Article
Endocrinology & Metabolism
Jenna Elizabeth Hunt, Bolette Hartmann, Kristina Schoonjans, Jens Juul Holst, Hannelouise Kissow
Summary: The study investigated the impact of a fiber-deficient diet on intestinal health and found that a lack of fiber led to changes in intestinal morphology, decreased secretion of gut hormones, and increased intestinal permeability.
FRONTIERS IN ENDOCRINOLOGY
(2021)
Article
Gastroenterology & Hepatology
Julia Leonhardt, Raphael S. Haider, Christoph Sponholz, Silke Leonhardt, Julia Drube, Katrin Spengler, Diana Mihaylov, Sophie Neugebauer, Michael Kiehntopf, Nevin A. Lambert, Andreas Kortgen, Tony Bruns, Frank Tacke, Carsten Hoffmann, Michael Bauer, Regine Heller
Summary: The study found that serum bile acids in patients with liver failure can activate TGR5, leading to compromised monocyte function and reduced response to bacterial challenge, which is significantly associated with mortality.
CELLULAR AND MOLECULAR GASTROENTEROLOGY AND HEPATOLOGY
(2021)
Article
Gastroenterology & Hepatology
Qiaoling Wang, Huibin Lin, Chongrong Shen, Minchun Zhang, Xingyu Wang, Miaomiao Yuan, Mingyang Yuan, Sheng Jia, Zhiwen Cao, Chao Wu, Banru Chen, Aibo Gao, Yufang Bi, Guang Ning, Weiqing Wang, Jiqiu Wang, Ruixin Liu
Summary: The gut microbiota regulates the release of postprandial GLP-1 through microbial metabolites, highlighting the essential interaction between gut microbiota and host in maintaining intestinal function and health.
Article
Endocrinology & Metabolism
Neil Tanday, Ryan A. Lafferty, Peter R. Flatt, Nigel Irwin
Summary: Sequential administration of SL-PYY and liraglutide showed improvements in energy intake, body weight, glucose and insulin levels in diabetic mice. Additionally, the combination therapy enhanced insulin sensitivity and modulated pancreatic hormones, suggesting potential as a treatment option for diabetes.
DIABETES OBESITY & METABOLISM
(2022)
Article
Cell Biology
Michele Biagioli, Silvia Marchiano, Rosalinda Roselli, Cristina Di Giorgio, Rachele Bellini, Martina Bordoni, Eleonora Distrutti, Bruno Catalanotti, Angela Zampella, Luigina Graziosi, Annibale Donini, Stefano Fiorucci
Summary: This study investigates the regulation of ACE2 expression in Crohn's disease patients and rodent models of colitis. The results suggest that ACE2 expression is regulated by TNF-α and GLP-1, and GPBAR1 acts as a positive modulator of ACE2.
Article
Endocrinology & Metabolism
Charlotte Bayer Christiansen, Simon Veedfald, Bolette Hartmann, Astrid Marie Gauguin, Soren Moller, Thomas Moritz, Sten Madsbad, Jens Juul Holst
Summary: Colon evacuation significantly reduced lactulose fermentation but did not change hormone releases in this study, suggesting that colonic luminal contents may not sufficiently affect colonic L-cell secretion. Further investigation is needed to determine the impact of colonic contribution to gut hormone concentrations.
JOURNAL OF CLINICAL ENDOCRINOLOGY & METABOLISM
(2022)
Article
Critical Care Medicine
Julia Leonhardt, Mirrin J. Dorresteijn, Sophie Neugebauer, Diana Mihaylov, Julia Kunze, Ignacio Rubio, Frank-Stephan Hohberger, Silke Leonhardt, Michael Kiehntopf, Klaus Stahl, Christian Bode, Sascha David, Frank A. D. T. G. Wagener, Peter Pickkers, Michael Bauer
Summary: The study found that circulating bile acids capable of inducing immunosuppression are present in septic shock patients, particularly in those with severe liver failure. Future research may need to explore whether modulating bile acid metabolism can improve the clinical course and outcome of sepsis in these patients.
Article
Immunology
Fengyuan Tian, Wangda Xu, Lan Chen, Tianxi Chen, Xiaohong Feng, Jie Chen, Danning Wei, Qi Huang
Summary: The study suggests that TGR5 can modulate the abundance of L-cells to enhance GLP-1 release through YAP-driven intestinal regeneration, alleviating incretin impairment in T2DM.
INTERNATIONAL IMMUNOPHARMACOLOGY
(2022)
Article
Medicine, General & Internal
Brittany Galuppo, Giuseppina Rosaria Umano, Zhongyao Li, Michelle Van Name, Stephanie L. Samuels, C. Lawrence Kien, Gary W. Cline, David A. Wagner, Emiliano Barbieri, Domenico Trico, Nicola Santoro
Summary: A study of youth aged 15 to 22 found that obesity and insulin resistance may be associated with colonic fermentation of dietary fibers, acetate production, gut-derived hormone secretion, and adipose tissue lipolysis. Compared to lean and insulin-sensitive groups, insulin-resistant youth had minimal metabolic modifications.
Article
Biology
Daniel Sanford, Leon Luong, John P. Vu, Suwan Oh, Arielle Gabalski, Michael Lewis, Joseph R. Pisegna, Patrizia Germano
Summary: This study is the first to comprehensively characterize the effects of VPAC1R on phenotype, metabolism, calorimetry, and homeostasis in a null murine model. The results demonstrate that VPAC1R(-/-) mice exhibit altered metabolism and insulin intolerance, as well as changes in feeding behavior, energy expenditure, and plasma metabolic hormone levels.
Article
Cell Biology
Lauren A. Jones, Emily W. Sun, Amanda L. Lumsden, Daniel W. Thorpe, Rochelle A. Peterson, Dayan De Fontgalland, Luigi Sposato, Philippa Rabbitt, Paul Hollington, David A. Wattchow, Damien J. Keating
Summary: The lining of our intestinal surface contains hormone-producing cells that can sense and respond to the internal environment in our gut. In this study, it is found that GLP-1 and PYY release is greater in the distal regions of the human colon and is negatively correlated with body mass index in the small intestine. Additionally, aging is associated with decreased secretion of GLP-1 and PYY in the large intestine.
MOLECULAR AND CELLULAR ENDOCRINOLOGY
(2023)
Article
Nutrition & Dietetics
Tetsuro E. Okada, Tony Quan, Marc R. Bomhof
Summary: This study investigated the effects of ketone ester on appetite-related hormones and appetite perception after exercise, finding that although ketone ester altered homeostatic regulators of appetite, it did not acutely affect energy intake during the post-exercise period in healthy adults.
FRONTIERS IN NUTRITION
(2021)
Article
Chemistry, Medicinal
Sheng-Li Wu, Chen-Chen Zhang, Ji-Jun Chen, Xue-Mei Zhang, Min Guan, Chang-An Geng
Summary: This study isolated a unique stilbene trimer-flavonoid hybrid called paeonilactiflobenoid (1) from the seeds of Paeonia lactiflora, along with six known stilbenes (2-7). It was found that compounds 2-7 had stimulative effects on GLP-1 secretion, with higher potency than the positive control oleoylethanolamide. Additionally, compounds 4 and 6 exhibited agonistic activity on the GPCR TGR5, indicating their potential as GLP-1 secretagogues.
Article
Gastroenterology & Hepatology
Emily W. Sun, Eva W. Iepsen, Nektaria Pezos, Amanda L. Lumsden, Alyce M. Martin, Gudrun Schober, Nichole J. Isaacs, Christopher K. Rayner, Nam Q. Nguyen, Dayan de Fontgalland, Philippa Rabbitt, Paul Hollington, David A. Wattchow, Torben Hansen, Jens-Christian Holm, Alice P. Liou, V. Margaret Jackson, Signe S. Torekov, Richard L. Young, Damien J. Keating
Summary: This study revealed a previously unidentified signaling nexus in the human gastrointestinal tract involving the release of a-MSH and the activation of MC4R on L cells in an autocrine and paracrine fashion. The findings have direct implications for targeting mucosal MC4R as a treatment for human metabolic disorders.
Article
Food Science & Technology
Shima Hajipoor, Azita Hekmatdoost, Yahya Pasdar, Reza Mohammadi, Meysam Alipour, Mansour Rezaie, Seyed Mostafa Nachvak, Celso Fasura Balthazar, Mohammad Reza Sobhiyeh, Amir Mohammad Mortazavian, Adriano G. Cruz
Summary: This study aimed to evaluate the synergistic effect of probiotics and vitamin D in yogurt matrix on weight management. The results showed that PY had the most significant effect, while vitamin D-fortified yogurt had the largest impact on vitamin D levels.
FOOD SCIENCE & NUTRITION
(2022)
Article
Chemistry, Multidisciplinary
Zheliang Yuan, Matthew B. Nodwell, Hua Yang, Noeen Malik, Helen Merkens, Francois Benard, Rainer E. Martin, Paul Schaffer, Robert Britton
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2018)
Article
Radiology, Nuclear Medicine & Medical Imaging
Matthew B. Nodwell, Hua Yang, Helen Merkens, Noeen Malik, Milena Colovic, Bjorn Wagner, Rainer E. Martin, Francxois Benard, Paul Schaffer, Robert Britton
JOURNAL OF NUCLEAR MEDICINE
(2019)
Review
Endocrinology & Metabolism
Sara L. Jepsen, Kaare Grunddal, Nicolai J. Wewer Albrechtsen, Maja S. Engelstoft, Maria B. N. Gabe, Elisa P. Jensen, Cathrine Orskov, Steen S. Poulsen, Mette M. Rosenkilde, Jens Pedersen, Fiona M. Gribble, Frank Reimann, Carolyn F. Deacon, Thue W. Schwartz, Andreas D. Christ, Rainer E. Martin, Jens J. Holst
AMERICAN JOURNAL OF PHYSIOLOGY-ENDOCRINOLOGY AND METABOLISM
(2019)
Article
Biochemistry & Molecular Biology
Patrick Schnider, Cosimo Dolente, Henri Stalder, Rainer E. Martin, Viktoria Reinmueller, Roman Marty, Caroline Wyss Gramberg, Bjorn Wagner, Holger Fischer, Andre M. Alker, Klaus Mueller
Article
Chemistry, Multidisciplinary
Josiah Newton, Daniel Driedger, Matthew B. Nodwell, Paul Schaffer, Rainer E. Martin, Robert Britton, Chadron M. Friesen
CHEMISTRY-A EUROPEAN JOURNAL
(2019)
Article
Chemistry, Physical
Zheliang Yuan, Hua Yang, Noeen Malik, Milena Colovic, David S. Weber, Darryl Wilson, Francois Benard, Rainer E. Martin, Jeffrey J. Warren, Paul Schaffer, Robert Britton
Article
Biochemistry & Molecular Biology
Leona T. Y. Ho, Anja Osterwald, Iris Ruf, Daniel Hunziker, Patrizio Mattei, Pratap Challa, Robin Vann, Christoph Ullmer, Ponugoti Vasanth Rao
BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR BASIS OF DISEASE
(2020)
Article
Chemistry, Organic
Josiah J. Newton, Benson J. Jelier, Michael Meanwell, Rainer E. Martin, Robert Britton, Chadron M. Friesen
Article
Medicine, Research & Experimental
Sara L. Jepsen, Nicolai J. Wewer Albrechtsen, Johanne Agerlin Windelov, Katrine D. Galsgaard, Jenna Elizabeth Hunt, Thomas B. Farb, Hannelouise Kissow, Jens Pedersen, Carolyn F. Deacon, Rainer E. Martin, Jens J. Holst
Summary: The study demonstrates that selective SSTR antagonists can improve glucose control primarily through the intestinal GLP-1 system in mice.
Article
Pharmacology & Pharmacy
Daniel Hunziker, Sabrina Reinehr, Marina Palmhof, Natalie Wagner, Thomas Biniasch, Gesa Stute, Patrizio Mattei, Petra Schmitz, Patrick DiGiorgio, Jerome Hert, Markus G. Rudolph, Joerg Benz, Martine Stihle, Bernard Gsell, Stephan Mueller, Rodolfo Gasser, Nina Schonhoven, Christoph Ullmer, Stephanie C. Joachim
Summary: The dysregulation of the autotaxin-lysophosphatidic acid (ATX-LPA) signaling pathway is suggested to contribute to glaucoma pathogenesis. In this study, a new ATX-inhibitor was developed and shown to reduce retinal ganglion cell (RGC) loss in two glaucoma models. These findings suggest that the dysregulation of the ATX-LPA axis may be an additional factor contributing to RGC loss in glaucoma patients.
FRONTIERS IN PHARMACOLOGY
(2022)
Article
Chemistry, Multidisciplinary
Josiah J. Newton, Gokce Engudar, Alan J. Brooke, Matthew B. Nodwell, Holly Horngren-Rhodes, Rainer E. Martin, Paul Schaffer, Robert Britton, Chadron M. Friesen
Summary: This article describes a unique and general process for O-H, N-H, and C-H difluoromethylation, involving the formation of a transient dithiole and facile desulfurative fluorination using silver(I) fluoride. The process is compatible with a wide range of functional groups and can be used for fluorine-18 labeling. It is expected to inspire new efforts in medicinal chemistry, agrochemistry, and radiotracer production.
CHEMISTRY-A EUROPEAN JOURNAL
(2023)
Article
Biochemical Research Methods
Tatjana Sela, Mads Manso, Michel Siegel, Celine Marban-Doran, Axel Ducret, Jens Niewoehner, Jacob Ravn, Rainer E. Martin, Annika Sommer, Sabine Lohmann, Ben-Fillippo Krippendorff, Mette Ladefoged, Annette Indlekofer, Tom Quaiser, Florian Bueddefeld, Erich Koller, Mohamed Y. Mohamed, Tobias Oelschlaegel, Kurt V. Gothelf, Kerstin Hofer, Felix F. Schumacher
Summary: This study demonstrates the key role of conjugate design in creating promising drug delivery vehicles for antisense-oligonucleotides (ASOs). By conjugating ASOs to antibodies, access to the central nervous system (CNS) can be facilitated after peripheral application and target engagement at the blood-brain barrier. The results of this study provide a blueprint for the design of peripherally delivered ASO-based drugs for the CNS in the future.
BIOCONJUGATE CHEMISTRY
(2023)
Article
Medicine, Research & Experimental
Anne-Gaelle Reinhart, Anja Osterwald, Philippe Ringler, Yael Leiser, Matthias E. Lauer, Rainer E. Martin, Christoph Ullmer, Felix Schumacher, Claudia Korn, Michael Keller
Summary: mRNA LNPs, as a novel vaccine carrier, require frozen storage and transportation conditions to maintain their full functionality. This study aims to assess the stability and in vitro delivery of LNPs under nonfrozen storage conditions. The findings suggest that LNPs can retain activity under certain conditions, but the effectiveness may vary with different lipid formulations and temperatures. Further research on the relationship between nanoparticle structure and activity is crucial to overcome storage and stability limitations.
MOLECULAR PHARMACEUTICS
(2023)
Article
Chemistry, Multidisciplinary
David F. Nippa, Kenneth Atz, Alex T. Mueller, Jens Wolfard, Clemens Isert, Martin Binder, Oliver Scheidegger, David B. Konrad, Uwe Grether, Rainer E. Martin, Gisbert Schneider
Summary: This study combines high-throughput experimentation and computational graph neural networks to identify suitable substrates for late-stage C-H alkylation. The results demonstrate the feasibility of using high-throughput experimentation and machine learning for virtual reaction screening, providing potential candidates for further optimization of drug molecules.
COMMUNICATIONS CHEMISTRY
(2023)
Article
Chemistry, Multidisciplinary
David F. Nippa, Kenneth Atz, Remo Hohler, Alex T. Muller, Andreas Marx, Christian Bartelmus, Georg Wuitschik, Irene Marzuoli, Vera Jost, Jens Wolfard, Martin Binder, Antonia F. Stepan, David B. Konrad, Uwe Grether, Rainer E. Martin, Gisbert Schneider
Summary: A late-stage functionalization platform based on geometric deep learning and high-throughput experimentation was developed, enabling the optimization of complex drug molecules. The computational model accurately predicted reaction outcomes, yields, and regioselectivity, reducing the need for de novo synthesis.
Article
Chemistry, Medicinal
Shibin Zhao, Julian Maceren, Mia Chung, Samantha Stone, Raphael Geiben, Melissa L. Boby, Bradley S. Sherborne, Derek S. Tan
Summary: Antibiotic resistance is a major threat to public health, with Gram-negative bacteria presenting unique challenges due to their low permeability and efflux pumps. Limited understanding of the chemical rules for overcoming these barriers hinders antibacterial drug discovery. Efforts to address this issue, such as screening compound libraries and using cheminformatic analysis, have led to the design of sulfamidoadenosines with diverse substituents, showing potential utility in accumulation in Escherichia coli.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Jichun Li, Qing Li, Shuai Xia, Jiahuang Tu, Longbo Zheng, Qian Wang, Shibo Jiang, Chao Wang
Summary: This study successfully developed a short peptide mimetic as a MERS-CoV fusion inhibitor by reproducing the key recognition features of the HR2 helix. The resulting 23-mer lipopeptide showed comparable inhibitory effect to the 36-mer HR2 peptide HR2P-M2. This has important implications for developing short peptide-based antiviral agents to treat MERS-CoV infection.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Krista Jaunsleine, Linda Supe, Jana Spura, Sten van Beek, Anna Sandstrom, Jessica Olsen, Carina Halleskog, Tore Bengtsson, Ilga Mutule, Benjamin Pelcman
Summary: Beta(2)-adrenergic receptor agonists can stimulate glucose uptake by skeletal muscle cells and are therefore potential treatments for type 2 diabetes. The chirality of compounds has a significant impact on the activity of these agonists. This study found that certain synthesized compounds showed higher glucose uptake activity. These findings provide important information for the design of novel beta(2)AR agonists for T2D treatment.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Xin Xu, Jia Chen, Guan Wang, Xiaojuan Zhang, Qiang Li, Xiaobo Zhou, Fengying Guo, Min Li
Summary: The study focuses on EZH2, a promising therapeutic target for various types of cancers. Researchers designed and synthesized a series of novel derivatives aiming to enhance the EZH2 inhibition activity. Among them, compound 28 displayed potent EZH2 inhibition activity and showed high anti-proliferative effects in lymphoma cell lines and xenograft mouse models. The study suggests that compound 28 has potential as a therapeutic candidate for EZH2-associated cancers.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Wei Zhang, Wei Liu, Ya-Dong Zhao, Li-Zi Xing, Ji Xu, Rui-Jun Li, Yun-Xiao Zhang
Summary: This study developed a series of aromatic amide derivatives based on Rhein and investigated their inhibitory activity against alpha-Syn aggregation. Two of these compounds showed promising potential in treating Parkinson's disease by stabilizing alpha-Syn's conformation and disassembling alpha-Syn oligomers and fibrils.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Mani Sharma, S. S. S. S. Sudha Ambadipudi, Neeraj Kumar Chouhan, V. Lakshma Nayak, Srihari Pabbaraja, Sai Balaji Andugulapati, Ramakrishna Sistla
Summary: Therapeutically active lipids in drug delivery systems can enhance the safety and efficacy of treatment. The liposome formulation created using synthesized biologically active lipids showed additive anti-cancer effects and reduced tumorigenic potential.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
