Article
Biochemistry & Molecular Biology
Pramisha Adhikari, Bing Xie, Ana Semeano, Alessandro Bonifazi, Francisco O. Battiti, Amy H. Newman, Hideaki Yano, Lei Shi
Summary: The study focuses on developing D3R selective agonists over D2R and identifies compound AB04-88 with significant D3R selectivity and G protein bias. The chirality of the primary pharmacophore is key in conferring improved D3R potency, selectivity, and G protein signaling bias.
Article
Medicine, Research & Experimental
Yong Mou, Juan Liu, Ting Pan, Qi Wang, Kang Miao, Yongjian Xu, Weining Xiong, Jun Yu
Summary: DA receptor agonists showed potential antifibrotic effects in IPF patients and mouse models by attenuating fibroblast differentiation and proliferation, protecting mice from pulmonary fibrosis induced by BLM.
BIOMEDICINE & PHARMACOTHERAPY
(2021)
Article
Neurosciences
Yasuharu Yamamoto, Keisuke Takahata, Manabu Kubota, Harumasa Takano, Hiroyoshi Takeuchi, Yasuyuki Kimura, Yasunori Sano, Shin Kurose, Hiroshi Ito, Masaru Mimura, Makoto Higuchi
Summary: The study revealed a significant positive correlation between DA synthesis capacity and DA transporter availability in the putamen, but no significant correlation between DA synthesis capacity and D2 receptor availability in the striatum, indicating a relationship between DA synthesis capacity and reuptake, while the total abundance of D2 receptors may not directly participate in the regulatory mechanism.
Review
Chemistry, Multidisciplinary
Emma Campbell, Christina Jordan, Ryan Gilmour
Summary: Carbohydrate diversity plays a crucial role in regulating cellular function and communication, making it an important area of research in biomedical diagnostics. The radiotracer 2-[F-18]-FDG, which utilizes metabolic trapping, has shown great success in positron emission tomography (PET). More complex sugars with specific selectivities are now being explored for molecular recognition and personalized medicine. This review provides an overview of the development of 2-[F-18]-FDG and glycan-based radiotracers for PET, highlighting their diagnostic functions and assisting in further interdisciplinary research.
CHEMICAL SOCIETY REVIEWS
(2023)
Article
Chemistry, Inorganic & Nuclear
Crist N. Filer, Joseph R. Andrews, Scot Pounds, Giliyar Ullas
Summary: This study presents an efficient method for radiolabeling several dopamine D-2 receptor agonists with tritium at high specific activity.
APPLIED RADIATION AND ISOTOPES
(2021)
Review
Endocrinology & Metabolism
Claudia Pivonello, Roberta Patalano, Mariarosaria Negri, Rosa Pirchio, Annamaria Colao, Rosario Pivonello, Renata Simona Auriemma
Summary: Pituitary neuroendocrine tumors are a common type of intracranial tumor. Treatment with dopamine agonists can be effective, but resistance may occur in some patients.
FRONTIERS IN ENDOCRINOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Josh Neuman, Nicole Roeder, Brittany Richardson, Teresa Quattrin, John Hamilton, Panayotis K. Thanos
Summary: The expression of the dopamine D2 gene plays a prominent role in the impact of a high-fat diet on GABA(A) receptors in the mouse brain.
NEUROCHEMICAL RESEARCH
(2022)
Article
Chemistry, Medicinal
Gengyang Yuan, Maeva Dhaynaut, Nicolas J. Guehl, Sepideh Afshar, Dalena Huynh, Sung-Hyun Moon, Suhasini M. Iyengar, Manish Kumar Jain, Julie E. Pickett, Hye Jin Kang, Mary Jo Ondrechen, Georges El Fakhri, Marc D. Normandin, Anna-Liisa Brownell
Summary: An array of triazolopyridines based on JNJ-46356479 were synthesized as potential radiotracers for mGluR2. These compounds showed enhanced activity and have the potential for translational studies.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Cell Biology
Hui Li, Wenzhuo Yang, Jianxin Xi, Zhenhua Wang, Han Lu, Zhishan Du, Weihang Li, Bo Wu, Shanshan Jiang, Yida Peng, Jingyi Liu, Luwei Liu, Xiangheng Zhang, Jiachun Feng
Summary: Dopamine receptor, particularly Dopamine receptor 2(D2), has been identified as a crucial drug target. Dopamine receptor agonists, drugs similar in function and structure to dopamine, have shown significant therapeutic effects on prolactinoma and Parkinson's Disease. Through virtual screening and molecular docking techniques, two compounds were identified as potential effective agonists of Dopamine receptor, showing promising results in cell experiments on pituitary tumor cells.
Article
Chemistry, Medicinal
Yongtao Li, Wenwei Lin, Sergio C. Chai, Jing Wu, Kavya Annu, Taosheng Chen
Summary: In this study, a selective and potent PXR antagonist was discovered through structural optimization of a series of compounds. This finding provides novel PXR inhibitors for basic research and future clinical studies and sheds light on reducing compound's binding affinity to PXR.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Zheng Dai, Sachit D. Saksena, Geraldine Horny, Christine Banholzer, Stefan Ewert, David K. Gifford
Summary: This study proposes a method of creating large libraries of candidate sequences that meet an objective function at low cost, called computationally designed factorizable libraries. By representing objective functions as an inner product of feature vectors, the authors introduce an optimization method called stochastically annealed product spaces (SAPS). Using this approach, they successfully design diverse and efficient libraries of antibody CDR-H3 sequences with various optimized characteristics.
Article
Neurosciences
Tove Freiburghaus, Jonas E. Svensson, Granville J. Matheson, Pontus Plaven-Sigray, Johan Lundberg, Lars Farde, Simon Cervenka
Summary: This study compared the binding potential of two PET radioligands – [C-11]FLB 457 and [C-11]raclopride – in extrastriatal brain regions in healthy control subjects. The weak to moderate within-subject correlations observed between the two radioligands suggest caution in interpreting extrastriatal D2-R measures obtained with [C-11]raclopride. These results underline the importance of considering the signal-to-noise ratio when using [C-11]raclopride for extrastriatal D2-R quantification.
Review
Obstetrics & Gynecology
Nuria Pellicer, Daniela Galliano, Sonia Herraiz, Yu Z. Bagger, Joan-Carles Arce, Antonio Pellicer
Summary: Endometriosis requires medical management during a woman's reproductive years, with most treatments aiming to create a hypoestrogenic environment. Targeting angiogenesis using dopamine agonists (DAs) is a promising strategy for reducing lesion size and pain in endometriosis by downregulating proangiogenic pathways and upregulating antiangiogenic pathways.
HUMAN REPRODUCTION
(2021)
Article
Biochemistry & Molecular Biology
Vladimir M. Pogorelov, Michael L. Martini, Jian Jin, William C. Wetsel, Marc G. Caron
Summary: L-DOPA is the main treatment for Parkinson's disease, but it can lead to dyskinesia over time. In this study, dopamine-depleted dopamine-transporter KO (DDD) mice were used as an acute PD model to screen novel compounds for anti-parkinsonian and L-DOPA-induced dyskinesia. The researchers found that oral stereotypies could be used as an index for LID in DDD mice.
Article
Chemistry, Physical
Pengbo Zhai, Zhilin Yang, Yi Wei, Xiangxin Guo, Yongji Gong
Summary: This paper reports the design of 2D fluorinated graphene-reinforced PVDF-HFP-LiTFSI polymer electrolytes for improving the mechanical properties and electrode/electrolyte interfacial reaction in solid-state lithium batteries. The use of this polymer electrolyte enables long-term Li plating/stripping and stable cycling, promoting the applications of solid polymer electrolytes in high-performance solid-state lithium batteries.
ADVANCED ENERGY MATERIALS
(2022)
Article
Neurosciences
Jogeshwar Mukherjee, Patrick J. Lao, Tobey J. Betthauser, Gurleen K. Samra, Min-Liang Pan, Ishani H. Patel, Christopher Liang, Raju Metherate, Bradley T. Christian
JOURNAL OF COMPARATIVE NEUROLOGY
(2018)
Article
Radiology, Nuclear Medicine & Medical Imaging
Tobey J. Betthauser, Ansel T. Hillmer, Patrick J. Lao, Emily Ehlerding, Jogeshwar Mukherjee, Charles K. Stone, Bradley T. Christian
NUCLEAR MEDICINE AND BIOLOGY
(2017)
Article
Neurosciences
Patrick J. Lao, Tobey J. Betthauser, Dana L. Tudorascu, Todd E. Barnhart, Ansel T. Hillmer, Charles K. Stone, Jogeshwar Mukherjee, Bradley T. Christian
Article
Biochemical Research Methods
Robert A. Coleman, Christopher Liang, Rima Patel, Sarah Ali, Jogeshwar Mukherjee
Article
Chemistry, Medicinal
Gurleen K. Samra, Irakli Intskirveli, Anitha P. Govind, Christopher Liang, Ronit Lazar, William N. Green, Raju Metherate, Jogeshwar Mukherjee
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2018)
Article
Chemistry, Medicinal
Gurleen K. Samra, Kenneth Dang, Heather Ho, Aparna Baranwal, Jogeshwar Mukherjee
MEDICINAL CHEMISTRY RESEARCH
(2018)
Article
Psychiatry
Nora S. Vyas, Monte S. Buchsbaum, Douglas S. Lehrer, Brian M. Merrill, Alex DeCastro, Nicholas A. Doninger, Bradley T. Christian, Jogeshwar Mukherjee
SCHIZOPHRENIA RESEARCH
(2018)
Meeting Abstract
Neurosciences
Monte Buchsbaum, Serge Mitelman, Bradley Christian, Brian Merrill, Bradley Buchsbaum, Jogeshwar Mukherjee, Douglas Lehrer
NEUROPSYCHOPHARMACOLOGY
(2018)
Meeting Abstract
Neurosciences
Nora Vyas, Douglas Lehrer, Brian Merrill, Alex DeCastro, Nicholas Doninger, Bradley Christian, Jogeshwar Mukherjee, Monte Buchsbaum
BIOLOGICAL PSYCHIATRY
(2017)
Meeting Abstract
Radiology, Nuclear Medicine & Medical Imaging
Christopher Liang, Gurleen Samra, Jogeshwar Mukherjee
JOURNAL OF NUCLEAR MEDICINE
(2017)
Meeting Abstract
Radiology, Nuclear Medicine & Medical Imaging
Patrick Lao, Tobey Betthauser, Dana Tudorascu, Todd Barnhart, Jogeshwar Mukherjee, Bradley Christian
JOURNAL OF NUCLEAR MEDICINE
(2017)
Meeting Abstract
Endocrinology & Metabolism
P. Lao, T. Betthauser, D. Tudorascu, T. Barnhart, J. Mukherjee, B. Christian
JOURNAL OF CEREBRAL BLOOD FLOW AND METABOLISM
(2017)
Meeting Abstract
Psychiatry
Monte Buchsbaum, Nora Vyas, Douglas Lehrer, Brian Merill, Alex DeCastro, Nicholas Donninger, Bradley Christian, Jogeshwar Mukherjee
SCHIZOPHRENIA BULLETIN
(2017)
Review
Endocrinology & Metabolism
Jogeshwar Mukherjee, Aparna Baranwal, Kimberly N. Schade
CURRENT DIABETES REVIEWS
(2016)
Article
Neurosciences
E. A. Kelly, T. M. Love, J. L. Fudge
Summary: Dopamine is involved in stress-related illnesses, and corticotropin-releasing factor plays a role in stress responses. This study examined the synaptic terminals between dopamine and non-dopamine cells and found that dopamine regulation may occur indirectly through contacts with non-dopamine neurons.