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Biochemistry & Molecular Biology
Olga A. Sukocheva, Dong Gui Hu, Robyn Meech, Anupam Bishayee
Summary: Breast cancer MCF-7 cell-line-derived mammospheres exhibit enriched CD44+/CD24- cells resembling breast cancer stem cells, expressing high levels of S1P3. Growth-promoting agents induce SphK1 and S1P3 translocation to the nucleus, while TNF alpha inhibits their nuclear translocation and promotes apoptosis in mammospheres. The study suggests inhibiting SphK1 and S1P3 nuclear translocation as a novel approach to prevent BCSC proliferation.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
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Biochemistry & Molecular Biology
Yudong Yin, Li Sun, Lixin Sheng, Liqiong Zhang, Jingjing Liu, Xiaoan Wen, Weibin Mo, Quande Wang, Keguang Cheng
Summary: To discover more effective and less toxic drugs in anti-tumor field, the backbone structure of 17/?-estradiol was modified and 11 target compounds were synthesized. Compounds 5 and 10 showed better anti-tumor activity and higher selectivity, inducing apoptosis in MCF-7 cells and binding to estradiol receptor alpha. They also upregulated the expression of apoptosis-related factors and downregulated anti-apoptotic factors, indicating the induction of cell death through both endogenous and exogenous pathways.
CHEMICO-BIOLOGICAL INTERACTIONS
(2023)
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Chemistry, Medicinal
Bapu R. Thorat, Suraj N. Mali, Rahul R. Wagh, Ramesh S. Yamgar
Summary: In this study, a series of Schiff-based-aryl-carbohydrazide analogues were synthesized and their antimicrobial, antifungal, antioxidant, and anticancer activities were evaluated. The results showed that these compounds exhibited potent antimicrobial activity and had higher docking scores against common antimicrobial and antifungal targets.
CURRENT COMPUTER-AIDED DRUG DESIGN
(2022)
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Chemistry, Medicinal
Koji Wada, Akira Takaguri, Kyosuke Kaneda, Megumi Mizukami, Yuji Suzuki, Hiroshi Yamashita
Summary: This study successfully synthesized novel diterpenoid alkaloid derivatives with antiproliferative activity through structure-based design, and significantly enhanced their inhibitory effects against MCF-7 cells. 11,15-diacylation is critical for producing antiproliferative activity in this alkaloid class and may introduce a new avenue for combating breast cancer cell proliferation using natural product derivatives.
JOURNAL OF NATURAL MEDICINES
(2023)
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Chemistry, Medicinal
Eman F. Abdelhaleem, Asmaa E. Kassab, Hala B. El-Nassan, Omneya M. Khalil
Summary: Breast cancer is the leading cause of cancer incidence worldwide, and this study aims to synthesize novel celecoxib analogues and evaluate their anticancer activity. Compound 4f showed stronger anticancer activity than celecoxib and induced cell apoptosis through multiple mechanisms, making it a promising candidate for the design of potent anticancer agents.
MEDICINAL CHEMISTRY
(2022)
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Genetics & Heredity
Samira Samadi Miandoab, Mehdi Haghi, Mitra Salehi, Mohammad Ali Hosseinpour Feizi
Summary: The study demonstrated that vitamin C can lead to demethylation of the CDH1 gene promoter by increasing TET enzyme activity and gene expression, resulting in upregulation of the CDH1 gene in the MCF-7 cell line.
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Chemistry, Multidisciplinary
Abass Kareem AL-Musawi, Salwa Hameed Naser Al-Rubae'i, Monther Faisal Mahdi, AbdAljabar Khalaf Ateia
Summary: Breast cancer is a serious medical issue, and two newly synthesized compounds have shown inhibitory activity against breast cancer cells, indicating promising cytotoxic activity.
EGYPTIAN JOURNAL OF CHEMISTRY
(2022)
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Developmental Biology
Matthew Hannaford, Nicolas Loyer, Francesca Tonelli, Martin Zoltner, Jens Januschke
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Pharmacology & Pharmacy
Fiona H. Greig, Katrin Nather, Margaret D. Ballantyne, Zeshan H. Kazi, Husam Alganga, Marie-Ann Ewart, Karolina E. Zaborska, Bracy Fertig, Nigel J. Pyne, Susan Pyne, Simon Kennedy
EUROPEAN JOURNAL OF PHARMACOLOGY
(2019)
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Chemistry, Medicinal
David R. Adams, Salha Tawati, Giacomo Berretta, Paula Lopez Rivas, Jessica Baiget, Zhong Jiang, Aisha Alsfouk, Simon P. Mackay, Nigel J. Pyne, Susan Pyne
JOURNAL OF MEDICINAL CHEMISTRY
(2019)
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Pharmacology & Pharmacy
Stephen P. H. Alexander, Doriano Fabbro, Eamonn Kelly, Alistair Mathie, John A. Peters, Emma L. Veale, Jane F. Armstrong, Elena Faccenda, Simon D. Harding, Adam J. Pawson, Joanna L. Sharman, Christopher Southan, Jamie A. Davies
BRITISH JOURNAL OF PHARMACOLOGY
(2019)
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Biology
Kerryn Berndsen, Pawel Lis, Wondwossen M. Yeshaw, Paulina S. Wawro, Raja S. Nirujogi, Melanie Wightman, Thomas Macartney, Mark Dorward, Axel Knebel, Francesca Tonelli, Suzanne R. Pfeffer, Dario R. Alessi
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Biochemistry & Molecular Biology
Mariam Alsanafi, Samuel L. Kelly, Melissa McNaughton, Alfred H. Merrill, Nigel J. Pyne, Susan Pyne
BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR AND CELL BIOLOGY OF LIPIDS
(2020)
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Multidisciplinary Sciences
Ying Fan, Francesca Tonelli, Shalini Padmanabhan, Marco A. S. Baptista, Lindsey Riley, Danielle Smith, Connie Marras, Andrew Howden, Dario R. Alessi, Esther Sammler
JOVE-JOURNAL OF VISUALIZED EXPERIMENTS
(2020)
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Biochemical Research Methods
Oezge Karayel, Francesca Tonelli, Sebastian Virreira Winter, Phillip E. Geyer, Ying Fan, Esther M. Sammler, Dario R. Alessi, Martin Steger, Matthias Mann
MOLECULAR & CELLULAR PROTEOMICS
(2020)
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Biochemistry & Molecular Biology
Raja S. Nirujogi, Francesca Tonelli, Matthew Taylor, Pawel Lis, Alexander Zimprich, Esther Sammler, Dario R. Alessi
Summary: This study introduces a new mass spectrometry assay for quantifying phosphorylated Rab substrates in different cells and tissues, finding that the VPS35[D620N] mutation enhances phosphorylation levels of multiple Rab proteins. This assay provides valuable insights into the impact of Parkinson's pathogenic mutations and inhibitors on LRRK2 Rab signaling pathways, showing that Rab1 is a physiological substrate for LRRK2 and highlighting the benefits over traditional immunoblotting approaches.
BIOCHEMICAL JOURNAL
(2021)
Article
Biology
Herschel S. Dhekne, Izumi Yanatori, Edmundo G. Vides, Yuriko Sobu, Federico Diez, Francesca Tonelli, Suzanne R. Pfeffer
Summary: The study reveals that RILPL2 binds preferentially to LRRK2-phosphorylated Rab8A and Rab10, providing insights into the molecular basis of LRRK2 pathogenesis.
LIFE SCIENCE ALLIANCE
(2021)
Article
Biology
Shahzad S. Khan, Yuriko Sobu, Herschel S. Dhekne, Francesca Tonelli, Kerryn Berndsen, Dario R. Alessi, Suzanne R. Pfeffer
Summary: Activating mutations of LRRK2 cause Parkinson's disease and result in cilia loss. The loss of cilia is associated with phosphorylation of Rab GTPases, defects in astrocytes, and dysregulation of the Hedgehog signaling pathway in the nigrostriatal pathway.
Article
Neurosciences
Sara Gomes, Alicia Garrido, Francesca Tonelli, Donina Obiang, Eduardo Tolosa, Maria Jose Marti, Javier Ruiz-Martinez, Ana Vinagre-Aragon, Haizea Hernandez-Eguiazu, Ioana Croitoru, Vicky L. Marshall, Theresa Koenig, Christoph Hotzy, Frank Hsieh, Marianna Sakalosh, Elizabeth Tengstrand, Shalini Padmanabhan, Kalpana Merchant, Christof Bruecke, Walter Pirker, Alexander Zimprich, Esther Sammler
Summary: Elevated urine BMP levels were consistently found in PD patients carrying LRRK2 G2019S, R1441G/C, and VPS35 D620N mutations. Urine BMP levels could serve as promising biomarkers for patient stratification and assessing target engagement in clinical trials of targeted PD therapies.
NPJ PARKINSONS DISEASE
(2023)
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Chemistry, Medicinal
John M. Hatcher, Monika Zwirek, Adil R. Sarhan, Prasanna S. Vatsan, Francesca Tonelli, Dario R. Alessi, Paul Davies, Nathanael S. Gray
Summary: The use of proteolysis-targeting chimeras (PROTACs) targeting LRRK2 offers a promising new approach for the treatment of Parkinson's Disease by eliminating both the kinase activity and scaffolding function of LRRK2.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2023)
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Biochemistry & Molecular Biology
Sun-Hye Shin, Hee-Yeon Kim, Hee-Soo Yoon, Woo-Jae Park, David R. Adams, Nigel J. Pyne, Susan Pyne, Joo-Won Park
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2020)