Death-associated protein kinase 1 phosphorylates MDM2 and inhibits its protein stability and function
Arch Pharm Res. 2023 Oct 7. doi: 10.1007/s12272-023-01469-8. Online ahead of print.ABSTRACTBreast cancer is one of the major malignancies in women, and most related deaths are due to recurrence, drug resistance, and metastasis. The expression of the mouse double minute 2 (MDM2) oncogene is upregulated in breast cancer; however, its regulatory mechanism has yet to be fully elucidated. Herein, we identified the tumor suppressor death-associated protein kinase 1 (DAPK1) as a novel MDM2 regulator by unbiased peptide library screening. DAPK1 is directly bound to MDM2 and phosphorylates it at Thr419. DAPK1-mediated MDM2 phosphor...
Source: Archives of Pharmacal Research - October 7, 2023 Category: Drugs & Pharmacology Authors: Mi Zhang Xindong Shui Xiaoqing Zheng Jong Eun Lee Yingxue Mei Ruomeng Li Yuan Tian Xiuzhi Zheng Quling Wang Long Wang Dongmei Chen Tao Zhang Byeong Mo Kim Jungho Kim Tae Ho Lee Source Type: research
Death-associated protein kinase 1 phosphorylates MDM2 and inhibits its protein stability and function
Arch Pharm Res. 2023 Oct 7. doi: 10.1007/s12272-023-01469-8. Online ahead of print.ABSTRACTBreast cancer is one of the major malignancies in women, and most related deaths are due to recurrence, drug resistance, and metastasis. The expression of the mouse double minute 2 (MDM2) oncogene is upregulated in breast cancer; however, its regulatory mechanism has yet to be fully elucidated. Herein, we identified the tumor suppressor death-associated protein kinase 1 (DAPK1) as a novel MDM2 regulator by unbiased peptide library screening. DAPK1 is directly bound to MDM2 and phosphorylates it at Thr419. DAPK1-mediated MDM2 phosphor...
Source: Archives of Pharmacal Research - October 7, 2023 Category: Drugs & Pharmacology Authors: Mi Zhang Xindong Shui Xiaoqing Zheng Jong Eun Lee Yingxue Mei Ruomeng Li Yuan Tian Xiuzhi Zheng Quling Wang Long Wang Dongmei Chen Tao Zhang Byeong Mo Kim Jungho Kim Tae Ho Lee Source Type: research
Death-associated protein kinase 1 phosphorylates MDM2 and inhibits its protein stability and function
Arch Pharm Res. 2023 Oct 7. doi: 10.1007/s12272-023-01469-8. Online ahead of print.ABSTRACTBreast cancer is one of the major malignancies in women, and most related deaths are due to recurrence, drug resistance, and metastasis. The expression of the mouse double minute 2 (MDM2) oncogene is upregulated in breast cancer; however, its regulatory mechanism has yet to be fully elucidated. Herein, we identified the tumor suppressor death-associated protein kinase 1 (DAPK1) as a novel MDM2 regulator by unbiased peptide library screening. DAPK1 is directly bound to MDM2 and phosphorylates it at Thr419. DAPK1-mediated MDM2 phosphor...
Source: Archives of Pharmacal Research - October 7, 2023 Category: Drugs & Pharmacology Authors: Mi Zhang Xindong Shui Xiaoqing Zheng Jong Eun Lee Yingxue Mei Ruomeng Li Yuan Tian Xiuzhi Zheng Quling Wang Long Wang Dongmei Chen Tao Zhang Byeong Mo Kim Jungho Kim Tae Ho Lee Source Type: research
Death-associated protein kinase 1 phosphorylates MDM2 and inhibits its protein stability and function
Arch Pharm Res. 2023 Oct 7. doi: 10.1007/s12272-023-01469-8. Online ahead of print.ABSTRACTBreast cancer is one of the major malignancies in women, and most related deaths are due to recurrence, drug resistance, and metastasis. The expression of the mouse double minute 2 (MDM2) oncogene is upregulated in breast cancer; however, its regulatory mechanism has yet to be fully elucidated. Herein, we identified the tumor suppressor death-associated protein kinase 1 (DAPK1) as a novel MDM2 regulator by unbiased peptide library screening. DAPK1 is directly bound to MDM2 and phosphorylates it at Thr419. DAPK1-mediated MDM2 phosphor...
Source: Archives of Pharmacal Research - October 7, 2023 Category: Drugs & Pharmacology Authors: Mi Zhang Xindong Shui Xiaoqing Zheng Jong Eun Lee Yingxue Mei Ruomeng Li Yuan Tian Xiuzhi Zheng Quling Wang Long Wang Dongmei Chen Tao Zhang Byeong Mo Kim Jungho Kim Tae Ho Lee Source Type: research
Death-associated protein kinase 1 phosphorylates MDM2 and inhibits its protein stability and function
Arch Pharm Res. 2023 Oct 7. doi: 10.1007/s12272-023-01469-8. Online ahead of print.ABSTRACTBreast cancer is one of the major malignancies in women, and most related deaths are due to recurrence, drug resistance, and metastasis. The expression of the mouse double minute 2 (MDM2) oncogene is upregulated in breast cancer; however, its regulatory mechanism has yet to be fully elucidated. Herein, we identified the tumor suppressor death-associated protein kinase 1 (DAPK1) as a novel MDM2 regulator by unbiased peptide library screening. DAPK1 is directly bound to MDM2 and phosphorylates it at Thr419. DAPK1-mediated MDM2 phosphor...
Source: Archives of Pharmacal Research - October 7, 2023 Category: Drugs & Pharmacology Authors: Mi Zhang Xindong Shui Xiaoqing Zheng Jong Eun Lee Yingxue Mei Ruomeng Li Yuan Tian Xiuzhi Zheng Quling Wang Long Wang Dongmei Chen Tao Zhang Byeong Mo Kim Jungho Kim Tae Ho Lee Source Type: research
Death-associated protein kinase 1 phosphorylates MDM2 and inhibits its protein stability and function
Arch Pharm Res. 2023 Oct 7. doi: 10.1007/s12272-023-01469-8. Online ahead of print.ABSTRACTBreast cancer is one of the major malignancies in women, and most related deaths are due to recurrence, drug resistance, and metastasis. The expression of the mouse double minute 2 (MDM2) oncogene is upregulated in breast cancer; however, its regulatory mechanism has yet to be fully elucidated. Herein, we identified the tumor suppressor death-associated protein kinase 1 (DAPK1) as a novel MDM2 regulator by unbiased peptide library screening. DAPK1 is directly bound to MDM2 and phosphorylates it at Thr419. DAPK1-mediated MDM2 phosphor...
Source: Archives of Pharmacal Research - October 7, 2023 Category: Drugs & Pharmacology Authors: Mi Zhang Xindong Shui Xiaoqing Zheng Jong Eun Lee Yingxue Mei Ruomeng Li Yuan Tian Xiuzhi Zheng Quling Wang Long Wang Dongmei Chen Tao Zhang Byeong Mo Kim Jungho Kim Tae Ho Lee Source Type: research
Death-associated protein kinase 1 phosphorylates MDM2 and inhibits its protein stability and function
Arch Pharm Res. 2023 Oct 7. doi: 10.1007/s12272-023-01469-8. Online ahead of print.ABSTRACTBreast cancer is one of the major malignancies in women, and most related deaths are due to recurrence, drug resistance, and metastasis. The expression of the mouse double minute 2 (MDM2) oncogene is upregulated in breast cancer; however, its regulatory mechanism has yet to be fully elucidated. Herein, we identified the tumor suppressor death-associated protein kinase 1 (DAPK1) as a novel MDM2 regulator by unbiased peptide library screening. DAPK1 is directly bound to MDM2 and phosphorylates it at Thr419. DAPK1-mediated MDM2 phosphor...
Source: Archives of Pharmacal Research - October 7, 2023 Category: Drugs & Pharmacology Authors: Mi Zhang Xindong Shui Xiaoqing Zheng Jong Eun Lee Yingxue Mei Ruomeng Li Yuan Tian Xiuzhi Zheng Quling Wang Long Wang Dongmei Chen Tao Zhang Byeong Mo Kim Jungho Kim Tae Ho Lee Source Type: research
2-Geranyl-1-methoxyerythrabyssin II alleviates lipid accumulation and inflammation in hepatocytes through AMPK activation and AKT inhibition
In conclusion, GMET alleviated lipid accumulation and inflammation to preserve normal hepatocyte function in steatohepatitis. Thus, GMET is a novel potential multi-targeting compound to improve steatohepatitis.PMID:37782374 | DOI:10.1007/s12272-023-01464-z (Source: Archives of Pharmacal Research)
Source: Archives of Pharmacal Research - October 2, 2023 Category: Drugs & Pharmacology Authors: Yiyuan Xi Soeun Kim Thi Thanh Thuy Nguyen Phil Jun Lee Jujia Zheng Zhuofeng Lin Namki Cho Source Type: research
2-Geranyl-1-methoxyerythrabyssin II alleviates lipid accumulation and inflammation in hepatocytes through AMPK activation and AKT inhibition
In conclusion, GMET alleviated lipid accumulation and inflammation to preserve normal hepatocyte function in steatohepatitis. Thus, GMET is a novel potential multi-targeting compound to improve steatohepatitis.PMID:37782374 | DOI:10.1007/s12272-023-01464-z (Source: Archives of Pharmacal Research)
Source: Archives of Pharmacal Research - October 2, 2023 Category: Drugs & Pharmacology Authors: Yiyuan Xi Soeun Kim Thi Thanh Thuy Nguyen Phil Jun Lee Jujia Zheng Zhuofeng Lin Namki Cho Source Type: research
2-Geranyl-1-methoxyerythrabyssin II alleviates lipid accumulation and inflammation in hepatocytes through AMPK activation and AKT inhibition
In conclusion, GMET alleviated lipid accumulation and inflammation to preserve normal hepatocyte function in steatohepatitis. Thus, GMET is a novel potential multi-targeting compound to improve steatohepatitis.PMID:37782374 | DOI:10.1007/s12272-023-01464-z (Source: Archives of Pharmacal Research)
Source: Archives of Pharmacal Research - October 2, 2023 Category: Drugs & Pharmacology Authors: Yiyuan Xi Soeun Kim Thi Thanh Thuy Nguyen Phil Jun Lee Jujia Zheng Zhuofeng Lin Namki Cho Source Type: research
2-Geranyl-1-methoxyerythrabyssin II alleviates lipid accumulation and inflammation in hepatocytes through AMPK activation and AKT inhibition
In conclusion, GMET alleviated lipid accumulation and inflammation to preserve normal hepatocyte function in steatohepatitis. Thus, GMET is a novel potential multi-targeting compound to improve steatohepatitis.PMID:37782374 | DOI:10.1007/s12272-023-01464-z (Source: Archives of Pharmacal Research)
Source: Archives of Pharmacal Research - October 2, 2023 Category: Drugs & Pharmacology Authors: Yiyuan Xi Soeun Kim Thi Thanh Thuy Nguyen Phil Jun Lee Jujia Zheng Zhuofeng Lin Namki Cho Source Type: research
2-Geranyl-1-methoxyerythrabyssin II alleviates lipid accumulation and inflammation in hepatocytes through AMPK activation and AKT inhibition
In conclusion, GMET alleviated lipid accumulation and inflammation to preserve normal hepatocyte function in steatohepatitis. Thus, GMET is a novel potential multi-targeting compound to improve steatohepatitis.PMID:37782374 | DOI:10.1007/s12272-023-01464-z (Source: Archives of Pharmacal Research)
Source: Archives of Pharmacal Research - October 2, 2023 Category: Drugs & Pharmacology Authors: Yiyuan Xi Soeun Kim Thi Thanh Thuy Nguyen Phil Jun Lee Jujia Zheng Zhuofeng Lin Namki Cho Source Type: research
Exploring new histone deacetylase 6 inhibitors and their effects on reversing the α-tubulin deacetylation and cell morphology changes caused by methamphetamine
Arch Pharm Res. 2023 Sep 30. doi: 10.1007/s12272-023-01467-w. Online ahead of print.ABSTRACTIndazole-based HDAC6 inhibitors with novel zinc-binding modifications were synthesized and evaluated to determine their potential to inhibit HDAC6. The analogs were subjected to a histone deacetylase (HDAC) enzyme assay, which led to identification of compounds 3a and 3b. Both compounds demonstrated higher potency and selectivity as HDAC6 inhibitors with IC50 values of 9.1 nM and 9.0 nM, respectively, and highlighted the importance of the hydroxamic acid moiety for binding to Zn2+ inside the catalytic pocket of HDAC enzymes. In the ...
Source: Archives of Pharmacal Research - September 30, 2023 Category: Drugs & Pharmacology Authors: Sunil K Gupta Khan Hashim Ali Sooyeun Lee Young Ho Seo Source Type: research
Exploring new histone deacetylase 6 inhibitors and their effects on reversing the α-tubulin deacetylation and cell morphology changes caused by methamphetamine
Arch Pharm Res. 2023 Sep 30. doi: 10.1007/s12272-023-01467-w. Online ahead of print.ABSTRACTIndazole-based HDAC6 inhibitors with novel zinc-binding modifications were synthesized and evaluated to determine their potential to inhibit HDAC6. The analogs were subjected to a histone deacetylase (HDAC) enzyme assay, which led to identification of compounds 3a and 3b. Both compounds demonstrated higher potency and selectivity as HDAC6 inhibitors with IC50 values of 9.1 nM and 9.0 nM, respectively, and highlighted the importance of the hydroxamic acid moiety for binding to Zn2+ inside the catalytic pocket of HDAC enzymes. In the ...
Source: Archives of Pharmacal Research - September 30, 2023 Category: Drugs & Pharmacology Authors: Sunil K Gupta Khan Hashim Ali Sooyeun Lee Young Ho Seo Source Type: research
Artemongolins A-K, undescribed germacrane-guaiane sesquiterpenoid dimers from Artemisia mongolica and their antihepatoma activities
Arch Pharm Res. 2023 Sep 28. doi: 10.1007/s12272-023-01466-x. Online ahead of print.ABSTRACTArtemongolins A-K (1-11), which are undescribed sesquiterpenoid dimers, were obtained from Artemisia mongolica and characterized through comprehensive spectral data, including HRESIMS, IR, 1D and 2D NMR, and ECD calculations. The absolute configurations of compounds 1, 4, and 7 were undoubtedly determined by a single-crystal X-ray crystallography. Artemongolins A-K (1-11) featured a rare 5/7/5/5/5/10 hexacyclic system composed of a germacrene and a guaianolide by a fused 2-oxaspiro[4,4]nonane-1-one ring system. Antihepatoma evaluati...
Source: Archives of Pharmacal Research - September 28, 2023 Category: Drugs & Pharmacology Authors: Chong Shang Yun-Bao Ma Yuan Wang Xiao-Feng He Tian-Ze Li Ji-Jun Chen Source Type: research
