Article
Endocrinology & Metabolism
Karol M. Pencina, Arthur L. Burnett, Thomas W. Storer, Wen Guo, Zhuoying Li, Adam S. Kibel, Grace Huang, Michelle Blouin, Donna L. Berry, Shehzad Basaria, Shalender Bhasin
Summary: This study evaluated the safety and efficacy of a selective androgen receptor modulator (OPK-88004) in androgen-deficient men who had undergone radical prostatectomy for organ-confined prostate cancer. The results showed that OPK-88004 increased lean body mass and decreased fat mass significantly, but did not improve sexual symptoms or physical performance.
JOURNAL OF CLINICAL ENDOCRINOLOGY & METABOLISM
(2021)
Article
Biochemistry & Molecular Biology
Tristan Moeller, Hui-Chung Wen, Nana Naumann, Oliver Krug, Mario Thevis
Summary: Selective androgen receptor modulators (SARMs) are a new class of drugs with potential for anabolic effects on muscle and bone, but with reduced side effects due to their tissue-selective mode of action. They are prohibited by the World Anti-Doping Agency (WADA) in sports due to their performance-enhancing properties. Continuous research into SARMs is necessary in the field of doping controls, as the number of adverse findings and total number of SARMs has increased since their inclusion in the WADA Prohibited List in 2008. The synthesis, characterization, and biotransformation of a novel SARM candidate, SARM 2f, were described in this study, with the aim of improving anti-doping efforts through testing procedures.
Article
Endocrinology & Metabolism
Luca Giovanelli, Richard Quinton
Summary: This review examines the available data on the therapeutic effects of androgens and selective androgen receptor modulators (SARMs) for cachexia, a complex wasting syndrome associated with various end-stage chronic diseases. Despite promising results, no approved drug has been found to date.
BEST PRACTICE & RESEARCH CLINICAL ENDOCRINOLOGY & METABOLISM
(2022)
Article
Cell Biology
Olivier Le Bacquer, Kassandra Lanchais, Kristell Combe, Loic Van Den Berghe, Stephane Walrand
Summary: Sarcopenia, age-related muscle loss, is associated with changes in skeletal muscle protein homeostasis, which may be regulated by the endocannabinoid system. The CB1 receptor antagonist rimonabant stimulates protein synthesis independently of CB1, suggesting potential for treating sarcopenia.
JOURNAL OF CELLULAR PHYSIOLOGY
(2021)
Article
Multidisciplinary Sciences
Tatsuya Hosoi, Mitsutaka Yakabe, Hiroko Sasakawa, Takayoshi Sasako, Kohjiro Ueki, Shigeaki Kato, Suzumi M. Tokuoka, Yoshiya Oda, Masahiro Abe, Toshio Matsumoto, Masahiro Akishita, Sumito Ogawa
Summary: Sarcopenia, a type of muscle degeneration, is closely linked to a shift in muscle fiber type. The function of androgen receptor (AR) pathway in sarcopenia is not well understood. In a mouse model, selectively deleting AR in fast-twitch muscle fibers resulted in reduced muscle strength and fatigue resistance, as well as a shift from fast-twitch to slow-twitch fibers. These findings suggest that AR pathway plays a crucial role in muscle composition and function, specifically in fast-twitch fibers.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
(2023)
Article
Chemistry, Analytical
Malin Nilsson Broberg, Heather Knych, Ulf Bondesson, Curt Pettersson, Borje Tidstedt, Scott Stanley, Mario Thevis, Mikael Hedeland
Summary: This study analyzed the in vivo metabolite profile of LGD-3303 and identified suitable new targets for equine doping control. A total of eight metabolites of LGD-3303 were identified, including one mono-hydroxylated metabolite suggested as an analytical target.
JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
(2023)
Article
Medicine, General & Internal
Sohaib Khan, Jaclyn Fackler, Asma Gilani, Stephanie Murphy, Lirio Polintan
Summary: Selective androgen receptor modulators (SARMs) are developed as an alternative to traditional synthetic steroids, with favorable effects on bones and muscles without androgenic side effects. Despite being popular among athletes and bodybuilders, the FDA has warned of their potential side effects including liver injury.
CUREUS JOURNAL OF MEDICAL SCIENCE
(2022)
Article
Biochemistry & Molecular Biology
Felicitas Wagener, Luisa Euler, Christian Goergens, Sven Guddat, Mario Thevis
Summary: This study investigated the excretion of RAD140 in human body using LC-HRMS/MS technology and described multiple metabolites. The findings contribute to better management of doping cases involving RAD140.
Article
Neurosciences
Xuzhu Lin, Cassandra Smith, Alba Moreno-Asso, Navabeh Zarekookandeh, Tara C. Brennan-Speranza, Gustavo Duque, Alan Hayes, Itamar Levinger
Summary: This study investigates the protective effects of the combination of undercarboxylated osteocalcin (ucOC) and ibandronate (IBN) against immobilization-induced muscle wasting and insulin resistance. The results show that the combined treatment significantly increases muscle weight and improves glucose tolerance compared to individual treatments.
JOURNAL OF PHYSIOLOGY-LONDON
(2023)
Review
Biotechnology & Applied Microbiology
Kai Sun, Shunyao Li, Youbin Si, Qingguo Huang
Summary: This article provides a comprehensive overview of laccase-triggered anabolism, from fundamental theory to biotechnology applications. Laccase can participate in anabolic processes in vivo to create multifarious functional biopolymers, such as fungal pigments, plant lignins, and insect cuticles, using mono/polyphenols and their derivatives as enzymatic substrates. Advanced biotechnology applications in vitro through fungal laccase-triggered macromolecular biosynthesis may provide a key research direction towards the rational design of green chemistry.
CRITICAL REVIEWS IN BIOTECHNOLOGY
(2021)
Article
Biochemistry & Molecular Biology
Johanna Abrigo, Hugo Olguin, Danae Gutierrez, Franco Tacchi, Marco Arrese, Daniel Cabrera, Mayalen Valero-Breton, Alvaro A. Elorza, Felipe Simon, Claudio Cabello-Verrugio
Summary: This study aimed to evaluate the impact of deoxycholic acid (DCA) and cholic acid (CA) on mitochondrial mass and function in muscle fibers and investigate the role of the TGR5 receptor. The results indicated that DCA and CA decreased mitochondrial mass, DNA, and potential in a TGR5-dependent fashion, and also reduced the oxygen consumption rate and complexes I and II from the mitochondrial electron transport chain. DCA and CA generated more mitochondrial reactive oxygen species than the control, which were abolished in TGR5(-/-) mice muscle fibers.
Article
Endocrinology & Metabolism
Daniel B. B. Hoffmann, Christoph Derout, Max Mueller-Reiter, Kai O. O. Boeker, Arndt F. F. Schilling, Paul J. J. Roch, Wolfgang Lehmann, Dominik Saul, Thelonius Hawellek, Stefan Taudien, Stephan Sehmisch, Marina Komrakova
Summary: The effect of ligandrol on bone tissue was investigated in ovariectomized rat model. The results showed that a high dose of ligandrol had a subtle anabolic effect on structural properties of osteoporotic bones, but no improvement in biomechanical properties.
JOURNAL OF BONE AND MINERAL METABOLISM
(2023)
Article
Nutrition & Dietetics
Marianna Rabelo de Carvalho, Ellen Fernandes Duarte, Maria Lua Marques Mendonca, Camila Souza de Morais, Gabriel Elias Ota, Jair Jose Gaspar-Junior, Wander Fernando de Oliveira Filiu, Felipe Cesar Damatto, Marina Politi Okoshi, Katashi Okoshi, Rodrigo Juliano Oliveira, Paula Felippe Martinez, Silvio Assis de Oliveira-Junior
Summary: This study evaluated the impact of creatine supplementation on the myostatin pathway and myosin heavy chain isoforms in resistance-trained rats. Resistance training alone increased muscle weight, cross-sectional area, and collagen fraction, as well as MyHC IIx and follistatin expressions, while reducing myostatin and ActRIIB expressions. Creatine supplementation did not affect these effects.
Article
Chemistry, Physical
Alexandru Turza, Gheorghe Borodi, Maria Miclaus, Marieta Muresan-Pop
Summary: This study provides a detailed analysis of the polymorphic structures of the synthetic agent YK11, with three crystal structures determined by single crystal X-ray diffraction. The crystal features were analyzed using crystal lattice and intermolecular interaction energies, and other experimental techniques were used for verification.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Review
Nutrition & Dietetics
Ellis Hall, Misha F. F. Vrolijk
Summary: This article reviews the interaction between selective androgen receptor modulators (SARMs) and the androgen receptor (AR) on cardiovascular health. It is found that SARMs may increase the risk of cardiovascular diseases through multiple factors, including the renin-angiotensin system, smooth muscle cells, sympathetic nervous system, lipid profile, inflammation, and platelet activity. However, there is a lack of clinical trials and literature on the relationship between SARMs, cardiovascular diseases, and the AR. More research is needed to understand the mechanisms and risk factors.
Article
Chemistry, Medicinal
Nicolas Desroy, Christopher Housseman, Xavier Bock, Agnes Joncour, Natacha Bienvenu, Laetitia Cherel, Virginie Labeguere, Emilie Rondet, Christophe Peixoto, Jean-Marie Grassot, Olivier Picolet, Denis Annoott, Nicolas Triballeau, Alain Monjardet, Emanuelle Wakselman, Veronique Roncoroni, Sandrine Le Tallec, Roland Blanque, Celine Cottereaux, Nele Vandervoort, Thierry Christophe, Patrick Mollat, Marieke Lamers, Marielle Auberval, Boska Hrvacic, Jovica Ralic, Line Oste, Ellen van der Aar, Reginald Brys, Bertrand Heckmann
JOURNAL OF MEDICINAL CHEMISTRY
(2017)
Article
Chemistry, Medicinal
Frederic Labeguere, Sonia Dupont, Luke Alvey, Florilene Soulas, Gregory Newsome, Amynata Tirera, Vanessa Quenehen, Thi Thu Trang Mai, Pierre Deprez, Roland Blanque, Line Oste, Sandrine Le Tallec, Steve De Vos, Annick Hagers, Ann Vandevelde, Luc Nelles, Nele Vandervoort, Katja Conrath, Thierry Christophe, Ellen van der Aar, Emanuelle Wakselman, Didier Merciris, Celine Cottereaux, Cecile da Costa, Laurent Saniere, Philippe Clement-Lacroix, Laura Jenkins, Graeme Milligan, Stephen Fletcher, Reginald Brys, Romain Gosmini
JOURNAL OF MEDICINAL CHEMISTRY
(2020)
Article
Chemistry, Medicinal
Franck Brebion, Romain Gosmini, Pierre Deprez, Marie Varin, Christophe Peixoto, Luke Alvey, Helene Jary, Natacha Bienvenu, Nicolas Triballeau, Roland Blanque, Celine Cottereaux, Thierry Christophe, Nele Vandervoort, Patrick Mollat, Robert Touitou, Philip Leonard, Frederic De Ceuninck, Iuliana Botez, Alain Monjardet, Ellen van der Aar, David Amantini
Summary: GLPG1972/S201086 is a potent and selective ADAMTS-5 inhibitor obtained through optimization of a promising hydantoin series. The compound has shown biochemical activity against rat and human ADAMTS-5, and demonstrated anticatabolic and anticatabolic activity.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Orthopedics
P. Clement-Lacroix, C. B. Little, M. M. Smith, C. Cottereaux, D. Merciris, S. Meurisse, P. Mollat, R. Touitou, F. Brebion, R. Gosmini, F. De Ceuninck, I Botez, L. Lepescheux, E. van der Aar, T. Christophe, N. Vandervoort, R. Blanque, D. Comas, P. Deprez, D. Amantini
Summary: GLPG1972/S201086 is a potent, selective, and orally available ADAMTS5 inhibitor that demonstrates significant protective efficacy on both cartilage and subchondral bone in preclinical OA models.
OSTEOARTHRITIS AND CARTILAGE
(2022)
Article
Cell Biology
Stephanie Lavazais, Manja Jargosch, Sonia Dupont, Frederic Labeguere, Christel Menet, Catherine Jagerschmidt, Frenz Ohm, Laszlo Kupcsik, Isabelle Parent, Celine Cottereaux, Florence Marsais, Line Oste, An Van de Water, Thierry Christophe, Steve De Vos, Padraic Fallon, Felix Lauffer, Philippe Clement-Lacroix, Kilian Eyerich, Reginald Brys
Summary: Innate immunity plays an important role in both environmental cue interpretation and adaptive responses, making modulators of innate immune responses potentially useful in treating immune-mediated inflammatory diseases. A selective IRAK4 inhibitor, GLPG2534, has been evaluated in various in vitro and in vivo models of inflammatory skin diseases, demonstrating inhibition of TLR and IL-1 responses in multiple cell types and dampening disease activity in murine models. Additionally, inhibiting IRAK4 reversed pathogenic molecular signatures in human lesional psoriasis and atopic dermatitis biopsies, highlighting its potential therapeutic strategy in chronic inflammatory skin diseases.
SCIENCE TRANSLATIONAL MEDICINE
(2023)
Article
Endocrinology & Metabolism
R Blanqué, C Cottereaux, CR Gardner
CALCIFIED TISSUE INTERNATIONAL
(2001)
Article
Biochemistry & Molecular Biology
CR Gardner, R Blanqué, C Cottereaux
PROSTAGLANDINS LEUKOTRIENES AND ESSENTIAL FATTY ACIDS
(2001)