Search

Your search keyword '"Mohardt, Mikaela L."' showing total 8 results
Start Over Author "Mohardt, Mikaela L."
8 results on '"Mohardt, Mikaela L."'

1. Identification of a potent and selective covalent Pin1 inhibitor

Author

Pinch, Benika J., Doctor, Zainab M., Nabet, Behnam, Browne, Christopher M., Seo, Hyuk-Soo, Mohardt, Mikaela L., Kozono, Shingo, Lian, Xiaolan, Manz, Theresa D., Chun, Yujin, Kibe, Shin, Zaidman, Daniel, Daitchman, Dina, Yeoh, Zoe C., Vangos, Nicholas E., Geffken, Ezekiel A., Tan, Li, Ficarro, Scott B., London, Nir, Marto, Jarrod A., Buratowski, Stephen, Dhe-Paganon, Sirano, Zhou, Xiao Zhen, Lu, Kun Ping, and Gray, Nathanael S.

Published
2020
Full Text
View/download PDF

3. Development and Characterization of Selective FAK Inhibitors and PROTACs with In Vivo Activity

Author

Koide, Eriko, primary, Mohardt, Mikaela L., additional, Doctor, Zainab M., additional, Yang, Annan, additional, Hao, Mingfeng, additional, Donovan, Katherine A., additional, Kuismi, Christina C., additional, Nelson, Alissa J., additional, Abell, Kathryn, additional, Aguiar, Mike, additional, Che, Jianwei, additional, Stokes, Matthew P., additional, Zhang, Tinghu, additional, Aguirre, Andrew J., additional, Fischer, Eric S., additional, Gray, Nathanael S., additional, Jiang, Baishan, additional, and Nabet, Behnam, additional

Published
2023
Full Text
View/download PDF

4. Identification of a potent and selective covalent Pin1 inhibitor

Author

Pinch, Benika J., Doctor, Zainab M., Nabet, Behnam, Browne, Christopher M., Seo, Hyuk-Soo, Mohardt, Mikaela L., Kozono, Shingo, Lian, Xiaolan, Manz, Theresa D., Chun, Yujin, Kibe, Shin, Zaidman, Daniel, Daitchman, Dina, Yeoh, Zoe C., Vangos, Nicholas E., Geffken, Ezekiel A., Tan, Li, Ficarro, Scott B., London, Nir, Marto, Jarrod A., Buratowski, Stephen, Dhe-Paganon, Sirano, Zhou, Xiao Zhen, Lu, Kun Ping, and Gray, Nathanael S.

Abstract

Peptidyl-prolyl cis/transisomerase NIMA-interacting 1 (Pin1) is commonly overexpressed in human cancers, including pancreatic ductal adenocarcinoma (PDAC). While Pin1 is dispensable for viability in mice, it is required for activated Ras to induce tumorigenesis, suggesting a role for Pin1 inhibitors in Ras-driven tumors, such as PDAC. We report the development of rationally designed peptide inhibitors that covalently target Cys113, a highly conserved cysteine located in the Pin1 active site. The inhibitors were iteratively optimized for potency, selectivity and cell permeability to give BJP-06-005-3, a versatile tool compound with which to probe Pin1 biology and interrogate its role in cancer. In parallel to inhibitor development, we employed genetic and chemical-genetic strategies to assess the consequences of Pin1 loss in human PDAC cell lines. We demonstrate that Pin1 cooperates with mutant KRAS to promote transformation in PDAC, and that Pin1 inhibition impairs cell viability over time in PDAC cell lines.

Published
2024
Full Text
View/download PDF

6. Rapid and direct control of target protein levels with VHL-recruiting dTAG molecules

Author

Nabet, Behnam, primary, Ferguson, Fleur M., additional, Seong, Bo Kyung A., additional, Kuljanin, Miljan, additional, Leggett, Alan L., additional, Mohardt, Mikaela L., additional, Robichaud, Amanda, additional, Conway, Amy S., additional, Buckley, Dennis L., additional, Mancias, Joseph D., additional, Bradner, James E., additional, Stegmaier, Kimberly, additional, and Gray, Nathanael S., additional

Published
2020
Full Text
View/download PDF

8. Front Cover: Development and Characterization of Selective FAK Inhibitors and PROTACs with In Vivo Activity (ChemBioChem 19/2023).

Author

Koide, Eriko, Mohardt, Mikaela L., Doctor, Zainab M., Yang, Annan, Hao, Mingfeng, Donovan, Katherine A., Kuismi, Christina C., Nelson, Alissa J., Abell, Kathryn, Aguiar, Mike, Che, Jianwei, Stokes, Matthew P., Zhang, Tinghu, Aguirre, Andrew J., Fischer, Eric S., Gray, Nathanael S., Jiang, Baishan, and Nabet, Behnam

Published
2023
Full Text
View/download PDF

Catalog

Books, media, physical & digital resources
See catalog results