A FOXC2 inhibitor, MC-1-F2, as a therapeutic candidate for targeting EMT in castration-resistant prostate cancer
Bioorg Med Chem Lett. 2023 Jun 6:129369. doi: 10.1016/j.bmcl.2023.129369. Online ahead of print.ABSTRACTAndrogen deprivation therapy (ADT) is the major treatment option for advanced prostate cancer. However, prostate cancer can develop into androgen-independent castration-resistant prostate cancer (CRPC) which is resistant to ADT. An alternative treatment strategy for CRPC can be targeting the epithelial-mesenchymal transition (EMT). EMT is governed by a series of transcription factors of which forkhead box protein C2 (FOXC2) is a central mediator. Our previous research into the inhibition of FOXC2 in breast cancer cells l...
Source: Bioorganic and Medicinal Chemistry Letters - June 8, 2023 Category: Chemistry Authors: Maria Castaneda Liandra Rodriguez Jihyun Oh Brittnee Cagle-White Hanna Suh May H Abdel Aziz Jiyong Lee Source Type: research

A FOXC2 inhibitor, MC-1-F2, as a therapeutic candidate for targeting EMT in castration-resistant prostate cancer
Bioorg Med Chem Lett. 2023 Jun 6:129369. doi: 10.1016/j.bmcl.2023.129369. Online ahead of print.ABSTRACTAndrogen deprivation therapy (ADT) is the major treatment option for advanced prostate cancer. However, prostate cancer can develop into androgen-independent castration-resistant prostate cancer (CRPC) which is resistant to ADT. An alternative treatment strategy for CRPC can be targeting the epithelial-mesenchymal transition (EMT). EMT is governed by a series of transcription factors of which forkhead box protein C2 (FOXC2) is a central mediator. Our previous research into the inhibition of FOXC2 in breast cancer cells l...
Source: Bioorganic and Medicinal Chemistry Letters - June 8, 2023 Category: Chemistry Authors: Maria Castaneda Liandra Rodriguez Jihyun Oh Brittnee Cagle-White Hanna Suh May H Abdel Aziz Jiyong Lee Source Type: research

Autocrine Proteinase-Activated Receptor (PAR) signaling in PC3 prostate cancer cells
In this study, we examined the androgen independent human prostatic cancer cell line PC3 and find functional expression of PAR1 and PAR2 but not PAR4. Using genetically encoded PAR cleavage biosensors, we show that PC3 cells secrete proteolytic enzymes that cleave PARs and trigger autocrine signaling. CRISPR/Cas9 targeting of PAR1 and PAR2 combined with microarray analysis revealed genes that are regulated through this autocrine signaling mechanism. We find several genes that are known PCa prognostic factors or biomarker to be differentially expressed in the PAR1-KO and PAR2-KO PC3 cells. We further examined PAR1 and PAR2 ...
Source: Am J Physiol Cell Ph... - June 5, 2023 Category: Cytology Authors: Arundhasa Chandrabalan Rithwik Ramachandran Source Type: research

Autocrine Proteinase-Activated Receptor (PAR) signaling in PC3 prostate cancer cells
In this study, we examined the androgen independent human prostatic cancer cell line PC3 and find functional expression of PAR1 and PAR2 but not PAR4. Using genetically encoded PAR cleavage biosensors, we show that PC3 cells secrete proteolytic enzymes that cleave PARs and trigger autocrine signaling. CRISPR/Cas9 targeting of PAR1 and PAR2 combined with microarray analysis revealed genes that are regulated through this autocrine signaling mechanism. We find several genes that are known PCa prognostic factors or biomarker to be differentially expressed in the PAR1-KO and PAR2-KO PC3 cells. We further examined PAR1 and PAR2 ...
Source: American Journal of Physiology. Cell Physiology - June 5, 2023 Category: Cytology Authors: Arundhasa Chandrabalan Rithwik Ramachandran Source Type: research

Autocrine Proteinase-Activated Receptor (PAR) signaling in PC3 prostate cancer cells
In this study, we examined the androgen independent human prostatic cancer cell line PC3 and find functional expression of PAR1 and PAR2 but not PAR4. Using genetically encoded PAR cleavage biosensors, we show that PC3 cells secrete proteolytic enzymes that cleave PARs and trigger autocrine signaling. CRISPR/Cas9 targeting of PAR1 and PAR2 combined with microarray analysis revealed genes that are regulated through this autocrine signaling mechanism. We find several genes that are known PCa prognostic factors or biomarker to be differentially expressed in the PAR1-KO and PAR2-KO PC3 cells. We further examined PAR1 and PAR2 ...
Source: Am J Physiol Cell Ph... - June 5, 2023 Category: Cytology Authors: Arundhasa Chandrabalan Rithwik Ramachandran Source Type: research

Autocrine Proteinase-Activated Receptor (PAR) signaling in PC3 prostate cancer cells
In this study, we examined the androgen independent human prostatic cancer cell line PC3 and find functional expression of PAR1 and PAR2 but not PAR4. Using genetically encoded PAR cleavage biosensors, we show that PC3 cells secrete proteolytic enzymes that cleave PARs and trigger autocrine signaling. CRISPR/Cas9 targeting of PAR1 and PAR2 combined with microarray analysis revealed genes that are regulated through this autocrine signaling mechanism. We find several genes that are known PCa prognostic factors or biomarker to be differentially expressed in the PAR1-KO and PAR2-KO PC3 cells. We further examined PAR1 and PAR2 ...
Source: American Journal of Physiology. Cell Physiology - June 5, 2023 Category: Cytology Authors: Arundhasa Chandrabalan Rithwik Ramachandran Source Type: research

Autocrine Proteinase-Activated Receptor (PAR) signaling in PC3 prostate cancer cells
In this study, we examined the androgen independent human prostatic cancer cell line PC3 and find functional expression of PAR1 and PAR2 but not PAR4. Using genetically encoded PAR cleavage biosensors, we show that PC3 cells secrete proteolytic enzymes that cleave PARs and trigger autocrine signaling. CRISPR/Cas9 targeting of PAR1 and PAR2 combined with microarray analysis revealed genes that are regulated through this autocrine signaling mechanism. We find several genes that are known PCa prognostic factors or biomarker to be differentially expressed in the PAR1-KO and PAR2-KO PC3 cells. We further examined PAR1 and PAR2 ...
Source: Am J Physiol Cell Ph... - June 5, 2023 Category: Cytology Authors: Arundhasa Chandrabalan Rithwik Ramachandran Source Type: research

Autocrine Proteinase-Activated Receptor (PAR) signaling in PC3 prostate cancer cells
In this study, we examined the androgen independent human prostatic cancer cell line PC3 and find functional expression of PAR1 and PAR2 but not PAR4. Using genetically encoded PAR cleavage biosensors, we show that PC3 cells secrete proteolytic enzymes that cleave PARs and trigger autocrine signaling. CRISPR/Cas9 targeting of PAR1 and PAR2 combined with microarray analysis revealed genes that are regulated through this autocrine signaling mechanism. We find several genes that are known PCa prognostic factors or biomarker to be differentially expressed in the PAR1-KO and PAR2-KO PC3 cells. We further examined PAR1 and PAR2 ...
Source: American Journal of Physiology. Cell Physiology - June 5, 2023 Category: Cytology Authors: Arundhasa Chandrabalan Rithwik Ramachandran Source Type: research

Autocrine Proteinase-Activated Receptor (PAR) signaling in PC3 prostate cancer cells
In this study, we examined the androgen independent human prostatic cancer cell line PC3 and find functional expression of PAR1 and PAR2 but not PAR4. Using genetically encoded PAR cleavage biosensors, we show that PC3 cells secrete proteolytic enzymes that cleave PARs and trigger autocrine signaling. CRISPR/Cas9 targeting of PAR1 and PAR2 combined with microarray analysis revealed genes that are regulated through this autocrine signaling mechanism. We find several genes that are known PCa prognostic factors or biomarker to be differentially expressed in the PAR1-KO and PAR2-KO PC3 cells. We further examined PAR1 and PAR2 ...
Source: Am J Physiol Cell Ph... - June 5, 2023 Category: Cytology Authors: Arundhasa Chandrabalan Rithwik Ramachandran Source Type: research

Autocrine Proteinase-Activated Receptor (PAR) signaling in PC3 prostate cancer cells
In this study, we examined the androgen independent human prostatic cancer cell line PC3 and find functional expression of PAR1 and PAR2 but not PAR4. Using genetically encoded PAR cleavage biosensors, we show that PC3 cells secrete proteolytic enzymes that cleave PARs and trigger autocrine signaling. CRISPR/Cas9 targeting of PAR1 and PAR2 combined with microarray analysis revealed genes that are regulated through this autocrine signaling mechanism. We find several genes that are known PCa prognostic factors or biomarker to be differentially expressed in the PAR1-KO and PAR2-KO PC3 cells. We further examined PAR1 and PAR2 ...
Source: American Journal of Physiology. Cell Physiology - June 5, 2023 Category: Cytology Authors: Arundhasa Chandrabalan Rithwik Ramachandran Source Type: research

Novel α-Trifluoromethyl Chalcone Exerts Antitumor Effects Against Prostate Cancer Cells
CONCLUSION: YS71 exhibits antitumor activity by inducing apoptosis in PCa cells, including taxane-resistant cells. It could be a potential future therapeutic option for hormone- and chemotherapy-resistant PCa.PMID:37247901 | DOI:10.21873/anticanres.16411 (Source: Cell Research)
Source: Cell Research - May 29, 2023 Category: Cytology Authors: Takafumi Shimada Renato Naito Ren Toriumi Ryunosuke Nakagawa Shuhei Aoyama Taiki Kamijima Hiroshi Kano Suguru Kadomoto Hiroaki Iwamoto Hiroshi Yaegashi Kouji Izumi Yoshifumi Kadono Hiroki Nakata Yohei Saito Kyoko Nakagawa-Goto Atsushi Mizokami Source Type: research