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Rakesh Naidu
Jeffrey Cheah School of Medicine and Health Sciences, Monash University Malaysia, Jalan Lagoon Selatan

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Review
Published: 23 August 2021 in Cancers
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Gliomas are the most common, highly malignant, and deadliest forms of brain tumors. These intra-cranial solid tumors are comprised of both cancerous and non-cancerous cells, which contribute to tumor development, progression, and resistance to the therapeutic regimen. A variety of soluble inflammatory mediators (e.g., cytokines, chemokines, and chemotactic factors) are secreted by these cells, which help in creating an inflammatory microenvironment and contribute to the various stages of cancer development, maintenance, and progression. The major tumor infiltrating immune cells of the tumor microenvironment include TAMs and TANs, which are either recruited peripherally or present as brain-resident macrophages (microglia) and support stroma for cancer cell expansion and invasion. These cells are highly plastic in nature and can be polarized into different phenotypes depending upon different types of stimuli. During neuroinflammation, glioma cells interact with TAMs and TANs, facilitating tumor cell proliferation, survival, and migration. Targeting inflammatory mediators along with the reprogramming of TAMs and TANs could be of great importance in glioma treatment and may delay disease progression. In addition, an inhibition of the key signaling pathways such as NF-κB, JAK/STAT, MAPK, PI3K/Akt/mTOR, and TLRs, which are activated during neuroinflammation and have an oncogenic role in glioblastoma (GBM), can exert more pronounced anti-glioma effects.

ACS Style

Abdul Samad Basheer; Faridah Abas; Iekhsan Othman; Rakesh Naidu. Role of Inflammatory Mediators, Macrophages, and Neutrophils in Glioma Maintenance and Progression: Mechanistic Understanding and Potential Therapeutic Applications. Cancers 2021, 13, 4226 .

AMA Style

Abdul Samad Basheer, Faridah Abas, Iekhsan Othman, Rakesh Naidu. Role of Inflammatory Mediators, Macrophages, and Neutrophils in Glioma Maintenance and Progression: Mechanistic Understanding and Potential Therapeutic Applications. Cancers. 2021; 13 (16):4226.

Chicago/Turabian Style

Abdul Samad Basheer; Faridah Abas; Iekhsan Othman; Rakesh Naidu. 2021. "Role of Inflammatory Mediators, Macrophages, and Neutrophils in Glioma Maintenance and Progression: Mechanistic Understanding and Potential Therapeutic Applications." Cancers 13, no. 16: 4226.

Original research article
Published: 20 July 2021 in Frontiers in Pharmacology
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Diarylpentanoids exhibit a high degree of anti-cancer activity and stability in vitro over curcumin in prostate cancer cells. Hence, this study aims to investigate the effects of a diarylpentanoid, 1,5-bis(4-hydroxy-3-methoxyphenyl)-1,4-pentadiene-3-one (MS13) on cytotoxicity, anti-proliferative, apoptosis-inducing, anti-migration properties, and the underlying molecular mechanisms on treated androgen-independent prostate cancer cells, DU 145 and PC-3. A cell viability assay has shown greater cytotoxicity effects of MS13-treated DU 145 cells (EC50 7.57 ± 0.2 µM) and PC-3 cells (EC50 7.80 ± 0.7 µM) compared to curcumin (EC50: DU 145; 34.25 ± 2.7 µM and PC-3; 27.77 ± 6.4 µM). In addition, MS13 exhibited significant anti-proliferative activity against AIPC cells compared to curcumin in a dose- and time-dependent manner. Morphological observation, increased caspase-3 activity, and reduced Bcl-2 protein levels in these cells indicated that MS13 induces apoptosis in a time- and dose-dependent. Moreover, MS13 effectively inhibited the migration of DU 145 and PC-3 cells. Our results suggest that cell cycle-apoptosis and PI3K pathways were the topmost significant pathways impacted by MS13 activity. Our findings suggest that MS13 may demonstrate the anti-cancer activity by modulating DEGs associated with the cell cycle-apoptosis and PI3K pathways, thus inhibiting cell proliferation and cell migration as well as inducing apoptosis in AIPC cells.

ACS Style

Nurul Azwa Abd. Wahab; Faridah Abas; Iekhsan Othman; Rakesh Naidu. Diarylpentanoid (1,5-bis(4-hydroxy-3-methoxyphenyl)-1,4-pentadiene-3-one) (MS13) Exhibits Anti-proliferative, Apoptosis Induction and Anti-migration Properties on Androgen-independent Human Prostate Cancer by Targeting Cell Cycle–Apoptosis and PI3K Signalling Pathways. Frontiers in Pharmacology 2021, 12, 1 .

AMA Style

Nurul Azwa Abd. Wahab, Faridah Abas, Iekhsan Othman, Rakesh Naidu. Diarylpentanoid (1,5-bis(4-hydroxy-3-methoxyphenyl)-1,4-pentadiene-3-one) (MS13) Exhibits Anti-proliferative, Apoptosis Induction and Anti-migration Properties on Androgen-independent Human Prostate Cancer by Targeting Cell Cycle–Apoptosis and PI3K Signalling Pathways. Frontiers in Pharmacology. 2021; 12 ():1.

Chicago/Turabian Style

Nurul Azwa Abd. Wahab; Faridah Abas; Iekhsan Othman; Rakesh Naidu. 2021. "Diarylpentanoid (1,5-bis(4-hydroxy-3-methoxyphenyl)-1,4-pentadiene-3-one) (MS13) Exhibits Anti-proliferative, Apoptosis Induction and Anti-migration Properties on Androgen-independent Human Prostate Cancer by Targeting Cell Cycle–Apoptosis and PI3K Signalling Pathways." Frontiers in Pharmacology 12, no. : 1.

Journal article
Published: 10 July 2021 in International Journal of Molecular Sciences
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Diarylpentanoid (DAP), an analog that was structurally modified from a naturally occurring curcumin, has shown to enhance anticancer efficacy compared to its parent compound in various cancers. This study aims to determine the cytotoxicity, antiproliferative, and apoptotic activity of diarylpentanoid MS13 on two subtypes of non-small cell lung cancer (NSCLC) cells: squamous cell carcinoma (NCI-H520) and adenocarcinoma (NCI-H23). Gene expression analysis was performed using Nanostring PanCancer Pathways Panel to determine significant signaling pathways and targeted genes in these treated cells. Cytotoxicity screening revealed that MS13 exhibited greater inhibitory effect in NCI-H520 and NCI-H23 cells compared to curcumin. MS13 induced anti-proliferative activity in both cells in a dose- and time-dependent manner. Morphological analysis revealed that a significant number of MS13-treated cells exhibited apoptosis. A significant increase in caspase-3 activity and decrease in Bcl-2 protein concentration was noted in both MS13-treated cells in a time- and dose-dependent manner. A total of 77 and 47 differential expressed genes (DEGs) were regulated in MS13 treated-NCI-H520 and NCI-H23 cells, respectively. Among the DEGs, 22 were mutually expressed in both NCI-H520 and NCI-H23 cells in response to MS13 treatment. The top DEGs modulated by MS13 in NCI-H520—DUSP4, CDKN1A, GADD45G, NGFR, and EPHA2—and NCI-H23 cells—HGF, MET, COL5A2, MCM7, and GNG4—were highly associated with PI3K, cell cycle-apoptosis, and MAPK signaling pathways. In conclusion, MS13 may induce antiproliferation and apoptosis activity in squamous cell carcinoma and adenocarcinoma of NSCLC cells by modulating DEGs associated with PI3K-AKT, cell cycle-apoptosis, and MAPK pathways. Therefore, our present findings could provide an insight into the anticancer activity of MS13 and merits further investigation as a potential anticancer agent for NSCLC cancer therapy.

ACS Style

Wan Wan Mohd Tajuddin; Faridah Abas; Iekhsan Othman; Rakesh Naidu. Molecular Mechanisms of Antiproliferative and Apoptosis Activity by 1,5-Bis(4-Hydroxy-3-Methoxyphenyl)1,4-Pentadiene-3-one (MS13) on Human Non-Small Cell Lung Cancer Cells. International Journal of Molecular Sciences 2021, 22, 7424 .

AMA Style

Wan Wan Mohd Tajuddin, Faridah Abas, Iekhsan Othman, Rakesh Naidu. Molecular Mechanisms of Antiproliferative and Apoptosis Activity by 1,5-Bis(4-Hydroxy-3-Methoxyphenyl)1,4-Pentadiene-3-one (MS13) on Human Non-Small Cell Lung Cancer Cells. International Journal of Molecular Sciences. 2021; 22 (14):7424.

Chicago/Turabian Style

Wan Wan Mohd Tajuddin; Faridah Abas; Iekhsan Othman; Rakesh Naidu. 2021. "Molecular Mechanisms of Antiproliferative and Apoptosis Activity by 1,5-Bis(4-Hydroxy-3-Methoxyphenyl)1,4-Pentadiene-3-one (MS13) on Human Non-Small Cell Lung Cancer Cells." International Journal of Molecular Sciences 22, no. 14: 7424.

Book chapter
Published: 09 July 2021 in Regulation and Dysfunction of Apoptosis [Working Title]
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The pathogenesis of many diseases is most closely related to inappropriate apoptosis (either too little or too much) and cancer is one of the situations where too little apoptosis happens, leading to malignant cells that highly proliferate. Defects at any points along apoptotic pathways may lead to malignant transformation of the affected cells, tumor metastasis, and resistance to anti-cancer drugs. Several major molecular mechanisms are involved in the evasion of apoptosis in cancer initiation and progression. Bcl-2 family of proteins and caspases are the central players in the apoptotic mechanism and regulate cell death. Their imperfections cause to the deficient apoptotic signaling and thereby the inadequate apoptosis in cancer cells and eventually carcinogenesis. Strategies targeting these master regulators in carcinoma cells has been a major focus of interest in cancer studies. Therefore, despite being the cause of problem, apoptosis can be targeted in cancer therapy. This chapter provides a comprehensive review of apoptotic cell death and how deficiencies in apoptotic master regulators, caspases and Bcl-2 family proteins, influence carcinogenesis and can be targeted in cancer treatment.

ACS Style

Reyhaneh Farghadani; Rakesh Naidu. The Role of Apoptosis as a Double-Edge Sword in Cancer. Regulation and Dysfunction of Apoptosis [Working Title] 2021, 1 .

AMA Style

Reyhaneh Farghadani, Rakesh Naidu. The Role of Apoptosis as a Double-Edge Sword in Cancer. Regulation and Dysfunction of Apoptosis [Working Title]. 2021; ():1.

Chicago/Turabian Style

Reyhaneh Farghadani; Rakesh Naidu. 2021. "The Role of Apoptosis as a Double-Edge Sword in Cancer." Regulation and Dysfunction of Apoptosis [Working Title] , no. : 1.

Review
Published: 08 July 2021 in Cancers
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Breast cancer is the most frequently diagnosed cancer and the leading cause of cancer death among women worldwide. Despite the overall successes in breast cancer therapy, hormone-independent HER2 negative breast cancer, also known as triple negative breast cancer (TNBC), lacking estrogens and progesterone receptors and with an excessive expression of human epidermal growth factor receptor 2 (HER2), along with the hormone-independent HER2 positive subtype, still remain major challenges in breast cancer treatment. Due to their poor prognoses, aggressive phenotype, and highly metastasis features, new alternative therapies have become an urgent clinical need. One of the most noteworthy phytochemicals, curcumin, has attracted enormous attention as a promising drug candidate in breast cancer prevention and treatment due to its multi-targeting effect. Curcumin interrupts major stages of tumorigenesis including cell proliferation, survival, angiogenesis, and metastasis in hormone-independent breast cancer through the modulation of multiple signaling pathways. The current review has highlighted the anticancer activity of curcumin in hormone-independent breast cancer via focusing on its impact on key signaling pathways including the PI3K/Akt/mTOR pathway, JAK/STAT pathway, MAPK pathway, NF-ĸB pathway, p53 pathway, and Wnt/β-catenin, as well as apoptotic and cell cycle pathways. Besides, its therapeutic implications in clinical trials are here presented.

ACS Style

Reyhaneh Farghadani; Rakesh Naidu. Curcumin: Modulator of Key Molecular Signaling Pathways in Hormone-Independent Breast Cancer. Cancers 2021, 13, 3427 .

AMA Style

Reyhaneh Farghadani, Rakesh Naidu. Curcumin: Modulator of Key Molecular Signaling Pathways in Hormone-Independent Breast Cancer. Cancers. 2021; 13 (14):3427.

Chicago/Turabian Style

Reyhaneh Farghadani; Rakesh Naidu. 2021. "Curcumin: Modulator of Key Molecular Signaling Pathways in Hormone-Independent Breast Cancer." Cancers 13, no. 14: 3427.

Original research article
Published: 30 April 2021 in Frontiers in Molecular Biosciences
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Curcumin analogs with excellent biological properties have been synthesized to address and overcome the poor pharmacokinetic profiles of curcumin. This study aims to investigate the cytotoxicity, anti-proliferative, and apoptosis-inducing ability of curcumin analog, MS13 on human glioblastoma U-87 MG, and neuroblastoma SH-SY5Y cells, and to examine the global proteome changes in these cells following treatment. Our current findings showed that MS13 induced potent cytotoxicity and anti-proliferative effects on both cells. Increased caspase-3 activity and decreased bcl-2 concentration upon treatment indicate that MS13 induces apoptosis in these cells in a dose- and time-dependent manner. The label-free shotgun proteomic analysis has defined the protein profiles in both glioblastoma and neuroblastoma cells, whereby a total of nine common DEPs, inclusive of glyceraldehyde 3-phosphate dehydrogenase (GAPDH), alpha-enolase (ENO1), heat shock protein HSP 90-alpha (HSP90AA1), Heat shock protein HSP 90-beta (HSP90AB1), Eukaryotic translation initiation factor 5A-1 (EFI5A), heterogenous nuclear ribonucleoprotein K (HNRNPK), tubulin beta chain (TUBB), histone H2AX (H2AFX), and Protein SET were identified. Pathway analysis further elucidated that MS13 may induce its anti-tumor effects in both cells via the common enriched pathways, “Glycolysis” and “Post-translational protein modification.” Conclusively, MS13 demonstrates an anti-cancer effect that may indicate its potential use in the management of brain malignancies.

ACS Style

Yee Qian Lee; Pathmanathan Rajadurai; Faridah Abas; Iekhsan Othman; Rakesh Naidu. Proteomic Analysis on Anti-Proliferative and Apoptosis Effects of Curcumin Analog, 1,5-bis(4-Hydroxy-3-Methyoxyphenyl)-1,4-Pentadiene-3-One-Treated Human Glioblastoma and Neuroblastoma Cells. Frontiers in Molecular Biosciences 2021, 8, 1 .

AMA Style

Yee Qian Lee, Pathmanathan Rajadurai, Faridah Abas, Iekhsan Othman, Rakesh Naidu. Proteomic Analysis on Anti-Proliferative and Apoptosis Effects of Curcumin Analog, 1,5-bis(4-Hydroxy-3-Methyoxyphenyl)-1,4-Pentadiene-3-One-Treated Human Glioblastoma and Neuroblastoma Cells. Frontiers in Molecular Biosciences. 2021; 8 ():1.

Chicago/Turabian Style

Yee Qian Lee; Pathmanathan Rajadurai; Faridah Abas; Iekhsan Othman; Rakesh Naidu. 2021. "Proteomic Analysis on Anti-Proliferative and Apoptosis Effects of Curcumin Analog, 1,5-bis(4-Hydroxy-3-Methyoxyphenyl)-1,4-Pentadiene-3-One-Treated Human Glioblastoma and Neuroblastoma Cells." Frontiers in Molecular Biosciences 8, no. : 1.

Review
Published: 05 April 2021 in Cancers
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MicroRNAs (miRNAs) are short-strand non-coding RNAs that are responsible for post-transcriptional regulation of many biological processes. Their differential expression is important in supporting tumorigenesis by causing dysregulation in normal biological functions including cell proliferation, apoptosis, metastasis and invasion and cellular metabolism. Cellular metabolic processes are a tightly regulated mechanism. However, cancer cells have adapted features to circumvent these regulations, recognizing metabolic reprogramming as an important hallmark of cancer. The miRNA expression profile may differ between localized lung cancers, advanced lung cancers and solid tumors, which lead to a varying extent of metabolic deregulation. Emerging evidence has shown the relationship between the differential expression of miRNAs with lung cancer metabolic reprogramming in perpetuating tumorigenesis. This review provides an insight into the role of different miRNAs in lung cancer metabolic reprogramming by targeting key enzymes, transporter proteins or regulatory components alongside metabolic signaling pathways. These discussions would allow a deeper understanding of the importance of miRNAs in tumor progression therefore providing new avenues for diagnostic, therapeutic and disease management applications.

ACS Style

Mohamed Azizi; Iekhsan Othman; Rakesh Naidu. The Role of MicroRNAs in Lung Cancer Metabolism. Cancers 2021, 13, 1716 .

AMA Style

Mohamed Azizi, Iekhsan Othman, Rakesh Naidu. The Role of MicroRNAs in Lung Cancer Metabolism. Cancers. 2021; 13 (7):1716.

Chicago/Turabian Style

Mohamed Azizi; Iekhsan Othman; Rakesh Naidu. 2021. "The Role of MicroRNAs in Lung Cancer Metabolism." Cancers 13, no. 7: 1716.

Review
Published: 16 March 2021 in Nutrients
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Glioblastoma (GBM) is the most malignant brain tumor and accounts for most adult brain tumors. Current available treatment options for GBM are multimodal, which include surgical resection, radiation, and chemotherapy. Despite the significant advances in diagnostic and therapeutic approaches, GBM remains largely resistant to treatment, with a poor median survival rate between 12 and 18 months. With increasing drug resistance, the introduction of phytochemicals into current GBM treatment has become a potential strategy to combat GBM. Phytochemicals possess multifarious bioactivities with multitarget sites and comparatively marginal toxicity. Among them, curcumin is the most studied compound described as a potential anticancer agent due to its multi-targeted signaling/molecular pathways properties. Curcumin possesses the ability to modulate the core pathways involved in GBM cell proliferation, apoptosis, cell cycle arrest, autophagy, paraptosis, oxidative stress, and tumor cell motility. This review discusses curcumin’s anticancer mechanism through modulation of Rb, p53, MAPK, P13K/Akt, JAK/STAT, Shh, and NF-κB pathways, which are commonly involved and dysregulated in preclinical and clinical GBM models. In addition, limitation issues such as bioavailability, pharmacokinetics perspectives strategies, and clinical trials were discussed.

ACS Style

Shu Wong; Muhamad Kamarudin; Rakesh Naidu. Anticancer Mechanism of Curcumin on Human Glioblastoma. Nutrients 2021, 13 .

AMA Style

Shu Wong, Muhamad Kamarudin, Rakesh Naidu. Anticancer Mechanism of Curcumin on Human Glioblastoma. Nutrients. 2021; 13 (3):.

Chicago/Turabian Style

Shu Wong; Muhamad Kamarudin; Rakesh Naidu. 2021. "Anticancer Mechanism of Curcumin on Human Glioblastoma." Nutrients 13, no. 3: .

Protocol
Published: 18 December 2020 in Methods in Molecular Biology
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Shotgun proteomics has been widely applied to study proteins in complex biological samples. Combination of high-performance liquid chromatography with mass spectrometry has allowed for comprehensive protein analysis with high resolution, sensitivity, and mass accuracy. Prior to mass spectrometry analysis, proteins are extracted from biological samples and subjected to in-solution trypsin digestion. The digested proteins are subjected for clean-up and injected into the liquid chromatography-mass spectrometry system for peptide mass identification. Protein identification is performed by analyzing the mass spectrometry data on a protein search engine software such as PEAKS studio loaded with protein database for the species of interest. Results such as protein score, protein coverage, number of peptides, and unique peptides identified will be obtained and can be used to determine proteins identified with high confidence. This method can be applied to understand the proteomic changes or profile brought by bio-carrier-based therapeutics in vitro. In this chapter, we describe methods in which proteins can be extracted for proteomic analysis using a shotgun approach. The chapter outlines important in vitro techniques and data analysis that can be applied to investigate the proteome dynamics.

ACS Style

Syafiq Asnawi Zainal Abidin; Iekhsan Othman; Rakesh Naidu. Shotgun and Mass as a Tool for Protein and of Bio-Carrier-Based Therapeutics on Human Cancer Cells. Methods in Molecular Biology 2020, 2211, 233 -240.

AMA Style

Syafiq Asnawi Zainal Abidin, Iekhsan Othman, Rakesh Naidu. Shotgun and Mass as a Tool for Protein and of Bio-Carrier-Based Therapeutics on Human Cancer Cells. Methods in Molecular Biology. 2020; 2211 ():233-240.

Chicago/Turabian Style

Syafiq Asnawi Zainal Abidin; Iekhsan Othman; Rakesh Naidu. 2020. "Shotgun and Mass as a Tool for Protein and of Bio-Carrier-Based Therapeutics on Human Cancer Cells." Methods in Molecular Biology 2211, no. : 233-240.

Review article
Published: 08 November 2020 in Journal of Biomolecular Structure and Dynamics
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G protein-coupled receptors (GPCRs) belong to the largest family of protein targets comprising over 800 members in which at least 500 members are the therapeutic targets. Among the GPCRs, G protein-coupled estrogen receptor-1 (GPER-1) has shown to have the ability in estrogen signaling. As GPER-1 plays a critical role in several physiological responses, GPER-1 has been considered as a potential therapeutic target to treat estrogen-based cancers and other non-communicable diseases. However, the progress in the understanding of GPER-1 structure and function is relatively slow due to the availability of a only a few selective GPER-1 modulators. As with many GPCRs, the X-ray crystal structure of GPER-1 is yet to be resolved and thus has led the researchers to search for new GPER-1 modulators using homology models of GPER-1. In this review, we aim to summarize various approaches used in the generation of GPER-1 homology model and their applications that have resulted in new GPER-1 ligands. Highlights Features and role of homology modeling in structure. Approaches to model structure. Application of the homology model for the identification of new ligand. Communicated by Ramaswamy H. Sarma

ACS Style

Shafi Ullah Khan; Nafees Ahemad; Lay-Hong Chuah; Rakesh Naidu; Thet Thet Htar. G protein-coupled estrogen receptor-1: homology modeling approaches and application in screening new GPER-1 modulators. Journal of Biomolecular Structure and Dynamics 2020, 1 -11.

AMA Style

Shafi Ullah Khan, Nafees Ahemad, Lay-Hong Chuah, Rakesh Naidu, Thet Thet Htar. G protein-coupled estrogen receptor-1: homology modeling approaches and application in screening new GPER-1 modulators. Journal of Biomolecular Structure and Dynamics. 2020; ():1-11.

Chicago/Turabian Style

Shafi Ullah Khan; Nafees Ahemad; Lay-Hong Chuah; Rakesh Naidu; Thet Thet Htar. 2020. "G protein-coupled estrogen receptor-1: homology modeling approaches and application in screening new GPER-1 modulators." Journal of Biomolecular Structure and Dynamics , no. : 1-11.

Review
Published: 31 August 2020 in Cancers
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Colorectal cancer (CRC) is one of the most frequently diagnosed cancers, with a high mortality rate globally. The pathophysiology of CRC is mainly initiated by alteration in gene expression, leading to dysregulation in multiple signalling pathways and cellular processes. Metabolic reprogramming is one of the important cancer hallmarks in CRC, which involves the adaptive changes in tumour cell metabolism to sustain the high energy requirements for rapid cell proliferation. There are several mechanisms in the metabolic reprogramming of cancer cells, such as aerobic glycolysis, oxidative phosphorylation, lactate and fatty acids metabolism. MicroRNAs (miRNAs) are a class of non-coding RNAs that are responsible for post-transcriptional regulation of gene expression. Differential expression of miRNAs has been shown to play an important role in different aspects of tumorigenesis, such as proliferation, apoptosis, and drug resistance, as well as metabolic reprogramming. Increasing evidence also reports that miRNAs could function as potential regulators of metabolic reprogramming in CRC cells. This review provides an insight into the role of different miRNAs in regulating the metabolism of CRC cells as well as to discuss the potential role of miRNAs as biomarkers or therapeutic targets in CRC tumour metabolism.

ACS Style

Kha Wai Hon; Syafiq Zainal Abidin; Iekhsan Othman; Rakesh Naidu. Insights into the Role of microRNAs in Colorectal Cancer (CRC) Metabolism. Cancers 2020, 12, 2462 .

AMA Style

Kha Wai Hon, Syafiq Zainal Abidin, Iekhsan Othman, Rakesh Naidu. Insights into the Role of microRNAs in Colorectal Cancer (CRC) Metabolism. Cancers. 2020; 12 (9):2462.

Chicago/Turabian Style

Kha Wai Hon; Syafiq Zainal Abidin; Iekhsan Othman; Rakesh Naidu. 2020. "Insights into the Role of microRNAs in Colorectal Cancer (CRC) Metabolism." Cancers 12, no. 9: 2462.

Journal article
Published: 20 August 2020 in Molecules
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The cytotoxic and apoptotic effects of turmeric (Curcuma longa) on colon cancer have been well documented but specific structural modifications of curcumin have been shown to possess greater growth-suppressive potential on colon cancer than curcumin. Therefore, the aim of this study is to identify the anti-cancer properties of curcumin analogue-MS13, a diarylpentanoid on the cytotoxicity, anti-proliferative and apoptotic activity of primary (SW480) and metastatic (SW620) human colon cancer cells. A cell viability assay showed that MS13 has greater cytotoxicity effect on SW480 (EC50: 7.5 ± 2.8 µM) and SW620 (EC50: 5.7 ± 2.4 µM) compared to curcumin (SW480, EC50: 30.6 ± 1.4 µM) and SW620, EC50: 26.8 ± 2.1 µM). Treatment with MS13 at two different doses 1X EC50 and 2X EC50 suppressed the colon cancer cells growth with lower cytotoxicity against normal cells. A greater anti-proliferative effect was also observed in MS13 treated colon cancer cells compared to curcumin at 48 and 72 h. Subsequent analysis on the induction of apoptosis showed that MS13 treated cells exhibited morphological features associated with apoptosis. The findings are also consistent with cellular apoptotic activities shown by increased caspase-3 activity and decreased Bcl-2 protein level in both colon cancer cell lines. In conclusion, MS13 able to suppress colon cancer cell growth by inhibiting cell proliferation and induce apoptosis in primary and metastatic human colon cancer cells.

ACS Style

Nor Isnida Ismail; Iekhsan Othman; Faridah Abas; Nordin H. Lajis; Rakesh Naidu. The Curcumin Analogue, MS13 (1,5-Bis(4-hydroxy-3- methoxyphenyl)-1,4-pentadiene-3-one), Inhibits Cell Proliferation and Induces Apoptosis in Primary and Metastatic Human Colon Cancer Cells. Molecules 2020, 25, 3798 .

AMA Style

Nor Isnida Ismail, Iekhsan Othman, Faridah Abas, Nordin H. Lajis, Rakesh Naidu. The Curcumin Analogue, MS13 (1,5-Bis(4-hydroxy-3- methoxyphenyl)-1,4-pentadiene-3-one), Inhibits Cell Proliferation and Induces Apoptosis in Primary and Metastatic Human Colon Cancer Cells. Molecules. 2020; 25 (17):3798.

Chicago/Turabian Style

Nor Isnida Ismail; Iekhsan Othman; Faridah Abas; Nordin H. Lajis; Rakesh Naidu. 2020. "The Curcumin Analogue, MS13 (1,5-Bis(4-hydroxy-3- methoxyphenyl)-1,4-pentadiene-3-one), Inhibits Cell Proliferation and Induces Apoptosis in Primary and Metastatic Human Colon Cancer Cells." Molecules 25, no. 17: 3798.

Communication
Published: 29 June 2020 in Processes
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The current research work is an endeavor to study the chemical profiling and enzyme-inhibition potential of different polarity solvent (n-hexane, dichloromethane—DCM and methanol—MeOH) extracts from the aerial and stem parts of Buxus papillosa C.K. Schneid. All the extracts were analyzed for HPLC-PDA phenolic quantification, while both (aerial and stem) DCM extracts were studied for UHPLC-MS phytochemical composition. The inhibitory activity against the clinically important enzymes having crucial role in different pathologies like skin diseases (tyrosinase), inflammatory problems (lipoxygenase—LOX) and diabetes mellitus (α-amylase) were studied using standard in vitro bioassays. The DCM extracts upon UHPLC-MS analysis conducted in both negative and positive ionization modes has led to the tentative identification of 52 important secondary metabolites. Most of these belonged to the alkaloid, flavonoid, phenolic and triterpenoid classes. The HPLC-PDA polyphenolic quantification identified the presence of 10 phenolic compounds. Catechin was present in significant amounts in aerial-MeOH (7.62 ± 0.45 μg/g extract) and aerial-DCM (2.39 ± 0.51-μg/g extract) extracts. Similarly, higher amounts of epicatechin (2.76 ± 0.32-μg/g extract) and p-hydroxybenzoic acid (1.06 ± 0.21 μg/g extract) were quantified in aerial-DCM and stem-MeOH extracts, respectively. Likewise, all the extracts exhibited moderate inhibition against all the tested enzymes. These findings explain the wide usage of this plant in folklore medicine and suggest that it could be further studied as an origin of novel bioactive phytocompounds and for the designing of new pharmaceuticals.

ACS Style

Hammad Saleem; Thet Thet Htar; Rakesh Naidu; Gokhan Zengin; Marcello Locatelli; Angela Tartaglia; Syafiq Asnawi Zainal Abidin; Nafees Ahemad. Phytochemical Composition and Enzyme Inhibition Studies of Buxus papillosa C.K. Schneid. Processes 2020, 8, 757 .

AMA Style

Hammad Saleem, Thet Thet Htar, Rakesh Naidu, Gokhan Zengin, Marcello Locatelli, Angela Tartaglia, Syafiq Asnawi Zainal Abidin, Nafees Ahemad. Phytochemical Composition and Enzyme Inhibition Studies of Buxus papillosa C.K. Schneid. Processes. 2020; 8 (7):757.

Chicago/Turabian Style

Hammad Saleem; Thet Thet Htar; Rakesh Naidu; Gokhan Zengin; Marcello Locatelli; Angela Tartaglia; Syafiq Asnawi Zainal Abidin; Nafees Ahemad. 2020. "Phytochemical Composition and Enzyme Inhibition Studies of Buxus papillosa C.K. Schneid." Processes 8, no. 7: 757.

Preprint content
Published: 30 April 2020
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Estrogen receptors are important regulators of the growth of breast tumors. The complexity of estrogen signaling became apparent when some of its effects did not fit the time course for transcriptional signalling. Estrogen receptors (ER), ERα and ERβ are classical steroid receptors that typically dimerize and translocate to the nucleus after ligand binding while 7-transmembrane G

ACS Style

Shafi Khan; Thet Thet Htar; Nafees Ahemad; Lay-Hong Chuah; Rakesh Naidu. Pharmacophore-based virtual screening: Identification of new scaffolds as GPER-1 modulators. 2020, 1 .

AMA Style

Shafi Khan, Thet Thet Htar, Nafees Ahemad, Lay-Hong Chuah, Rakesh Naidu. Pharmacophore-based virtual screening: Identification of new scaffolds as GPER-1 modulators. . 2020; ():1.

Chicago/Turabian Style

Shafi Khan; Thet Thet Htar; Nafees Ahemad; Lay-Hong Chuah; Rakesh Naidu. 2020. "Pharmacophore-based virtual screening: Identification of new scaffolds as GPER-1 modulators." , no. : 1.

Preprint content
Published: 30 April 2020
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Estrogen receptors are important regulators of the growth of breast tumors. The complexity of estrogen signaling became apparent when some of its effects did not fit the time course for transcriptional signalling. Estrogen receptors (ER), ERα and ERβ are classical steroid receptors that typically dimerize and translocate to the nucleus after ligand binding while 7-transmembrane G

ACS Style

Shafi Khan; Thet Thet Htar; Nafees Ahemad; Lay-Hong Chuah; Rakesh Naidu. Pharmacophore-based virtual screening: Identification of new scaffolds as GPER-1 modulators. 2020, 1 .

AMA Style

Shafi Khan, Thet Thet Htar, Nafees Ahemad, Lay-Hong Chuah, Rakesh Naidu. Pharmacophore-based virtual screening: Identification of new scaffolds as GPER-1 modulators. . 2020; ():1.

Chicago/Turabian Style

Shafi Khan; Thet Thet Htar; Nafees Ahemad; Lay-Hong Chuah; Rakesh Naidu. 2020. "Pharmacophore-based virtual screening: Identification of new scaffolds as GPER-1 modulators." , no. : 1.

Preprint content
Published: 30 April 2020
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Estrogen receptors are important regulators of the growth of breast tumors. The complexity of estrogen signaling became apparent when some of its effects did not fit the time course for transcriptional signalling. Estrogen receptors (ER), ERα and ERβ are classical steroid receptors that typically dimerize and translocate to the nucleus after ligand binding while 7-transmembrane G

ACS Style

Shafi Khan; Thet Thet Htar; Nafees Ahemad; Lay-Hong Chuah; Rakesh Naidu. Pharmacophore-based virtual screening: Identification of new scaffolds as GPER-1 modulators. 2020, 1 .

AMA Style

Shafi Khan, Thet Thet Htar, Nafees Ahemad, Lay-Hong Chuah, Rakesh Naidu. Pharmacophore-based virtual screening: Identification of new scaffolds as GPER-1 modulators. . 2020; ():1.

Chicago/Turabian Style

Shafi Khan; Thet Thet Htar; Nafees Ahemad; Lay-Hong Chuah; Rakesh Naidu. 2020. "Pharmacophore-based virtual screening: Identification of new scaffolds as GPER-1 modulators." , no. : 1.

Preprint content
Published: 30 April 2020
Reads 0
Downloads 0

Estrogen receptors are important regulators of the growth of breast tumors. The complexity of estrogen signaling became apparent when some of its effects did not fit the time course for transcriptional signalling. Estrogen receptors (ER), ERα and ERβ are classical steroid receptors that typically dimerize and translocate to the nucleus after ligand binding while 7-transmembrane G

ACS Style

Shafi Khan; Thet Thet Htar; Nafees Ahemad; Lay-Hong Chuah; Rakesh Naidu. Pharmacophore-based virtual screening: Identification of new scaffolds as GPER-1 modulators. 2020, 1 .

AMA Style

Shafi Khan, Thet Thet Htar, Nafees Ahemad, Lay-Hong Chuah, Rakesh Naidu. Pharmacophore-based virtual screening: Identification of new scaffolds as GPER-1 modulators. . 2020; ():1.

Chicago/Turabian Style

Shafi Khan; Thet Thet Htar; Nafees Ahemad; Lay-Hong Chuah; Rakesh Naidu. 2020. "Pharmacophore-based virtual screening: Identification of new scaffolds as GPER-1 modulators." , no. : 1.

Preprint content
Published: 30 April 2020
Reads 0
Downloads 0

Estrogen receptors are important regulators of the growth of breast tumors. The complexity of estrogen signaling became apparent when some of its effects did not fit the time course for transcriptional signalling. Estrogen receptors (ER), ERα and ERβ are classical steroid receptors that typically dimerize and translocate to the nucleus after ligand binding while 7-transmembrane G

ACS Style

Shafi Khan; Thet Thet Htar; Nafees Ahemad; Lay-Hong Chuah; Rakesh Naidu. Pharmacophore-based virtual screening: Identification of new scaffolds as GPER-1 modulators. 2020, 1 .

AMA Style

Shafi Khan, Thet Thet Htar, Nafees Ahemad, Lay-Hong Chuah, Rakesh Naidu. Pharmacophore-based virtual screening: Identification of new scaffolds as GPER-1 modulators. . 2020; ():1.

Chicago/Turabian Style

Shafi Khan; Thet Thet Htar; Nafees Ahemad; Lay-Hong Chuah; Rakesh Naidu. 2020. "Pharmacophore-based virtual screening: Identification of new scaffolds as GPER-1 modulators." , no. : 1.

Preprint content
Published: 27 April 2020
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G protein-coupled estrogen receptor-1 (GPER-1) is a seven transmembrane receptor, responsible for mediating rapid estrogen signaling in many physiological responses in reproductive, nervous, endocrine, immune and cardiovascular systems. Due to unavailability of the crystal structure of GPER-1, a sequential ligand-based virtual screening (LBVS) and structure-based screening (SBVS)

ACS Style

Shafi Khan; Thet Thet Htar; Nafees Ahemad; Lay-Hong Chuah; Rakesh Naidu. Retrospective and prospective validated high-throughput virtual screening approach for the identification of new GPER-1 modulators. 2020, 1 .

AMA Style

Shafi Khan, Thet Thet Htar, Nafees Ahemad, Lay-Hong Chuah, Rakesh Naidu. Retrospective and prospective validated high-throughput virtual screening approach for the identification of new GPER-1 modulators. . 2020; ():1.

Chicago/Turabian Style

Shafi Khan; Thet Thet Htar; Nafees Ahemad; Lay-Hong Chuah; Rakesh Naidu. 2020. "Retrospective and prospective validated high-throughput virtual screening approach for the identification of new GPER-1 modulators." , no. : 1.

Preprint content
Published: 27 April 2020
Reads 0
Downloads 0

G protein-coupled estrogen receptor-1 (GPER-1) is a seven transmembrane receptor, responsible for mediating rapid estrogen signaling in many physiological responses in reproductive, nervous, endocrine, immune and cardiovascular systems. Due to unavailability of the crystal structure of GPER-1, a sequential ligand-based virtual screening (LBVS) and structure-based screening (SBVS)

ACS Style

Shafi Khan; Thet Thet Htar; Nafees Ahemad; Lay-Hong Chuah; Rakesh Naidu. Retrospective and prospective validated high-throughput virtual screening approach for the identification of new GPER-1 modulators. 2020, 1 .

AMA Style

Shafi Khan, Thet Thet Htar, Nafees Ahemad, Lay-Hong Chuah, Rakesh Naidu. Retrospective and prospective validated high-throughput virtual screening approach for the identification of new GPER-1 modulators. . 2020; ():1.

Chicago/Turabian Style

Shafi Khan; Thet Thet Htar; Nafees Ahemad; Lay-Hong Chuah; Rakesh Naidu. 2020. "Retrospective and prospective validated high-throughput virtual screening approach for the identification of new GPER-1 modulators." , no. : 1.