Article
Biology
Ikki Sakuma, Hidekazu Nagano, Naoko Hashimoto, Masanori Fujimoto, Akitoshi Nakayama, Takahiro Fuchigami, Yuki Taki, Tatsuma Matsuda, Hiroyuki Akamine, Satomi Kono, Takashi Kono, Masataka Yokoyama, Motoi Nishimura, Koutaro Yokote, Tatsuki Ogasawara, Yoichi Fujii, Seishi Ogawa, Eunyoung Lee, Takashi Miki, Tomoaki Tanaka
Summary: Fructose-1,6-bisphosphatase (FBPase) deficiency, caused by an FBP1 mutation, is a rare disease characterized by hypoglycemic lactic acidosis. This study identified compound heterozygous missense mutations of FBP1 in an adult patient, which resulted in decreased protein expression and loss of enzyme activity. The findings suggest that protein misfolding plays a key role in the pathogenesis of FBPase deficiency, particularly for Type 2 mutations.
COMMUNICATIONS BIOLOGY
(2023)
Article
Multidisciplinary Sciences
Anna Selezneva, Luke N. M. Harding, Hiten Gutka, Farahnaz Movahedzadeh, Celerino Abad-Zapatero
Summary: This study presents the crystal structures of FBPaseII in both active and inactivated states, providing insights into the catalytic mechanism of this enzyme. The analysis of interatomic distances among the substrate, product, and metal cofactors has led to a revision of the previously proposed mechanism. Furthermore, the study also supports the novel catalytic mechanism of similar enzymes in other microorganisms.
Article
Microbiology
Christina Wilkinson, Meredith T. Morris
Summary: This study demonstrates a complex relationship between FBPase activity and extracellular glucose levels in Trypanosoma brucei, suggesting a potential additional role for FBPase in parasite metabolism. The differential expression of FBPase in various parasite cell lines and growth conditions implies regulation via post-translational modifications. These findings provide new insights into the metabolic pathways of Trypanosoma brucei.
Article
Biochemistry & Molecular Biology
Mandy Pack, Tim Nikolai Gulde, Michelle Victoria Voelcker, Anne S. Boewe, Selina Wrublewsky, Emmanuel Ampofo, Mathias Montenarh, Claudia Goetz
Summary: Glucose homeostasis is vital for organism survival and is regulated by CK2. In this study, a qRT-PCR array was used to identify diabetes-associated genes and it was found that inhibition of CK2 led to decreased gene expression and activity of fructose-1,6-bisphosphatase 1 (FBP1), a central enzyme in gluconeogenesis. As a result, glucose secretion was reduced. These findings highlight FBP1 as a new factor in the CK2-regulated network of carbohydrate metabolism control.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Agriculture, Multidisciplinary
Li Yan-yan, Guo Li-na, Liang Cheng-zhen, Meng Zhi-gang, Syed Tahira, Guo San-dui, Zhang Rui
Summary: Elevated expression levels of cyFBPase and SBPase genes positively regulated each other and had synergistic effects on photosynthesis rates and growth traits of transgenic tobacco plants. Transgenic plants overexpressing cyFBPase and/or SBPase genes showed improvements in sucrose and starch contents.
JOURNAL OF INTEGRATIVE AGRICULTURE
(2022)
Article
Biochemistry & Molecular Biology
Xiaoyan Liang, Xiaoliang Liu, Wenjing Li, Lu Zhang, Bijun Zhang, Guangrui Lai, Yanyan Zhao
Summary: This article reports a case of rare FBPase deficiency in a Chinese boy, which is caused by mutations in the FBP1 gene. The study found that the mutant FBP1 protein has reduced stability and enzymatic activity, and is subjected to enhanced ubiquitination and proteasomal degradation mediated by NEDD4-2.
ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS
(2023)
Article
Radiology, Nuclear Medicine & Medical Imaging
Wanqian Rao, Bei Chen, Ling Xiao, Haoyue Zhu, Chen Chen, Yongxiang Tang, Shuo Hu
Summary: This study found that the expression of fructose-1,6-bisphosphatase 1 (FBP1) is associated with [F-18]FDG PET uptake and postsurgical outcomes in patients with mesial temporal lobe epilepsy (mTLE). The results also showed that FBP1 inhibits [F-18]FDG uptake by regulating GLUT-3 expression. High FBP1 expression is indicative of low GABA(A)R expression and poor prognosis.
EUROPEAN RADIOLOGY
(2023)
Article
Chemistry, Medicinal
Xiaoyu Wang, Rui Zhao, Wenming Ji, Jie Zhou, Quan Liu, Linxiang Zhao, Zhufang Shen, Shuainan Liu, Bailing Xu
Summary: A series of new indole and benzofuran analogues were designed and synthesized to evaluate their inhibitory activity against FBPase. Compounds with N-acylsulfonamide moiety on the 3-position of the indole-2-carboxylic acid scaffold showed submicromolar IC50 values, providing insights for creating structurally distinct FBPase inhibitors with high potency and drug-like properties. Three X-ray crystal structures of the complexes were solved, revealing the structural basis for the inhibitory activity.
ACS MEDICINAL CHEMISTRY LETTERS
(2022)
Article
Biochemistry & Molecular Biology
Isha Sengupta, Payel Mondal, Amrita Sengupta, Atanu Mondal, Vipin Singh, Swagata Adhikari, Sinjini Dhang, Siddhartha Roy, Chandrima Das
Summary: During HBV infection, the upregulation of FBP1 and the reprogramming of Sp110 protein contribute to the progression of HBV-induced HCC. High expression of Sp110 can serve as a prognostic marker and a potential therapeutic target for HBV-induced HCCs.
Article
Cell Biology
Olena Dmytruk, Nina Bulbotka, Anastasya Zazulya, Marta Semkiv, Kostyantyn Dmytruk, Andriy Sibirny
Summary: Enzymes involved in methanol metabolism of methylotrophic yeasts are localized in peroxisomes and cytosol, with a decrease in activity observed after shifting cells from methanol to glucose medium. The mechanism of cytosolic enzyme inactivation remains unknown, with studies showing protein degradation as a cause in some strains. Autophagy pathway is found to play a role in degradation of certain enzymes in glucose medium, suggesting a complex regulatory mechanism in methanol metabolism.
CELL BIOLOGY INTERNATIONAL
(2021)
Article
Oncology
Alexander Damanakis, Patrick Sven Plum, Florian Gebauer, Wolfgang Schroeder, Reinhard Buettner, Thomas Zander, Christiane Josephine Bruns, Alexander Quaas
Summary: This study describes the prognostic and potentially therapeutic relevance of FBP1 in esophageal adenocarcinoma (EAC). Intratumoral FBP1 expression in EAC patients is significantly associated with a better prognosis and elevated FBP1 expression is an independent biomarker associated with a favorable prognosis.
JOURNAL OF CANCER RESEARCH AND CLINICAL ONCOLOGY
(2022)
Article
Plant Sciences
C. M. Yu, Y. C. Ke, K. P. Zhang, M. Yan, H. R. Jin, Y. H. Chen, J. Zhang
Summary: Saccharides are a crucial energy source and primary component in wheat. However, genes related to the metabolism of primary saccharides in wheat have not been fully characterized. In this study, genes encoding key enzymes involved in saccharide metabolism were identified and their functions during wheat growth were explored. The findings suggest that these genes cooperate in wheat growth and the knockout of TaPFP beta may decrease wheat vitality.
BIOLOGIA PLANTARUM
(2021)
Article
Oncology
Bi Wang, Yingnan Yuan, Yin Zou, Zhengjun Qi, Guijia Huang, Yi Liu, Shan Xia, Yu Huang, Zhi Huang
Summary: Growing evidence supports the important role of aerobic glycolysis in cervical cancer. This study reveals that FBP2 plays a role in cervical cancer progression by inhibiting aerobic glycolysis through inducing PKM2 ubiquitination.
Article
Endocrinology & Metabolism
Magali Gorce, Elise Lebigot, Alina Arion, Anais Brassier, Aline Cano, Pascale De Lonlay, Francois Feillet, Claire Gay, Francois Labarthe, Marie-Cecile Nassogne, Sandrine Roche, Agathe Roubertie, Elise Sacaze, Guy Touati, Pierre Broue
Summary: Fructose-1,6-bisphosphatase deficiency can lead to liver diseases, including hepatomegaly, elevated liver enzymes, and acute liver failure. Liver steatosis may be caused by endoplasmic reticulum stress and de novo lipogenesis activation, potentially resulting in severe long-term liver complications.
JOURNAL OF INHERITED METABOLIC DISEASE
(2022)
Article
Plant Sciences
Fernanda Espinoza-Hernandez, Adolfo Andrade-Cetto, Sonia Escandon-Rivera, Gerardo Mata-Torres, Rachel Mata
Summary: The aqueous extract of Eryngium cymosum has a significant hypoglycemic effect in hyperglycaemic rats by reducing blood glucose levels and inhibiting gluconeogenic enzymes activity, while also affecting insulin levels. Therefore, E. cymosum may have potential effectiveness in treating type 2 diabetes.
JOURNAL OF ETHNOPHARMACOLOGY
(2021)
Article
Chemistry, Medicinal
Ping Lan, F. Anthony Romero, Dariusz Wodka, Andrew J. Kassick, Qun Dang, Tony Gibson, Daniel Cashion, Gaochao Zhou, Yuli Chen, Xiaoping Zhang, Aihua Zhang, Ying Li, Maria E. Trujillo, Qing Shao, Margaret Wu, Shiyao Xu, Huaibing He, Deidre MacKenna, Jocelyn Staunton, Kevin T. Chapman, Ann Weber, Iyassu K. Sebhat, Gergely M. Makarat
JOURNAL OF MEDICINAL CHEMISTRY
(2017)
Article
Chemistry, Medicinal
Marion Lanier, Jason Pickens, Simone V. Bigi, Erica L. Bradshaw-Pierce, Alison Chambers, Zacharia S. Cheruvallath, Derek Cole, Douglas R. Dougan, Jacques Ermolieff, Tony Gibson, Petro Halkowycz, Aid Hirokawa, Anthony Ivetac, Joanne Miura, Evan Nunez, Mark Sabat, John Tyhonas, Haixia Wang, Xiaolun Wang, Steve Swann
ACS MEDICINAL CHEMISTRY LETTERS
(2017)
Article
Chemistry, Applied
Jinbao Xiang, Dongsheng Wen, Hongxiang Xie, Qun Dang, Xu Bai
JOURNAL OF COMBINATORIAL CHEMISTRY
(2010)
Article
Chemistry, Medicinal
Qun Dang, Yan Liu, Daniel K. Cashion, Srinivas Rao Kasibhatla, Tao Jiang, Frank Taplin, Jason D. Jacintho, Haiqing Li, Zhili Sun, Yi Fan, Jay DaRe, Feng Tian, Wenyu Li, Tony Gibson, Robert Lemus, Paul D. van Poelje, Scott C. Potter, Mark D. Erion
JOURNAL OF MEDICINAL CHEMISTRY
(2011)
Article
Biochemistry & Molecular Biology
Jinbao Xiang, Hanghang Li, Kai Yang, Lang Yi, Yongnan Xu, Qun Dang, Xu Bai
MOLECULAR DIVERSITY
(2012)
Article
Biochemistry & Molecular Biology
Jinbao Xiang, Chao Geng, Lang Yi, Qun Dang, Xu Bai
MOLECULAR DIVERSITY
(2011)
Article
Biochemistry & Molecular Biology
Qun Dang, Srinivas Rao Kasibthatla, Tao Jiang, Frank Taplin, Tony Gibson, Scott C. Potter, Paul D. van Poelje, Mark D. Erion
Article
Chemistry, Applied
Kai Yang, Jinbao Xiang, Guochen Bao, Qun Dang, Xu Bai
ACS COMBINATORIAL SCIENCE
(2013)
Article
Chemistry, Medicinal
Andrew C. Flick, Carolyn A. Leverett, Hong X. Ding, Emma McInturff, Sarah J. Fink, Subham Mahapatra, Daniel W. Carney, Erick A. Lindsey, Jacob C. DeForest, Scott P. France, Simon Berritt, Simone Bigi-Botterill, Tony S. Gibson, Yiyang Liu, Christopher J. O'Donnell
Summary: New drugs introduced to the market are privileged structures with affinities for biological targets implicated in human diseases, providing insights into molecular recognition and guiding future drug design.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Andrew C. Flick, Carolyn A. Leverett, Hong X. Ding, Emma L. McInturff, Sarah J. Fink, Subham Mahapatra, Daniel W. Carney, Erick A. Lindsey, Jacob C. DeForest, Scott P. France, Simon Berritt, Simone Bigi-Botterill, Tony S. Gibson, Rebecca B. Watson, Yiyang Liu, Christopher J. O'Donnell
Summary: This Review presents the most likely process-scale synthetic approaches to 44 new chemical entities approved for the first time anywhere in the world during 2020. These privileged structures with affinities for biological targets implicated in human diseases and conditions, particularly small molecules and antibody-drug conjugates (ADCs), provide insight into molecular recognition and serve as leads for future drug design.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Emma L. McInturff, Scott P. France, Carolyn A. Leverett, Andrew C. Flick, Erick A. Lindsey, Simon Berritt, Daniel W. Carney, Jacob C. DeForest, Hong X. Ding, Sarah J. Fink, Tony S. Gibson, Kaitlyn Gray, Aran K. Hubbell, Amber M. Johnson, Yiyang Liu, Subham Mahapatra, Indrawan J. McAlpine, Rebecca B. Watson, Christopher J. O'Donnell
Summary: New drugs introduced to the market each year provide valuable insights into molecular recognition and potential leads for future medicines. This annual review focuses on the process-scale synthetic approaches to 35 newly approved compounds worldwide in 2021, including small molecules and antibody-drug conjugates.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Gastroenterology & Hepatology
John R. Konen, Melody M. Haag, Daria Guseva, Molly Hurd, Alisha A. Linton, Brigitte Lavoie, Colleen B. Kerrigan, Emily Joyce, Stephan C. Bischoff, Steve Swann, Luana Griffin, Jun Matsukawa, Matthew D. Falk, Tony S. Gibson, Grant W. Hennig, Jill Wykosky, Gary M. Mawe
Summary: Stimulation of epithelial 5-HT(4)Rs can enhance propulsive motility, indicating mucosal 5-HT(4)Rs may represent a safe and effective therapeutic target for constipation treatment.
NEUROGASTROENTEROLOGY AND MOTILITY
(2021)
Article
Chemistry, Medicinal
Tony S. Gibson, Benjamin Johnson, Andrea Fanjul, Petro Halkowycz, Douglas R. Dougan, Derek Cole, Steven Swann
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2017)
Article
Chemistry, Medicinal
Rebecca Nofsinger, Sophie-Dorothee Clas, Rosa Sanchez, Abbas Walji, Kimberly Manser, Becky Nissley, Jaume Balsells, Amrithraj Nair, Qun Dang, David Jonathan Bennett, Michael Hafey, Junying Wang, John Higgins, Allen Templeton, Paul Coleman, Jay Grobler, Ronald Smith, Yunhui Wu