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 …
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 …
human cancers, including pancreatic ductal adenocarcinoma (PDAC). While Pin1 is …
[PDF][PDF] Targeting Pin1 renders pancreatic cancer eradicable by synergizing with immunochemotherapy
Pancreatic ductal adenocarcinoma (PDAC) is characterized by notorious resistance to
current therapies attributed to inherent tumor heterogeneity and highly desmoplastic and …
current therapies attributed to inherent tumor heterogeneity and highly desmoplastic and …
[PDF][PDF] Development and characterization of a Wee1 kinase degrader
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 …
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 …
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 …
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 …
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-…
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, …
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…
promyelocytic leukemia, but their mechanisms of action and efficacy are not fully understood…