Small-molecule p21-activated kinase inhibitor PF-3758309 is a potent inhibitor of oncogenic signaling and tumor growth
- B. Murray, Chuangxing Guo, T. Smeal
- Biology, ChemistryProceedings of the National Academy of Sciences
- 3 May 2010
PAK4-related pathways are defined, additional support for PAK4 as a therapeutic target with a unique combination of functions (apoptotic, cytoskeletal, cell-cycle), and a potent, orally available small-molecule PAK inhibitor with significant promise for the treatment of human cancers is identified.
The conformation of hepatitis C virus NS3 proteinase with and without NS4A: a structural basis for the activation of the enzyme by its cofactor.
- R. Love, H. Parge, Z. Hostomska
- BiologyClinical and Diagnostic Virology
- 15 July 1998
Identification of inhibitors for putative malaria drug targets among novel antimalarial compounds.
- Gregory J. Crowther, A. Napuli, K. Kuhen
- Biology, ChemistryMolecular and biochemical parasitology (Print)
- 1 January 2011
Discovery of pyrroloaminopyrazoles as novel PAK inhibitors.
- Chuangxing Guo, Indrawan J. McAlpine, B. Murray
- Biology, ChemistryJournal of Medicinal Chemistry
- 14 May 2012
The efflux of the pyrrolopyrazole series was effectively reduced by applying multiple medicinal chemistry strategies, leading to a series of PAK inhibitors that are orally active in inhibiting tumor growth in vivo.
Structure-based design of novel human Pin1 inhibitors (I).
- Chuangxing Guo, Xinjun Hou, B. Murray
- Chemistry, BiologyBioorganic & Medicinal Chemistry Letters
- 1 October 2009
Structure-based design of novel human Pin1 inhibitors (II).
- Liming Dong, J. Marakovits, B. Murray
- Chemistry, BiologyBioorganic & Medicinal Chemistry Letters
- 2010
Structure-based design of novel human Pin1 inhibitors (III): optimizing affinity beyond the phosphate recognition pocket.
- Chuangxing Guo, Xinjun Hou, B. Murray
- Chemistry, BiologyBioorganic & Medicinal Chemistry Letters
- 1 September 2014
Identification and characterization of a novel and functional murine Pin1 isoform.
- Jeff X. Zhu, E. Dagostino, P. Rejto, B. Mroczkowski, B. Murray
- BiologyBiochemical and Biophysical Research…
- 3 August 2007
Abstract PR-2: Discovery of p21‐activated kinase inhibitor PF‐03758309
- Chuangxing Guo, Zhang Junhu, B. Murray
- Biology, Chemistry
- 10 December 2009
The pharmacodynamic and antitumor effects of PF‐3758309 support its evaluation as an anticancer agent, and Broad kinase screening has demonstrated that this is a selective pan‐PAK inhibitor with potential additional activities (e.g. AMPK).
TRAIL stabilization and cancer cell sensitization to its pro-apoptotic activity achieved through genetic fusion with arginine deiminase
- E. Brin, Katherine C Wu, J. Thomson
- Biology, MedicineOncoTarget
- 11 December 2018
The fusion protein of TRAIL and arginine deiminase was efficacious in a number of cell lines and synergized with some standard of care drugs and was superior to rhTRAIL administered at the same molar amounts.
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