Preclinical Evaluation of Serine/Threonine Kinase Inhibitors Against Prostate Cancer Metastases

2007 ◽  
Author(s):  
Theresa Guise
Keyword(s):  
Prostate Cancer ◽  
Kinase Inhibitors ◽  
Serine Threonine Kinase ◽  
Threonine Kinase ◽  
Preclinical Evaluation ◽  
Cancer Metastases

scholarly journals Identification of PIM1 substrates reveals a role for NDRG1 phosphorylation in prostate cancer cellular migration and invasion

2021 ◽  
Vol 4 (1) ◽  
Author(s):  
Russell J. Ledet ◽  
Sophie E. Ruff ◽  
Yu Wang ◽  
Shruti Nayak ◽  
Jeffrey A. Schneider ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Cellular Migration ◽  
Migration And Invasion ◽  
Prostate Cancer Cells ◽  
Invasion And Metastasis ◽  
Serine Threonine Kinase ◽  
Prostate Tumorigenesis ◽  
Threonine Kinase ◽  
Chemical Genetic ◽  
Protein Levels

AbstractPIM1 is a serine/threonine kinase that promotes and maintains prostate tumorigenesis. While PIM1 protein levels are elevated in prostate cancer relative to local disease, the mechanisms by which PIM1 contributes to oncogenesis have not been fully elucidated. Here, we performed a direct, unbiased chemical genetic screen to identify PIM1 substrates in prostate cancer cells. The PIM1 substrates we identified were involved in a variety of oncogenic processes, and included N-Myc Downstream-Regulated Gene 1 (NDRG1), which has reported roles in suppressing cancer cell invasion and metastasis. NDRG1 is phosphorylated by PIM1 at serine 330 (pS330), and the level of NDRG1 pS330 is associated higher grade prostate tumors. We have shown that PIM1 phosphorylation of NDRG1 at S330 reduced its stability, nuclear localization, and interaction with AR, resulting in enhanced cell migration and invasion.

scholarly journals Non-canonical role of Hippo tumor suppressor serine/threonine kinase 3 STK3 in prostate cancer.

2021 ◽  
Author(s):  
Amelia U. Schirmer ◽  
Lucy M. Driver ◽  
Megan T. Zhao ◽  
Carrow I. Wells ◽  
Julie E. Pickett ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Tumor Suppressor ◽  
Serine Threonine Kinase ◽  
Threonine Kinase

scholarly journals ROLE OF SERIN/ THREONINE KINASE INHIBITOR IN THERAPY NON-ALCOHOLIC STEATOHEPATITIS AND ALCOHOLIC HEPATITIS

2019 ◽  
Vol 6 (3) ◽  
pp. 101-109
Author(s):  
Novriantika Lestari
Keyword(s):  
Signal Transduction ◽  
Liver Fibrosis ◽  
Kinase Inhibitors ◽  
Kinase Inhibitor ◽  
Binding Activity ◽  
Serine Threonine Kinase ◽  
Threonine Kinase ◽  
Receptor Binding Activity ◽  
Marked Accumulation

Liver fibrosis is a reversible response to a wound healing with marked accumulation of extracellular matrix which caused by injury to the liver. Liver fibrosis can be caused by various factors including alcohol and non-alcohol steatohepatitis. The process of fibrosis serves to localize the inflammation during chronic exposure. The hepatic stem cell (HSC) has a key role in the pathogenesis of liver fibrosis. The HSC activation is characterized by increased profibrogenic mediators including members of the TGF-? superfamily. In order to enable signal transduction, the mediator needs to bind to its receptors. The serine/ threonine kinase receptor is a receptor that binds to the TGF-? superfamily ligand, including TGF-?, BMP, activin and other mediators. The ligand receptor-binding activity will stimulate signal transduction that will translocate into the nucleus and phosphorylate various transcription factors that play a role in cell proliferation, differentiation, or apoptosis. There is currently no standard therapy for liver fibrosis. Based on the central role of the serine/ threonine kinase receptor in the pathogenesis of liver fibrosis, it is thought that the use of serine/ threonine kinase inhibitors is a promising therapy.

Allosteric Small-Molecule Serine/Threonine Kinase Inhibitors

2019 ◽  
pp. 253-278 ◽  
Author(s):  
Resmi C. Panicker ◽  
Souvik Chattopadhaya ◽  
Anthony G. Coyne ◽  
Rajavel Srinivasan
Keyword(s):  
Small Molecule ◽  
Kinase Inhibitors ◽  
Serine Threonine Kinase ◽  
Threonine Kinase

scholarly journals Fas Activated Serine-Threonine Kinase Domains 2 (FASTKD2) mediates apoptosis of breast and prostate cancer cells through its novel FAST2 domain

BMC Cancer ◽  
2014 ◽  
Vol 14 (1) ◽  
Author(s):  
Sharmistha Das ◽  
Kay T Yeung ◽  
Muktar A Mahajan ◽  
Herbert H Samuels
Keyword(s):  
Prostate Cancer ◽  
Cancer Cells ◽  
Prostate Cancer Cells ◽  
Serine Threonine Kinase ◽  
Threonine Kinase ◽  
Breast And Prostate Cancer

Breaking the DNA Damage Response via Serine/Threonine Kinase Inhibitors to Improve Cancer Treatment

2019 ◽  
Vol 26 (8) ◽  
pp. 1425-1445 ◽  
Author(s):  
Wioletta Rozpędek ◽  
Dariusz Pytel ◽  
Alicja Nowak-Zduńczyk ◽  
Dawid Lewko ◽  
Radosław Wojtczak ◽  
...  
Keyword(s):  
Dna Damage ◽  
Dna Replication ◽  
Cancer Treatment ◽  
Dna Damage Response ◽  
Ataxia Telangiectasia ◽  
Kinase Inhibitors ◽  
Serine Threonine Kinase ◽  
Threonine Kinase ◽  
Anti Cancer ◽  
Damage Response

Multiple, both endogenous and exogenous, sources may induce DNA damage and DNA replication stress. Cells have developed DNA damage response (DDR) signaling pathways to maintain genomic stability and effectively detect and repair DNA lesions. Serine/ threonine kinases such as Ataxia-telangiectasia mutated (ATM) and Ataxia-telangiectasia and Rad3-Related (ATR) are the major regulators of DDR, since after sensing stalled DNA replication forks, DNA double- or single-strand breaks, may directly phosphorylate and activate their downstream targets, that play a key role in DNA repair, cell cycle arrest and apoptotic cell death. Interestingly, key components of DDR signaling networks may constitute an attractive target for anti-cancer therapy through two distinct potential approaches: as chemoand radiosensitizers to enhance the effectiveness of currently used genotoxic treatment or as single agents to exploit defects in DDR in cancer cells via synthetic lethal approach. Moreover, the newest data reported that serine/threonine protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK) is also closely associated with cancer development and progression. Thereby, utilization of small-molecule, serine/threonine kinase inhibitors may provide a novel, groundbreaking, anti-cancer treatment strategy. Currently, a range of potent, highlyselective toward ATM, ATR and PERK inhibitors has been discovered, but after foregoing study, additional investigations are necessary for their future clinical use.

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