[PDF][PDF] Mapping the degradable kinome provides a resource for expedited degrader development
Targeted protein degradation (TPD) refers to the use of small molecules to induce ubiquitin-dependent
degradation of proteins. TPD is of interest in drug development, as it can address …
degradation of proteins. TPD is of interest in drug development, as it can address …
[PDF][PDF] Targeting Pin1 renders pancreatic cancer eradicable by synergizing with immunochemotherapy
…, N Sekino, N Kim, TD Manz, BJ Pinch, D Akshinthala… - 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 …
current therapies attributed to inherent tumor heterogeneity and highly desmoplastic and …
Sulfopin is a covalent inhibitor of Pin1 that blocks Myc-driven tumors in vivo
…, K Koikawa, D Zaidman, E Poon, TD Manz… - 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
…, X Lian, TD Manz, Y Chun, S Kibe, D Zaidman… - 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 the PI5P4K lipid kinase family in cancer using covalent inhibitors
…, CM Browne, HS Seo, MN Paddock, TD Manz… - Cell chemical …, 2020 - cell.com
The PI5P4Ks have been demonstrated to be important for cancer cell proliferation and other
diseases. However, the therapeutic potential of targeting these kinases is understudied due …
diseases. However, the therapeutic potential of targeting these kinases is understudied due …
Development of potent and selective degraders of PI5P4Kγ
Phosphatidylinositol 5-phosphate 4-kinases (PI5P4Ks), a family of three members in mammals
(α, β and γ), have emerged as potential therapeutic targets due to their role in regulating …
(α, β and γ), have emerged as potential therapeutic targets due to their role in regulating …
Targeting the Dark Lipid Kinase PIP4K2C with a Potent and Selective Binder and Degrader
Phosphatidylinositol 5‐phosphate 4‐kinase, type II, gamma (PIP4K2C) remains a poorly
understood lipid kinase with minimal enzymatic activity but potential scaffolding roles in immune …
understood lipid kinase with minimal enzymatic activity but potential scaffolding roles in immune …
Discovery and Structure–Activity Relationship Study of (Z)-5-Methylenethiazolidin-4-one Derivatives as Potent and Selective Pan-phosphatidylinositol 5-Phosphate 4 …
TD Manz, SC Sivakumaren, FM Ferguson… - Journal of medicinal …, 2020 - ACS Publications
Due to their role in many important signaling pathways, phosphatidylinositol 5-phosphate 4-kinases
(PI5P4Ks) are attractive targets for the development of experimental therapeutics for …
(PI5P4Ks) are attractive targets for the development of experimental therapeutics for …
Structure–activity relationship study of covalent pan-phosphatidylinositol 5-phosphate 4-kinase inhibitors
TD Manz, SC Sivakumaren, A Yasgar… - ACS medicinal …, 2019 - ACS Publications
Phosphatidylinositol 5-phosphate 4-kinases (PI5P4Ks) are important molecular players in a
variety of diseases, such as cancer. Currently available PI5P4K inhibitors are reversible …
variety of diseases, such as cancer. Currently available PI5P4K inhibitors are reversible …
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-…