1 regulates the …

[PDF][PDF] A strategy to assess the cellular activity of E3 ligase components against neo-substrates using electrophilic probes

BJ Pinch, DL Buckley, S Gleim, SM Brittain… - Cell chemical …, 2022 - cell.com
While there are hundreds of predicted E3 ligases, characterizing their applications for
targeted protein degradation has proved challenging. Here, we report a chemical biology …

[HTML][HTML] A novel bifunctional alkylphenol anesthetic allows characterization of γ-aminobutyric acid, type A (GABAA), receptor subunit binding selectivity in …

KA Woll, S Murlidaran, BJ Pinch, J Hénin… - Journal of Biological …, 2016 - ASBMB
Propofol, an intravenous anesthetic, is a positive modulator of the GABA A receptor, but the
mechanistic details, including the relevant binding sites and alternative targets, remain …

[PDF][PDF] A novel bifunctional alkylphenol anesthetic allows characterization of GABAA receptor subunit binding selectivity in synaptosomes

KA Woll, S Murlidaran, BJ Pinch, J Hénin… - Journal of Biological …, 2016 - drive.google.com
Propofol, an intravenous anesthetic, is a positive modulator of the GABAA receptor, but the
mechanistic details, including the relevant binding sites and alternative targets, remain …

Sulfopin, a selective covalent inhibitor of Pin1, blocks Myc-driven tumor initiation and growth in vivo

C Dubiella, BJ Pinch, D Zaidman, TD Manz, E Poon… - bioRxiv, 2020 - biorxiv.org
The peptidyl-prolyl cis-trans isomerase, Pin1, acts as a unified signaling hub that is exploited
in cancer to activate oncogenes and inactivate tumor suppressors, in particular through up-…

A strategy to assess the cellular activity of E3 ligases against neo-substrates using electrophilic probes

BJ Pinch, DL Buckley, S Gleim, SM Brittain, L Tandeske… - BioRXiv, 2020 - biorxiv.org
Targeted protein degradation is a rapidly developing therapeutic modality that promises lower
dosing and enhanced selectivity as compared to traditional occupancy-driven inhibitors, …

[HTML][HTML] Arsenic targets Pin1 and cooperates with retinoic acid to inhibit cancer-driving pathways and tumor-initiating cells

S Kozono, YM Lin, HS Seo, B Pinch, X Lian… - Nature …, 2018 - nature.com
Arsenic trioxide (ATO) and all-trans retinoic acid (ATRA) combination safely cures fatal acute
promyelocytic leukemia, but their mechanisms of action and efficacy are not fully understood…