Rhein potentiates doxorubicin in treating triple negative breast cancer by inhibiting cancer-associated fibroblasts
Biochem Pharmacol. 2024 Mar 16;223:116139. doi: 10.1016/j.bcp.2024.116139. Online ahead of print.ABSTRACTCancer-associated fibroblasts (CAFs), one of the most abundant stromal cells in the tumor microenvironment, mediate desmoplastic responses. CAFs are major drivers for the failure of triple-negative breast cancer (TNBC) chemotherapy. It is well-documented that many traditional Chinese medicines (TCMs) exhibit potent anti-fibrotic effects based on their capacity to suppress the production of ECM proteins. Therefore, the combination of TCMs exhausting CAFs with chemotherapy is a potential regimen for treating TNBC. Here, T...
Source: Biochemical Pharmacology - March 18, 2024 Category: Drugs & Pharmacology Authors: Shujun Xu Shuang Zheng Ninghui Ma Hongyan Zhang Jingbin Shi Jingyi Huang Ninghchao Luo Menglin Wang Yang Xiong Source Type: research

PLCE1 enhances mitochondrial dysfunction to promote GSDME-mediated pyroptosis in doxorubicin-induced cardiotoxicity
CONCLUSIONS: We discovered firstly that PLCE1 inhibition protected cardiomyocytes from DOX-induced pyroptotic injury and promoted cardiac function. This information offers a theoretical basis for promising therapy.PMID:38499110 | DOI:10.1016/j.bcp.2024.116142 (Source: Biochemical Pharmacology)
Source: Biochemical Pharmacology - March 18, 2024 Category: Drugs & Pharmacology Authors: Maierhaba Tuersuntuoheti Fei Peng Juexing Li Lei Zhou Hailan Gao Hui Gong Source Type: research

Dbl family RhoGEFs in cancer: Different roles and targeting strategies
Biochem Pharmacol. 2024 Mar 16:116141. doi: 10.1016/j.bcp.2024.116141. Online ahead of print.ABSTRACTSmall Ras homologous guanosine triphosphatase (Rho GTPase) family proteins are highly associated with tumorigenesis and development. As intrinsic exchange activity regulators of Rho GTPases, Rho guanine nucleotide exchange factors (RhoGEFs) have been demonstrated to be closely involved in tumor development and received increasing attention. They mainly contain two families: the diffuse B-cell lymphoma (Dbl) family and the dedicator of cytokinesis (Dock) family. More and more emphasis has been paid to the Dbl family members ...
Source: Biochemical Pharmacology - March 18, 2024 Category: Drugs & Pharmacology Authors: Xin-Yi Chen Ao-Yu Cheng Zi-Ying Wang Jin-Mei Jin Jia-Yi Lin Bei Wang Ying-Yun Guan Hao Zhang Yi-Xin Jiang Xin Luan Li-Jun Zhang Source Type: research

Rhein potentiates doxorubicin in treating triple negative breast cancer by inhibiting cancer-associated fibroblasts
Biochem Pharmacol. 2024 Mar 16:116139. doi: 10.1016/j.bcp.2024.116139. Online ahead of print.ABSTRACTCancer-associated fibroblasts (CAFs), one of the most abundant stromal cells in the tumor microenvironment, mediate desmoplastic responses. CAFs are major drivers for the failure of triple-negative breast cancer (TNBC) chemotherapy. It is well-documented that many traditional Chinese medicines (TCMs) exhibit potent anti-fibrotic effects based on their capacity to suppress suppress the production of ECM proteins. Therefore, the combination of TCMs exhausting CAFs with chemotherapy is a potential regimen for treating TNBC. He...
Source: Biochemical Pharmacology - March 18, 2024 Category: Drugs & Pharmacology Authors: Shujun Xu Shuang Zheng Ninghui Ma Hongyan Zhang Jingbin Shi Jingyi Huang Ninghchao Luo Menglin Wang Yang Xiong Source Type: research

PLCE1 enhances mitochondrial dysfunction to promote GSDME-mediated pyroptosis in doxorubicin-induced cardiotoxicity
CONCLUSIONS: We discovered firstly that PLCE1 inhibition protected cardiomyocytes from DOX-induced pyroptotic injury and promoted cardiac function. This information offers a theoretical basis for promising therapy.PMID:38499110 | DOI:10.1016/j.bcp.2024.116142 (Source: Biochemical Pharmacology)
Source: Biochemical Pharmacology - March 18, 2024 Category: Drugs & Pharmacology Authors: Maierhaba Tuersuntuoheti Fei Peng Juexing Li Lei Zhou Hailan Gao Hui Gong Source Type: research

Dbl family RhoGEFs in cancer: Different roles and targeting strategies
Biochem Pharmacol. 2024 Mar 16:116141. doi: 10.1016/j.bcp.2024.116141. Online ahead of print.ABSTRACTSmall Ras homologous guanosine triphosphatase (Rho GTPase) family proteins are highly associated with tumorigenesis and development. As intrinsic exchange activity regulators of Rho GTPases, Rho guanine nucleotide exchange factors (RhoGEFs) have been demonstrated to be closely involved in tumor development and received increasing attention. They mainly contain two families: the diffuse B-cell lymphoma (Dbl) family and the dedicator of cytokinesis (Dock) family. More and more emphasis has been paid to the Dbl family members ...
Source: Biochemical Pharmacology - March 18, 2024 Category: Drugs & Pharmacology Authors: Xin-Yi Chen Ao-Yu Cheng Zi-Ying Wang Jin-Mei Jin Jia-Yi Lin Bei Wang Ying-Yun Guan Hao Zhang Yi-Xin Jiang Xin Luan Li-Jun Zhang Source Type: research

Rhein potentiates doxorubicin in treating triple negative breast cancer by inhibiting cancer-associated fibroblasts
Biochem Pharmacol. 2024 Mar 16:116139. doi: 10.1016/j.bcp.2024.116139. Online ahead of print.ABSTRACTCancer-associated fibroblasts (CAFs), one of the most abundant stromal cells in the tumor microenvironment, mediate desmoplastic responses. CAFs are major drivers for the failure of triple-negative breast cancer (TNBC) chemotherapy. It is well-documented that many traditional Chinese medicines (TCMs) exhibit potent anti-fibrotic effects based on their capacity to suppress suppress the production of ECM proteins. Therefore, the combination of TCMs exhausting CAFs with chemotherapy is a potential regimen for treating TNBC. He...
Source: Biochemical Pharmacology - March 18, 2024 Category: Drugs & Pharmacology Authors: Shujun Xu Shuang Zheng Ninghui Ma Hongyan Zhang Jingbin Shi Jingyi Huang Ninghchao Luo Menglin Wang Yang Xiong Source Type: research

PLCE1 enhances mitochondrial dysfunction to promote GSDME-mediated pyroptosis in doxorubicin-induced cardiotoxicity
CONCLUSIONS: We discovered firstly that PLCE1 inhibition protected cardiomyocytes from DOX-induced pyroptotic injury and promoted cardiac function. This information offers a theoretical basis for promising therapy.PMID:38499110 | DOI:10.1016/j.bcp.2024.116142 (Source: Biochemical Pharmacology)
Source: Biochemical Pharmacology - March 18, 2024 Category: Drugs & Pharmacology Authors: Maierhaba Tuersuntuoheti Fei Peng Juexing Li Lei Zhou Hailan Gao Hui Gong Source Type: research

Corrigendum to "Effects of 5-aminoisoquinolinone, a water-soluble, potent inhibitor of the activity of poly (ADP-ribose) polymerase, in a rodent model of lung injury" [Biochem. Pharmacol. 63(1) (2002) 293-304]
Biochem Pharmacol. 2024 Mar 16;223:116099. doi: 10.1016/j.bcp.2024.116099. Online ahead of print.NO ABSTRACTPMID:38493595 | DOI:10.1016/j.bcp.2024.116099 (Source: Biochemical Pharmacology)
Source: Biochemical Pharmacology - March 17, 2024 Category: Drugs & Pharmacology Authors: Salvatore Cuzzocrea Michelle C McDonald Emanuela Mazzon Laura Dugo Ivana Serraino Mike Threadgill Achille P Caputi Christoph Thiemermann Source Type: research

Bifunctional iRGD-Exo-DOX crosses the blood-brain barrier to target central nervous system lymphoma
Biochem Pharmacol. 2024 Mar 15:116138. doi: 10.1016/j.bcp.2024.116138. Online ahead of print.ABSTRACTCentral nervous system lymphoma (CNSL) is a type of hematological tumor. Treatment of CNSL is difficult due to the existence of the blood-brain barrier (BBB). Here, we used exosomes (Exos), a type of extracellular vesicle, and iRGD to construct a new drug carrier system and use it to load doxorubicin (DOX). The results of in vitro and in vivo experiments showed that the iRGD-Exo-DOX system can efficiently and securely transport DOX through the BBB and target tumor cells. The results suggest that iRGD-Exo-DOX may cross the B...
Source: Biochemical Pharmacology - March 17, 2024 Category: Drugs & Pharmacology Authors: Tian Xia Zhenyu Liu Ying Du Jiejie Zhang Xu Liu Jian Ouyang Peipei Xu Bing Chen Source Type: research

Periodic injections of Relaxin 2, its pharmacokinetics and remodeling of rat hearts
Biochem Pharmacol. 2024 Mar 15:116136. doi: 10.1016/j.bcp.2024.116136. Online ahead of print.ABSTRACTRelaxin-2 (RLX), a critical hormone in pregnancy, has been investigated as a therapy for heart failure. In most studies, the peptide was delivered continuously, subcutaneously for 2 weeks in animals or intravenously for 2-days in human subjects, for stable circulating [RLX]. However, pulsatile hormone levels may better uncover the normal physiology. This premise was tested by subcutaneously injecting Sprague Dawley rats (250 g, N = 2 males, 2 females/group) with human RLX (0, 30, 100, or 500 µg/kg), every 12 h for 1 day, t...
Source: Biochemical Pharmacology - March 17, 2024 Category: Drugs & Pharmacology Authors: Beth Gabris-Weber Rameen Forghani Thomas Bernd Dschietzig Guillermo Romero Guy Salama Source Type: research

Bile acids serve as endogenous antagonists of the Leukemia inhibitory factor (LIF) receptor in oncogenesis
Biochem Pharmacol. 2024 Mar 15:116134. doi: 10.1016/j.bcp.2024.116134. Online ahead of print.ABSTRACTThe leukemia inhibitory factor (LIF) is member of interleukin (IL)-6 family of cytokines involved immune regulation, morphogenesis and oncogenesis. In cancer tissues, LIF binds a heterodimeric receptor (LIFR), formed by a LIFRβ subunit and glycoprotein(gp)130, promoting epithelial mesenchymal transition and cell growth. Bile acids are cholesterol metabolites generated at the interface of host metabolism and the intestinal microbiota. Here we demonstrated that bile acids serve as endogenous antagonist to LIFR in oncogenesis...
Source: Biochemical Pharmacology - March 17, 2024 Category: Drugs & Pharmacology Authors: Cristina Di Giorgio Elva Morretta Antonio Lupia Rachele Bellini Carmen Massa Ginevra Urbani Martina Bordoni Silvia Marchian ò Ginevra Lachi Pasquale Rapacciuolo Claudia Finamore Valentina Sepe Maria Chiara Monti Federica Moraca Nicola Natalizi Luigina Gr Source Type: research

Adipose tissue in cortisol excess: What Cushing's syndrome can teach us?
Biochem Pharmacol. 2024 Mar 15:116137. doi: 10.1016/j.bcp.2024.116137. Online ahead of print.ABSTRACTEndogenous Cushing's syndrome (CS) is a rare condition due to prolonged exposure to elevated circulating cortisol levels that features its typical phenotype characterised by moon face, proximal myopathy, easy bruising, hirsutism in females and a centripetal distribution of body fat. Given the direct and indirect effects of hypercortisolism, CS is a severe disease burdened by increased cardio-metabolic morbidity and mortality in which visceral adiposity plays a leading role. Although not commonly found in clinical setting, e...
Source: Biochemical Pharmacology - March 17, 2024 Category: Drugs & Pharmacology Authors: Alessandro Bavaresco Pierluigi Mazzeo Martina Lazzara Mattia Barbot Source Type: research

HNF1A induces glioblastoma by upregulating EPS8 and activating PI3K/AKT signaling pathway
Biochem Pharmacol. 2024 Mar 15:116133. doi: 10.1016/j.bcp.2024.116133. Online ahead of print.ABSTRACTDespite the exact biological role of HNF1 homolog A (HNF1A) in the regulatory mechanism of glioblastoma (GBM), the molecular mechanism, especially the downstream regulation as a transcription factor, remains to be further elucidated. Immunohistochemistry was used to detect the expression and clinical relevance of HNF1A in GBM patients. CCK8, TUNEL, and subcutaneous tumor formation in nude mice were used to evaluate the effect of HNF1A on GBM in vitro and in vivo. The correction between HNF1A and epidermal growth factor rece...
Source: Biochemical Pharmacology - March 17, 2024 Category: Drugs & Pharmacology Authors: Gang Yang Fei Su Bin-Xiao Han Hong-Xin Su Chen-Hao Guo Shao-Hua Yu Quan-Lin Guan Xiao-Ming Hou Source Type: research

Role of carboxylesterase and arylacetamide deacetylase in drug metabolism, physiology, and pathology
Biochem Pharmacol. 2024 Mar 14:116128. doi: 10.1016/j.bcp.2024.116128. Online ahead of print.ABSTRACTCarboxylesterases (CES1 and CES2) and arylacetamide deacetylase (AADAC), which are expressed primarily in the liver and/or gastrointestinal tract, hydrolyze drugs containing ester and amide bonds in their chemical structure. These enzymes often catalyze the conversion of prodrugs, including the COVID-19 drugs remdesivir and molnupiravir, to their pharmacologically active forms. Information on the substrate specificity and inhibitory properties of these enzymes, which would be useful for drug development and toxicity avoidan...
Source: Biochemical Pharmacology - March 16, 2024 Category: Drugs & Pharmacology Authors: Mai Nagaoka Yoshiyuki Sakai Miki Nakajima Tatsuki Fukami Source Type: research