Article
Biochemistry & Molecular Biology
Mahadev Latha, Achintya Kumar Dolui, Panneerselvam Vijayaraj
Summary: A seed-specific lipase, SL-AT4G28520, was identified to have monoacylglycerol lipase activity during germination, while the canonical FL-AT4G28520 did not show detectable activity. This study suggests that the activity of SL-AT4G28520 lipase is dependent on physiological conditions and provides insights into lipid mobilization during germination.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2021)
Article
Food Science & Technology
Didem Sutay Kocabas, John Lyne, Zeynep Ustunol
Summary: Hydrolytic enzymes play a crucial role in the dairy industry, impacting the sensory qualities of dairy products such as texture, taste, and aroma. Microbial hydrolases are favored over plant and animal derived alternatives. There is a growing demand for hydrolytic enzymes with superior properties to enhance the quality of dairy products.
TRENDS IN FOOD SCIENCE & TECHNOLOGY
(2022)
Article
Chemistry, Medicinal
Shuhei Ikeda, Hideyuki Sugiyama, Hidekazu Tokuhara, Masataka Murakami, Minoru Nakamura, Yuya Oguro, Jumpei Aida, Nao Morishita, Satoshi Sogabe, Douglas R. Dougan, Sean C. Gay, Ling Qin, Naoto Arimura, Yasuko Takahashi, Masako Sasaki, Yusuke Kamada, Kazunobu Aoyama, Kouya Kimoto, Makoto Kamata
Summary: This study presents a novel spirochemical series as potent and reversible MAGL inhibitors with a different binding mode, showing potential therapeutic benefits for central nervous system-related diseases. Starting from hit compound 1, various spiro scaffolds were generated using a structure-based drug discovery approach, resulting in the development of a promising reversible MAGL inhibitor with significant pharmacodynamic changes in mice.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Multidisciplinary Sciences
Adam M. Crowe, Jessica M. C. Krekhno, Kirstin L. Brown, Jayesh A. Kulkarni, Katherine C. Yam, Lindsay D. Eltis
Summary: Mycobacterium abscessus contains genes predicted to encode two steroid catabolic pathways, and unlike other similar bacteria, it lacks genes encoding MCP hydrolase. The study shows that cholesterol is essential for the growth of the bacteria and the catabolic pathways are not solely dependent on coenzyme A sequestration.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
(2022)
Article
Biochemistry & Molecular Biology
Ziad Omran
Summary: Novel disulfiram derivatives were evaluated as potent inhibitors of MAGL, showing high selectivity over FAAH. Compound 2i displayed low micromolar inhibition of MAGL without inhibitory activity against FAAH.
Article
Biochemistry & Molecular Biology
Mohamad Fawzi Mahomoodally, Devina Lobine, Marie Carene Nancy Picot-Allain, Nabeelah Sadeer, Sharmeen Jugreet, Gokhan Zengin
Summary: This review provides an overview of the pathogenesis of diabetes mellitus and its associated complications, as well as the potential mechanisms of herbal remedies in managing diabetes. It also evaluates the recent progress of herbal products in treating diabetes by regulating inflammation and gut microbiota. Furthermore, the review discusses the promising potential of natural plant-derived compounds as antidiabetic agents and their effects on key enzymes linked to diabetes and its complications.
CURRENT MEDICINAL CHEMISTRY
(2021)
Review
Chemistry, Multidisciplinary
Sophie Elisabeth Honeder, Tamara Tomin, Maximilian Schinagl, Raphael Pfleger, Julia Hoehlschen, Barbara Darnhofer, Matthias Schittmayer, Ruth Birner-Gruenberger
Summary: Activity-based proteomic profiling (ABPP) is a versatile protein profiling technique that allows the functional study of enzymes by using small molecule probes that bind covalently to the active site of an enzyme. This technique enables the targeting and labeling of enzymes in their native state, even in cells and tissues. In the context of lipid hydrolase research, ABPP has been used to discover and characterize lipid hydrolases, as well as to identify commonly used probes and inhibitors through competitive ABPP. However, there are caveats and limitations that need to be considered when using this protein profiling technique.
ISRAEL JOURNAL OF CHEMISTRY
(2023)
Review
Biochemistry & Molecular Biology
Soe Maung Maung Phone Myint, Liou Y. Sun
Summary: L-serine is a crucial amino acid involved in protein synthesis, cell proliferation, development, and sphingolipid formation in the central nervous system. It has neuroprotective and anti-inflammatory effects by activating glycine receptors and upregulating PPAR-γ. L-serine has potential as a protective agent in various neurological diseases and neurodegenerative disorders.
Article
Biochemistry & Molecular Biology
Marco Mangiagalli, Alberto Barbiroli, Carlo Santambrogio, Cristian Ferrari, Marco Nardini, Marina Lotti, Stefania Brocca
Summary: The study investigates the dimerization mechanism of the psychrophilic acyl aminoacyl peptidase from Sporosarcina psychrophila, revealing the importance of the A1 helix in maintaining the quaternary structure and activity.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2021)
Article
Biochemistry & Molecular Biology
Renia Fotiadou, Dimitrios Lefas, Despina Vougiouklaki, Aliki Tsakni, Dimitra Houhoula, Haralambos Stamatis
Summary: Enzymatic lipophilization using immobilized lipase on biogenic nanoparticles was employed to prepare modified oils rich in structured phenolipids. The effects of temperature and enzyme concentration on the bioprocess efficiency and nanobiocatalyst reusability were investigated. The modified oils showed enhanced antioxidant activity and improved oxidative stability. A fortified mayonnaise containing the modified oil exhibited increased stability compared to the control mayonnaise. Enzymatically modified oils have great potential for applications in the nutraceutical and food industry.
Article
Microbiology
Robert W. B. Brown, Aabha Sharma, Miguel Rey Villanueva, Xiaomo Li, Ouma Onguka, Leeor Zilbermintz, Helen Nguyen, Ben A. Falk, Cheryl L. Olson, Joann M. Taylor, Conrad L. Epting, Rahul S. Kathayat, Neri Amara, Bryan C. Dickinson, Matthew Bogyo, David M. Engman
Summary: Dynamic post-translational modifications in eukaryotic cells allow rapid and specific regulation of protein functions. The S-acylation process involves reversible lipid modification of proteins, while depalmitoylation is necessary for acylation homeostasis. The identification of a homologue of human APT1 in Trypanosoma brucei, named TbAPT-L, suggests a lipase function rather than depalmitoylase activity, with modulation of TbAPT-L showing no effect on parasite growth or cellular depalmitoylation activity in vitro.
Article
Chemistry, Multidisciplinary
Nicholas G. S. McGregor, Joan Coines, Valentina Borlandelli, Satoko Amaki, Marta Artola, Alba Nin-Hill, Daniel Linzel, Chihaya Yamada, Takatoshi Arakawa, Akihiro Ishiwata, Yukishige Ito, Gijsbert A. van der Marel, Jeroen D. C. Codee, Shinya Fushinobu, Herman S. Overkleeft, Carme Rovira, Gideon J. Davies
Summary: The discovery of zinc-dependent retaining glycoside hydrolases presents unresolved mechanistic questions, particularly the controversy surrounding the proposed mechanism involving a zinc-coordinated cysteine nucleophile and a thioglycosyl enzyme intermediate. A synthesized beta-l-arabinofuranosidase inhibitor reacts exclusively with the cysteine thiol catalytic nucleophiles of GH families 127 and 146, supporting further research into the breakdown of the thioglycosyl enzyme intermediate. X-ray crystal structures and simulations provide insight into the mechanisms of zinc-coordinated cysteine as the catalytic nucleophile and the energetics of this unique metalloenzyme clan.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2021)
Article
Biochemistry & Molecular Biology
Cory L. Brooks, David A. Ostrov, Nicholas C. Schumann, Schuchi Kakkad, Danmeng Li, Karla Pena, Brady Paul Williams, Nathan E. Goldfarb
Summary: This study presents the crystal structure of the apo form of the hydrolase Hip1, revealing insights into the active site architecture of this drug target. By co-crystallizing Hip1 with the irreversible serine protease inhibitor AEBSF, the researchers discovered a mechanism for the conversion of the enzyme to an anhydro form. They also provide a comparative analysis of the structures of anhydrohip1 and Hip1, propose a mechanism for ligand-induced conformational changes, and expand upon the putative lipid binding pocket in the enzyme. These findings are valuable for the structure-based drug design of novel therapeutics targeting Hip1 in M. tuberculosis.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2022)
Review
Chemistry, Multidisciplinary
Brittney Racioppo, Nan Qiu, Alexander Adibekian
Summary: Protein profiling and probe development in the field of serine hydrolases are crucial for studying biological processes. The use of activity-based protein profiling and probes has expanded our understanding of the SH proteome and led to the development of selective inhibitors and imaging agents with broad applications.
ISRAEL JOURNAL OF CHEMISTRY
(2023)
Review
Cell Biology
Alessandro Papa, Silvia Pasquini, Chiara Contri, Sandra Gemma, Giuseppe Campiani, Stefania Butini, Katia Varani, Fabrizio Vincenzi
Summary: Polypharmacology challenges the traditional paradigm of one-drug, one target, one disease by using multitarget compounds for the treatment of complex diseases. The endocannabinoid system is an attractive therapeutic target in central nervous system disorders and neurodegenerative diseases.
