Article
Biochemistry & Molecular Biology
Zeyana M. Al-Dahmani, Mojgan Hadian, Angel J. Ruiz-Moreno, Sabogal-Guaqueta Angelica Maria, Fernando A. Batista, Ran Zhang, Yang Luo, Afsaneh Sadremomtaz, Robin van der Straat, Mette Spoor, Amalia M. Dolga, Frank J. Dekker, S. S. Alexander Domling, Harry van Goor, Matthew R. Groves
Summary: A small molecule activator of human TST, identified through screening, increases TST activity and may have therapeutic benefits for diabetes and obesity. Two distinct isomers and an allosteric mode of activation are required for full activation. Molecular docking and dynamics suggest an allosteric site for the activator's binding, and increased TST activity enhances mitochondrial respiration.
Article
Entomology
Bin Liu, Danyang Fu, Hang Ning, Ming Tang, Hui Chen
Summary: The Chinese white pine beetle, Dendroctonus armandi, is a destructive pest of coniferous forests in the middle Qinling Mountains of China. Research has shown that its food intake is regulated by the sNPF signaling pathway, and RNA interference knockdown of sNPF and sNPFR significantly increased mortality, reduced food intake, and body weight.
Article
Clinical Neurology
Anneke Kuipers, Marta Balasko, Erika Petervari, Andreas Koller, Susanne M. Brunner, Gert N. Moll, Barbara Kofler
Summary: This study describes the development of a novel ligand, M89b, with specificity for GAL(2)R and increased stability by modifying a galanin-related peptide. M89b significantly reduced food intake in rats and showed promising potential for clinical application.
Article
Multidisciplinary Sciences
Chris Cook, Nicolas Nunn, Amy A. Worth, David A. Bechtold, Todd Suter, Susan Gackeheimer, Lisa Foltz, Paul J. Emmerson, Michael A. Statnick, Simon M. Luckman
Summary: This study shows that central administration of QRFP increases food intake and locomotor activity without affecting energy expenditure or reward. Knocking out both QRFP receptor orthologs does not produce a metabolic phenotype, but both receptors are required for the effect of centrally administered QRFP. QRFP and orexin have overlapping effects on behavior, but QRFP also affects other appetitive behaviors. The feeding response to QRFP is dependent on orexin/hypocretin receptor signaling.
Article
Medicine, Research & Experimental
David A. Lomas, James A. Irving, Christopher Arico-Muendel, Svetlana Belyanskaya, Andrew Brewster, Murray Brown, Chun-wa Chung, Hitesh Dave, Alexis Denis, Nerina Dodic, Anthony Dossang, Peter Eddershaw, Diana Klimaszewska, Imran Haq, Duncan S. Holmes, Jonathan P. Hutchinson, Alistair M. Jagger, Toral Jakhria, Emilie Jigorel, John Liddle, Ken Lind, Stefan J. Marciniak, Jeff Messer, Margaret Neu, Allison Olszewski, Adriana Ordonez, Riccardo Ronzoni, James Rowedder, Martin Ruediger, Steve Skinner, Kathrine J. Smith, Rebecca Terry, Lionel Trottet, Iain Uings, Steve Wilson, Zhengrong Zhu, Andrew C. Pearce
Summary: The study identified small molecules that bind to and stabilize mutant alpha(1)-antitrypsin, blocking aberrant polymerisation and increasing secretion, providing a potential treatment for deficiency. Oral dosing in transgenic mice showed a significant increase in secretion without observable clearance of hepatic inclusions, demonstrating the potential of mutation ameliorating small molecules in treating the disease.
EMBO MOLECULAR MEDICINE
(2021)
Article
Biochemistry & Molecular Biology
Melika Loriamini, Melissa M. Lewis-Bakker, Kayluz Frias Boligan, Siming Wang, Mairead B. Holton, Lakshmi P. Kotra, Donald R. Branch
Summary: In our initial publication, we demonstrated that small molecules can inhibit phagocytosis based on in vitro testing of over 200 compounds. We found four hit molecules with pyrazole core structure in a chemical library screening. Further evaluation resulted in the selection of two lead compounds with negligible toxicity and high efficacy in inhibiting phagocytosis. The rational development of these discoveries will lead to the selection of a lead compound(s) for pre-clinical evaluation through independent synthesis and in vivo activities.
Review
Biology
Daniel Assan, Umar Farouk Mustapha, Huapu Chen, Zhiyuan Li, Yuhao Peng, Guangli Li
Summary: The Neuropeptide Y family, including Npy and Pyy, has been extensively studied in fish to understand mechanisms related to feeding, heart activity, and emotional regulation. These studies aid in determining feeding regimes and growth in aquaculture settings.
Article
Physiology
Bin Liu, Danyang Fu, Haiming Gao, Hang Ning, Yaya Sun, Hui Chen, Ming Tang
Summary: The study cloned NPF precursor and receptor genes in Chinese white pine beetle, finding that the NPF signaling pathway plays a significant positive role in regulating food intake, providing a potential target for sustainable management of this pest.
FRONTIERS IN PHYSIOLOGY
(2021)
Article
Multidisciplinary Sciences
Kyeong Seop Kim, Mi Ae Kim, Keunwan Park, Young Chang Sohn
Summary: The study found a high specificity of the neuropeptide F signaling system in Pacific abalone, with Hdh-NPFR responding specifically to Hdh-NPF. Phylogenetic analysis revealed a likely common ancestor between bilaterian NPF/NPY and their receptors, suggesting co-evolution of the ligand-receptor system. In vivo experiments showed that injection of Hdh-NPF peptide increased food consumption in abalone, supporting the role of the neuropeptide system in regulating feeding behavior.
SCIENTIFIC REPORTS
(2021)
Article
Cell Biology
Li-Bin Gao, Ya-Hong Wang, Zhi-Hua Liu, Yu Sun, Peng Cai, Qing Jing
Summary: The study demonstrated that the small molecule SR9009 effectively suppresses the senescence-associated secretory phenotype (SASP) by activating the NRF2 pathway, preventing cellular senescence. It also showed efficacy in inhibiting cellular aging and inflammation in mouse models.
Article
Pharmacology & Pharmacy
Xuxu Wei, Jiarui Yang, Simin Li, Boyuan Li, Mengzhen Chen, Yukang Lu, Xiang Wu, Zeyu Cheng, Xiaoyu Zhang, Zhao Chen, Chunxia Wang, Edwin Wang, Ruiqing Zheng, Xue Xu, Hongcai Shang
Summary: TAIGET is a user-friendly graphical web interface that assists non-expert users in virtual target identification and annotation, reducing the entry barrier.
FRONTIERS IN PHARMACOLOGY
(2022)
Article
Pharmacology & Pharmacy
Xianling Ning, Hailong Qi, Yuyao Yuan, Ridong Li, Yuanyuan Wang, Zhiqiang Lin, Yuxin Yin
Summary: In this study, a small molecule compound 8 was found to initiate ferroptosis and inhibit tumor growth. It was demonstrated that compound 8 may trigger ferroptosis by regulating VDAC3. This study provides new opportunities for developing ferroptosis inducers and has important implications for cancer therapy.
EUROPEAN JOURNAL OF PHARMACOLOGY
(2022)
Article
Cell Biology
Ke Lu, Xiaodan Jia, Jiaqi Wu, Qiuling Wang, Xu-Fang Liang
Summary: In this study, a npy2r-deficient medaka model was established using the CRISPR/Cas9 system. The deletion of npy2r resulted in an all-male medaka population and increased food intake. It also led to significant changes in the expression levels of appetite stimulating and anorexia factors. Moreover, npy2r deletion improved sociability and reduced anxiety-like behavior in medaka, accompanied by decreased expression levels of anxiety-related genes.
FRONTIERS IN CELL AND DEVELOPMENTAL BIOLOGY
(2023)
Review
Chemistry, Multidisciplinary
Sophia M. N. Hoenig, Christian Lemmen, Matthias Rarey
Summary: The superposition of small molecules is a crucial technique in molecular modeling and drug discovery for assessing similarity and understanding structure-activity relationships. Continuous development of new methods highlights the need for rigorous benchmarking.
WILEY INTERDISCIPLINARY REVIEWS-COMPUTATIONAL MOLECULAR SCIENCE
(2023)
Article
Food Science & Technology
Gaelle Boudry, Ilario Mennella, Olivia Menard, Regis Janvier, Isabelle Nogret, Ashkan Madadlou, Armelle Cahu, Laurence Le Normand, Eric Bobillier-Chaumont, Rosalia Ferracane, Paola Vitaglione, Didier Dupont, David Val-Laillet
Summary: This study investigated the effect of OEA delivery kinetics on appetite suppression using different forms of dairy snacks. The results showed that liquid snacks containing OEA significantly reduced the amount of food consumed by minipigs, while semi-solid snacks did not have the same effect. Further experiments suggested that enhanced release of OEA in liquid snacks may affect endocannabinoid and other related metabolism.
JOURNAL OF FUNCTIONAL FOODS
(2023)
Review
Pharmacology & Pharmacy
Mariana Rae, Mariana Lemos Duarte, Ivone Gomes, Rosana Camarini, Lakshmi A. Devi
Summary: OT and AVP exhibit opposite roles in modulating stress, anxiety, and social behaviors, potentially due to their high sequence homology with their receptors. The crosstalk between these peptides and receptors in vivo remains unclear, but understanding this interaction is essential for elucidating the roles of OT and AVP, as well as for therapeutic targets in treating human disorders.
BRITISH JOURNAL OF PHARMACOLOGY
(2022)
Article
Anesthesiology
Elaine F. Toniolo, Achla Gupta, Adriano C. Franciosi, Ivone Gomes, Lakshmi A. Devi, Camila S. Dale
Summary: The interaction between CB1R and opioid receptors may be targeted for the treatment of diabetic neuropathy. CB1R-MOR and CB1R-DOR complexes are involved in diabetic neuropathy, and the peptide endocannabinoid hemopressin shows potential as a therapeutic for this condition.
Article
Andrology
Abhishek Kumar, Subrata Kumar Ghosh, Rahul Katiyar, Amare Eshetu Gemeda, Rupali Rautela, Amarjeet Bisla, Neeraj Srivastava, Sanjeev Kumar Bhure, Huidrom Lakshmi Devi, Vikash Chandra
Summary: This study investigated the effects of Mito TEMPO and acetovanillone on the freezability of buffalo spermatozoa. The results showed that the addition of these compounds, either individually or in combination, significantly improved post-thaw semen quality.
Article
Pharmacology & Pharmacy
Seshat M. Mack, Ivone Gomes, Amanda K. Fakira, Mariana Lemos Duarte, Achla Gupta, Lloyd Fricker, Lakshmi A. Devi
Summary: PEN is an abundant neuropeptide that activates G protein-coupled receptor 83, playing a role in regulating feeding, reward, and anxiety-related behaviors. Different forms of PEN peptides and procholecystokinin-derived peptides can differentially activate GPR83, showing bias in signal transduction pathways.
MOLECULAR PHARMACOLOGY
(2022)
Article
Multidisciplinary Sciences
Ambre M. Bertholet, Andrew M. Natale, Paola Bisignano, Junji Suzuki, Andriy Fedorenko, James Hamilton, Tatiana Brustovetsky, Lawrence Kazak, Ryan Garrity, Edward T. Chouchani, Nickolay Brustovetsky, Michael Grabe, Yuriy Kirichok
Summary: Mitochondria generate heat through H+ leakage mediated by UCP1 and AAC. Protonophores induce H+ leakage, but their clinical application is limited. This study directly measured the effect of protonophores on H+ leakage and found that it is dependent on AAC and UCP1. Through molecular structure analysis and mathematical modeling, a mechanism of uncoupler-dependent H+ leakage through AAC is proposed.
Article
Biochemistry & Molecular Biology
Beatriz C. Moraes, Helder Ribeiro-Filho, Allan P. Roldao, Elaine F. Toniolo, Gustavo P. B. Carretero, German G. Sgro, Fernanda A. H. Batista, Damian E. Berardi, Victoria R. S. Oliveira, Rebeka Tomasin, Felipe M. Vieceli, Dimitrius T. Pramio, Alexandre B. Cardoso, Ana C. M. Figueira, Shaker C. Farah, Lakshmi A. Devi, Camila S. Dale, Paulo S. L. de Oliveira, Deborah Schechtman
Summary: Chronic pain is a major health issue, and finding new analgesics is important due to the addictive properties and side effects of opioids. This study investigated mutations in a gene associated with congenital insensitivity to pain with anhidrosis (CIPA) to identify potential drug targets. They developed a cell-permeable phosphopeptide that inhibited a specific signaling pathway and demonstrated pain relief effects.
Article
Reproductive Biology
Lakshmi H. Devi, Shital D. Nagargoje, Shriti Pandey, T. Yasotha, Vikash Chandra, Taru G. Sharma
Summary: This study investigates the impact of buffalo uterine epithelial cells and their conditioned medium on in vitro embryo production. The results show that co-culture of embryos with steroid treated UECs and their CM improves blastocyst and hatching rate.
Article
Neurosciences
Lloyd D. Fricker, Mariana Lemos Duarte, Andrei Jeltyi, Lindsay Lueptow, Amanda K. Fakira, Alexandre K. Tashima, Ute Hochgeschwender, William C. Wetsel, Lakshmi A. Devi
Summary: Carboxypeptidase E (CPE) is not a rate-limiting enzyme in the production of most neuropeptides, contrary to previous claims that small decreases in CPE activity contribute to obesity and other physiological effects.
Article
Biotechnology & Applied Microbiology
Bhairavi Tolani, Anna Celli, Yanmin Yao, Yong Zi Tan, Richard Fetter, Christina R. Liem, Adam J. de Smith, Thamiya Vasanthakumar, Paola Bisignano, Adam D. Cotton, Ian B. Seiple, John L. Rubinstein, Marco Jost, Jonathan S. Weissman
Summary: The study discovered a cytotoxic agent, 249C, that selectively targets Ras-mutant cancer cells and effectively inhibits tumor growth, offering a potential therapeutic strategy for cancers driven by specific KRAS mutations.
NATURE BIOTECHNOLOGY
(2022)
Article
Optics
R. Reddappa, L. Lakshmi Devi, Ch Basavapoornima, Shobha Rani Depuru, J. Kaewkhao, Wisanu Pecharapa, C. K. Jayasankar
Summary: Di-calcium silicate (Ca2SiO4) phosphors doped with various Ln(3+) ions were prepared using a high temperature solid-state reaction technique. The raw materials were derived from renewable sources instead of non-renewable minerals. The resulting phosphors exhibited strong and characteristic photoluminescence peaks, and their emission characteristics were quantified and found to be better than other phosphors derived from non-renewable minerals. Therefore, Ca2SiO4:Ln(3+) phosphors have the potential to be used in low-cost solid-state lighting devices while utilizing renewable agricultural and food waste materials effectively.
Meeting Abstract
Biochemistry & Molecular Biology
Ambre M. Bertholet, Andrew M. Natale, Paola Bisignano, Junji Suzuki, Andriy Fedorenko, James Hamilton, Tatiana Brustovetsky, Lawrence Kazak, Ryan Garrity, Edward T. Chouchani, Nickolay Brustovetsky, Michael Grabe, Yuriy Kirichok
BIOCHIMICA ET BIOPHYSICA ACTA-BIOENERGETICS
(2022)
Article
Chemistry, Medicinal
Ashif I. Bhuiyan, Athena H. Choi, Sarbani Ghoshal, Ugochi A. Adiele, Dibyendu Dana, Jun Yong Choi, Karl R. Fath, Tanaji T. Talele, Sanjai K. Pathak
Summary: In this study, a novel spirocyclic inhibitor (V8) of Nek2 kinase was identified through high-throughput virtual screening. It was shown to selectively inhibit Nek2 kinase activity and attenuate the signaling and phenotypes of highly aggressive cancer cell lines. V8 could be a promising lead compound for the development of potent and selective Nek2 inhibitors.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2023)
Meeting Abstract
Biophysics
Michael Grabe, Andrew M. Natale, Ambre M. Bertholet, Paola Bisignano, Yuriy V. Kirichok, Junji Suzuki
BIOPHYSICAL JOURNAL
(2022)
Review
Biochemistry & Molecular Biology
Dibyendu Dana, Tuhin Das, Athena Choi, Ashif I. Bhuiyan, Tirtha K. Das, Tanaji T. Talele, Sanjai K. Pathak
Summary: Nek2 kinase plays an important role in the signal transduction of cell proliferation, growth, and differentiation. It is tightly regulated during the cell cycle and its increased levels can lead to various cellular abnormalities and diseases, including tumor growth and metastasis. Recent studies have also revealed new roles of Nek2 in drug resistance, bone diseases, ciliopathies, immune and kidney diseases, and parasitic diseases such as malaria.
Article
Biochemistry & Molecular Biology
Lloyd D. Fricker, Alexandre K. Tashima, Amanda K. Fakira, Ute Hochgeschwender, William C. Wetsel, Lakshmi A. Devi
Summary: This study utilized a conditional disruption mouse model of the Cpe gene to identify specific forms of neuropeptides through peptidomics, revealing the specific forms of neuropeptides in cells with disrupted Cpe gene.
CELL CHEMICAL BIOLOGY
(2021)
