Article
Biochemistry & Molecular Biology
Eslam M. H. Ali, Mohammed S. Abdel-Maksoud, Usama M. Ammar, Karim Mersal, Kyung Ho Yoo, Park Jooryeong, Chang-Hyun Oh
Summary: The study developed and synthesized a series of compounds with anticancer potential, demonstrating promising activity in various cancer types. Two compounds showed notable anti-cancer effects on Melanoma cancer cell lines.
BIOORGANIC CHEMISTRY
(2021)
Article
Immunology
Marianna Nicoletta Rossi, Silvia Federici, Andrea Uva, Chiara Passarelli, Camilla Celani, Ivan Caiello, Valentina Matteo, Stefano Petrocchi, Eva Piano Mortari, Fabrizio De Benedetti, Giusi Prencipe, Antonella Insalaco
Summary: A20 gene mutations are associated with the development of HA20, an autoimmune disease, and functional analysis confirmed the pathogenicity of the mutations. The study demonstrated the role of A20 not only in regulating the NF-kB pathway, but also the IFN gamma pathway.
FRONTIERS IN IMMUNOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Ines Maestro, Enrique Madruga, Patricia Boya, Ana Martinez
Summary: SGK1 is involved in various neurodegenerative pathways and has the potential to be a pharmacological target for diseases like apoptosis, neuroinflammation, and autophagy. However, there are currently no inhibitors that can cross the blood-brain barrier. In this study, virtual screening identified the deazapurine moiety as a promising scaffold for SGK1 inhibitors. These inhibitors were found to provide neuroprotection in vitro and block mitophagy independently of PRKN, suggesting their potential as neuroprotective chemical tools.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Lei Xu, Simeng Chen, Bin Wen, Hao Shi, Changbiao Chi, Chenxi Liu, Kangyu Wang, Xianglin Tao, Ming Wang, Jun Lv, Liang Yan, Liefeng Ling, Guoping Zhu
Summary: UV irradiation leads to the formation of CPDs and 6-4 photoproducts in DNA, which can be repaired by CPD photolyases and 6-4 photolyases. A novel class of short photolyase-like proteins, identified through phylogenetic analyses, have high similarity to CPD photolyases and may be the ancestors of the cryptochrome/photolyase family.
MOLECULAR BIOLOGY AND EVOLUTION
(2021)
Article
Biochemistry & Molecular Biology
David M. Andrews, Sharon Cartic, Sabina Cosulich, Nullin Divecha, Paul Faulder, Vikki Flemington, Oliver Kern, Jason G. Kettle, Ellen MacDonald, Jennifer McKelvie, Kurt G. Pike, Bryan Roberts, Rachel Rowlinson, James M. Smith, Martin Stockley, Martin E. Swarbrick, Iris Treinies, Michael J. Waring
Summary: A novel and highly specific inhibitor of PIP5K has been discovered, which demonstrates potent biochemical and cellular activity, providing valuable insight into the role of PIP5K in human cancers.
BIOORGANIC & MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Sifan Lyu, Yunshuo Zhao, Xiao Zeng, Xiaotong Chen, Qingqing Meng, Zhe Ding, Wenshan Zhao, Yuanming Qi, Yanfeng Gao, Jiangfeng Du
Summary: This study identified novel compounds with CD73 inhibitory activity using computer-aided drug discovery and enzymatic-based assays. Compounds based on phelligridin showed the best inhibitory effects and may serve as lead compounds for developing CD73-targeting drugs. The molecular weight of the identified inhibitors is around 500 Daltons, and they are predicted to primarily form hydrogen bonds with CD73, in addition to hydrophobic stacking interactions.
JOURNAL OF CHEMICAL INFORMATION AND MODELING
(2021)
Article
Biochemistry & Molecular Biology
Larissa Kever, Max Hunnefeld, Jannis Brehm, Ralf Heermann, Julia Frunzke
Summary: Bacteriophages can be a powerful source for identifying novel antimicrobial proteins by targeting key regulatory hubs of their host. The Gip protein, encoded by CGP3 prophage, was found to interact directly with DNA gyrase subunit A and specifically inhibit the DNA gyrase of Corynebacterium glutamicum, resulting in growth defects and induction of the SOS response. The overexpression of Gip also led to the induction of the cryptic CGP3 prophage, likely caused by topological alterations.
MOLECULAR MICROBIOLOGY
(2021)
Review
Oncology
Gianluca Mauri, Erica Bonazzina, Alessio Amatu, Federica Tosi, Katia Bencardino, Viviana Gori, Daniela Massihnia, Tiziana Cipani, Francesco Spina, Silvia Ghezzi, Salvatore Siena, Andrea Sartore-Bianchi
Summary: The BRAF(V600E) mutation is detected in 8-10% of patients with metastatic colorectal cancer (mCRC) and has a poor prognostic outlook, with median overall survival below 20 months. Treatment options include immune checkpoint inhibitors (CPIs) for those with concomitant MSI-H status, and a combination of cytotoxic chemotherapy + anti-VEGF or EGFR and BRAF inhibitors for first and second line treatment, respectively. However, acquired resistance limits the potential benefits and survival remains poor. Ongoing clinical trials are exploring various strategies to improve treatment outcomes for this subset of patients.
Article
Genetics & Heredity
Rongrong Wang, Xiaohui Bai, Huiming Yang, Jingyu Ma, Shudong Yu, Zhiming Lu
Summary: A novel variant of AIFM1 was identified for the first time in a Chinese family with AN. This study is of great significance for understanding the molecular mechanism and genetic cause of AN.
FRONTIERS IN GENETICS
(2022)
Article
Chemistry, Medicinal
Raquel B. M. de Almeida, Deyse B. B. Barbosa, Mayra R. R. do Bomfim, Jessika A. O. Amparo, Bruno S. S. Andrade, Silvia L. L. Costa, Joaquin M. Campos, Jorddy N. Cruz, Cleydson B. R. Santos, Franco H. A. Leite, Mariana B. B. Botura
Summary: The compound ZINC390718 was found to exhibit inhibitory activity against acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE), and showed low cytotoxicity in vitro. Molecular dynamics (MD) simulation revealed that ZINC390718 interacted with the catalytic residue sites of both enzymes. These findings suggest that ZINC390718 could be a potential chemotype for the development of new dual cholinesterase inhibitors.
Article
Biochemistry & Molecular Biology
Qingyan Zhang, Feng Sang, Jieyu Qian, ShaoLi Lyu, Wang Wang, Ying Wang, Qiang Li, LinFang Du
Summary: This study identified a novel potential PI3Kα inhibitor, TCM-N1, through structure-based virtual screening, bioassays, and molecular dynamics simulations. TCM-N1 exhibited superior binding affinity and moderate inhibition activity against PI3Kα, as well as relatively high anti-tumor proliferation ability in gastric, colorectal, and cervical cancer cells. The compound was tightly embedded into the ATP-binding pocket via hydrogen bonds, van der Waals interactions, and hydrophobic interactions, suggesting promise for the development of more potent PI3Kα-inhibiting analogs.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2021)
Article
Agronomy
Tengda Sun, Xiaoyu Jin, Xiaoming Zhang, Xingxing Lu, Huan Xu, Jialin Cui, Xinling Yang, Xili Liu, Li Zhang, Yun Ling
Summary: The introduction of hydrogen-bonded receptors such as morpholine and piperazine enhances the inhibitory activity, antifungal activity, and antirice blast activity of target compounds. Experimental results showed that all target compounds exhibited inhibitory activity against laccase, and some compounds showed even stronger inhibitory effects than a2. Compound m14 showed good antifungal activity and antirice blast activity.
PEST MANAGEMENT SCIENCE
(2023)
Article
Biology
Paulina Rzasa, Sarah Whelan, Pooyeh Farahmand, Hong Cai, Inna Guterman, Raquel Palacios-Gallego, Shanthi S. Undru, Lauren Sandford, Caleb Green, Catherine Andreadi, Maria Mintseva, Emma Parrott, Hong Jin, Fiona Hey, Susan Giblett, Nicolas B. Sylvius, Natalie S. Allcock, Anna Straatman-Iwanowska, Roberto Feuda, Cristina Tufarelli, Karen Brown, Catrin Pritchard, Alessandro Rufini
Summary: BRAF mutations occur early in serrated colorectal cancers, but their long-term influence on tissue homeostasis is poorly characterized. Short-term and long-term expression of Braf(V600E) in the intestinal tissue perturbs the homeostasis of intestinal epithelial cells, impairs differentiation of enterocytes, and leads to persistent transcriptional reprogramming.
COMMUNICATIONS BIOLOGY
(2023)
Article
Microbiology
Hideki Kondo, Naoto Yoshida, Miki Fujita, Kazuyuki Maruyama, Kiwamu Hyodo, Hiroshi Hisano, Tetsuo Tamada, Ida Bagus Andika, Nobuhiro Suzuki
Summary: A novel wheat virus Q (WVQ) was discovered to be associated with yellow mosaic disease in winter wheat, potentially transmitted through soil to wheat plants. Laboratory tests confirmed that WVQ infection induces antiviral RNA silencing responses in plants.
FRONTIERS IN MICROBIOLOGY
(2021)
Article
Biochemistry & Molecular Biology
Consuelo Coronel Arrechea, Maria Luz Giolito, Iris Alejandra Garcia, Gaston Soria, Javier Valdez Taubas
Summary: Protein palmitoylation, a common post-translational modification, plays important roles in various cancers, neurodegenerative diseases, and infectious diseases. Lack of specific inhibitors has hampered research progress in this field. A yeast-based high-throughput method has been developed to screen for small molecules that inhibit protein palmitoylation effectively.
Review
Neurosciences
Hedwig Stanisz, Adina Vultur, Meenhard Herlyn, Alexander Roesch, Ivan Bogeski
JOURNAL OF PHYSIOLOGY-LONDON
(2016)
Letter
Oncology
Adina Vultur, Tim Schanstra, Meenhard Herlyn
Article
Oncology
Batool Shannan, Quan Chen, Andrea Watters, Michela Perego, Clemens Krepler, Rakhee Thombre, Ling Li, Geena Rajan, Scott Peterson, Phyllis A. Gimotty, Melissa Wilson, Katherine L. Nathanson, Tara C. Gangadhar, Lynn M. Schuchter, Ashani T. Weeraratna, Meenhard Herlyn, Adina Vultur
PIGMENT CELL & MELANOMA RESEARCH
(2016)
Article
Oncology
Batool Shannan, Andrea Watters, Quan Chen, Stefan Mollin, Markus Doerr, Eric Meggers, Xiaowei Xu, Phyllis A. Gimotty, Michela Perego, Ling Li, Joseph Benci, Clemens Krepler, Patricia Brafford, Jie Zhang, Zhi Wei, Gao Zhang, Qin Liu, Xiangfan Yin, Katherine L. Nathanson, Meenhard Herlyn, Adina Vultur
Article
Oncology
Clemens Krepler, Min Xiao, Minu Samanta, Adina Vultur, Hsin-Yi Chen, Patricia Brafford, Patricia I. Reyes-Uribe, Molly Halloran, Thomas Chen, Xu He, Denitsa Hristova, Qin Liu, Ahmed A. Samatar, Michael A. Davies, Katherine L. Nathanson, Mizuho Fukunaga-Kalabis, Meenhard Herlyn, Jessie Villanueva
Article
Oncology
Shujing Liu, Michael T. Tetzlaff, Tao Wang, Xiang Chen, Ruifeng Yang, Suresh M. Kumar, Adina Vultur, Pengxiang Li, James S. Martin, Meenhard Herlyn, Ravi Amaravadi, Bin Li, Xiaowei Xu
Article
Cell Biology
Clemens Krepler, Katrin Sproesser, Patricia Brafford, Marilda Beqiri, Bradley Garman, Min Xiao, Batool Shannan, Andrea Watters, Michela Perego, Gao Zhang, Adina Vultur, Xiangfan Yin, Qin Liu, Ioannis N. Anastopoulos, Bradley Wubbenhorst, Melissa A. Wilson, Wei Xu, Giorgos Karakousis, Michael Feldman, Xiaowei Xu, Ravi Amaravadi, Tara C. Gangadhar, David E. Elder, Lauren E. Haydu, Jennifer A. Wargo, Michael A. Davies, Yiling Lu, Gordon B. Mills, Dennie T. Frederick, Michal Barzily-Rokni, Keith T. Flaherty, Dave S. Hoon, Michael Guarino, Joseph J. Bennett, Randall W. Ryan, Nicholas J. Petrelli, Carol L. Shields, Mizue Terai, Takami Sato, Andrew E. Aplin, Alexander Roesch, David Darr, Steve Angus, Rakesh Kumar, Ensar Halilovic, Giordano Caponigro, Sebastien Jeay, Jens Wuerthner, Annette Walter, Matthias Ocker, Matthew B. Boxer, Lynn Schuchter, Katherine L. Nathanson, Meenhard Herlyn
Review
Physiology
Adina Vultur, Christine S. Gibhardt, Hedwig Stanisz, Ivan Bogeski
PFLUGERS ARCHIV-EUROPEAN JOURNAL OF PHYSIOLOGY
(2018)
Article
Biochemistry & Molecular Biology
A. Vultur, J. Villanueva, C. Krepler, G. Rajan, Q. Chen, M. Xiao, L. Li, P. A. Gimotty, M. Wilson, J. Hayden, F. Keeney, K. L. Nathanson, M. Herlyn
Article
Biochemistry & Molecular Biology
D. Ravindran Menon, S. Das, C. Krepler, A. Vultur, B. Rinner, S. Schauer, K. Kashofer, K. Wagner, G. Zhang, E. Bonyadi Rad, N. K. Haass, H. P. Soyer, B. Gabrielli, R. Somasundaram, G. Hoefler, M. Herlyn, H. Schaider
Article
Biochemistry & Molecular Biology
Xin Zhang, Christine S. Gibhardt, Thorsten Will, Hedwig Stanisz, Christina Koerbel, Miso Mitkovski, Ioana Stejerean, Sabrina Cappello, David Pacheu-Grau, Jan Dudek, Nasser Tahbaz, Lucas Mina, Thomas Simmen, Matthias W. Laschke, Michael D. Menger, Michael P. Schoen, Volkhard Helms, Barbara A. Niemeyer, Peter Rehling, Adina Vultur, Ivan Bogeski
Article
Oncology
Sabrina Cappello, Hsu-Min Sung, Christian Ickes, Christine S. Gibhardt, Adina Vultur, Hilal Bhat, Zhongwen Hu, Patricia Brafford, Andreas Denger, Ioana Stejerean-Todoran, Rixa-Mareike Koehn, Verena Lorenz, Nicolas Kuenzel, Gabriela Salinas, Hedwig Stanisz, Tobias Legler, Peter Rehling, Michael P. Schoen, Karl S. Lang, Volkhard Helms, Meenhard Herlyn, Markus Hoth, Carsten Kummerow, Ivan Bogeski
Summary: The study reveals the potential therapeutic benefits of harnessing Natural Killer (NK) cells in melanoma immunotherapy and identifies certain proteins that can affect NK cell-mediated melanoma killing. These findings contribute to the identification of novel prognostic biomarkers related to NK cells and may lead to improved and personalized melanoma-directed immunotherapies.
Article
Dermatology
Denitsa M. Hristova, Takeshi Fukumoto, Chihiro Takemori, Le Gao, Xia Hua, Joshua X. Wang, Ling Li, Marilda Beqiri, Andrea Watters, Adina Vultur, Yusra Gimie, Vito Rebecca, Anastasia Samarkina, Haruki Jimbo, Chikako Nishigori, Jie Zhang, Chaoran Cheng, Zhi Wei, Rajasekharan Somasundaram, Mizuho Fukunaga-Kalabis, Meenhard Herlyn
Summary: NUMB plays a role in suppressing invasion and metastasis in melanoma by regulating the NOTCH-CCNE axis.
JOURNAL OF INVESTIGATIVE DERMATOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Ioana Stejerean-Todoran, Katharina Zimmermann, Christine S. Gibhardt, Adina Vultur, Christian Ickes, Batool Shannan, Zurine Bonilla del Rio, Anna Wolling, Sabrina Cappello, Hsu-Min Sung, Magdalena Shumanska, Xin Zhang, Maithily Nanadikar, Muhammad U. Latif, Anna Wittek, Felix Lange, Andrea Waters, Patricia Brafford, Jorg Wilting, Henning Urlaub, Dorthe M. Katschinski, Peter Rehling, Christof Lenz, Stefan Jakobs, Volker Ellenrieder, Alexander Roesch, Michael P. Schon, Meenhard Herlyn, Hedwig Stanisz, Ivan Bogeski
Summary: MCUA expression correlates with melanoma patient survival and MCUA knockdown suppresses melanoma cell growth and stimulates migration and invasion. Knockdown of MCUA reduces tumor volumes but promotes lung metastases.
Article
Oncology
Ioana Stejerean-Todoran, Phyllis A. Gimotty, Andrea Watters, Patricia Brafford, Clemens Krepler, Tetiana Godok, Haiyin Li, Zurine Bonilla del Rio, Anke Zieseniss, Dorthe M. Katschinski, Sinem M. Sertel, Silvio O. Rizzoli, Bradley Garman, Katherine L. Nathanson, Xiaowei Xu, Qing Chen, Jack H. Oswald, Michal Lotem, Gordon B. Mills, Michael A. Davies, Michael P. Schon, Ivan Bogeski, Meenhard Herlyn, Adina Vultur
Summary: Melanoma brain metastases (MBM) have distinct genetic and molecular characteristics compared to metastases in other sites. In this study, the researchers identified a specific molecular process, RAC1 signaling, that plays a role in the adaptation of MBM to the brain microenvironment. Understanding these molecular processes can aid in the molecular characterization and treatment of brain metastases.