Choose a journal from the journal list. Please note: If you switch to a different device, you may be asked to login again with only your ACS ID. The Journal of Medicinal Chemistry and Drug Design (JMCDD) (ISSN 2578-9589) presents up-to-date coverage of advanced drug systems and their applications in medicine. This Viewpoint discusses the discovery, published in this journal, that a highly potent and specific GPR52 antagonist was identified through high-throughput screening and structure–activity relationship study, which diminishes not only mHTT protein levels, but also ameliorates HD-like phenotypes in the animal disease models. A new series of 1,2,4-oxadiazolylphenyl alanine derivatives were identified as TPH1 inhibitors. In line with these positive observations, 14g exhibited an excellent water solubility of 31.4 mg/mL, which was more than 1000-fold higher than that of TNBG (4 μg/mL). Search. Moreover, in vivo study showed that Comp-43 not only reduces mHTT levels but also rescues HD-related phenotypes in HdhQ140 mice. 28 th of 59 in Chemistry, Medicinal. The study identified compound 7e, which acts as a potent 5-hydroxytryptamine type 6 receptor (5-HT6R) neutral antagonist at Gs and does not impact neurite growth (process controlled by Cdk5). In addition, we report the first X-ray crystal structures of C. neoformans Hsp90 nucleotide binding domain (NBD), as the apoprotein and in complexes with the non-species-selective Hsp90 inhibitor NVP-AUY922 and three RAPs revealing unique ligand-induced conformational rearrangements, which reaffirm the hypothesis that intrinsic differences in protein flexibility can confer selective inhibition of fungal versus human Hsp90 isoforms. The identification of drugs to treat COVID-19 and other coronavirus diseases is an urgent global need, thus different strategies targeting either virus or host cell are still under investigation. Der Journal Impact, deutsch Impact-Faktor, ist eine errechnete Zahl, deren Höhe den Einfluss einer wissenschaftlichen Fachzeitschrift wiedergibt. Please check the relevant section in this Guide for Authors for more details. Article. Therefore, potent chemical tools with favorable pharmacokinetic profiles are desirable to characterize this enzyme. American Journal of Medicinal Chemistry is an Open Access journal and we do not charge the end user when accessing a manuscript or any article. Herein, we report the discovery of a potent and novel OGA inhibitor, compound 5i, comprising an aminopyrimidine scaffold, identified by virtual screening based on multiple methodologies combining structure-based and ligand-based approaches, followed by sequential optimization with a focus on ligand lipophilicity efficiency. To correlate biological data with configuration, all four ifenprodil stereoisomers were prepared by diastereoselective reduction and subsequent separation of enantiomers by chiral HPLC. You’re seeing our new journal sites and we’d like your opinion, please send feedback. Several novel glucose-lowering strategies are currently under clinical investigation, highlighting the need for more robust treatments. The Journal of Medicinal Chemistry is a peer-reviewed medical journal covering research in medicinal chemistry. Indeed, previous studies from our laboratories identified a critical role for the fragment linked at C6 in determining whether triazolopyrimidines promote MT stabilization or, conversely, disrupt MT integrity in cells. Archives of Natural and Medicinal Chemistry is an online, open access journal covers various aspects like pharmaceutical chemistry, natural products, organic compounds along with biological products such as biochemistry, molecular biology, pharmacognosy, pharmacology, toxicology setting altogether for safety and efficacy of drugs in treatment of diseases. Medicinal Chemistry Research. Consequently, inhibition of the Hsp90 protein folding machinery results in a combinatorial attack on numerous oncogenic pathways. Notably, (2) in the detection of bioactive species, fluorophores with relatively lower fluorescence quantum yield favor the detection sensitivity. Find out more about the change.. Meet Our Editorial Board Member. Journal of Enzyme Inhibition and Medicinal Chemistry. Experimental, theoretical and applied original research studies in all fields of medicinal and chemistry are welcomed for submission. GPR52 is an orphan G protein-coupled receptor (GPCR) that has been recently implicated as a potential drug target of Huntington’s disease (HD), an incurable monogenic neurodegenerative disorder. It provides a medium for publication … International contributors cover the entire spectrum of new drug research, including methods of synthesis; results of pharmacological, … MD simulations highlighted receptor conformational changes for 7e and inverse agonist PZ-1444. Ranking and Category. The Journal of Medicinal Chemistry publishes studies that contribute to an understanding of the relationship between molecular structure and biological activity or mode of action. Supports open access. Journal of Enzyme Inhibition and Medicinal Chemistry. Michael Kassiou University of Sydney, Australia. Notably, intravenous injection of RGD-SS-CA (2) into mice-bearing human tumor xenografts induced significant tumor growth suppression with negligible toxicity. Volume 19 Issue 4 . Herein, we report our work exploring the essential requirements for fluorophore selection during the development of various fluorescence applications. Journal of Medicinal Chemistry, Articles ASAP (Featured Article) Publication Date (Web): November 13, 2020. The optimized compound CJ2-150 (37) showed a non-ATP competitive allosteric mode of action in a mixed-type inhibition for Aurora B kinase. In addition, we discovered a highly potent and specific GPR52 antagonist Comp-43 with an IC50 value of 0.63 μM by a structure–activity relationship (SAR) study. These preclinical data support further clinical development of dosimertinib for the treatment of NSCLC. GPR52 is an orphan G protein-coupled receptor (GPCR) highly expressed in the brain, especially in the striatum, and represents an emerging therapeutic target for Huntington’s disease (HD), an incurable monogenic neurodegenerative disorder caused by the mutation of the huntingtin (mHTT) gene. RSC Medicinal Chemistry is the new name for MedChemComm. You’ve supercharged your research process with ACS and Mendeley! Your Mendeley pairing has expired. Der erste Chefredakteur war von 1959 bis einschließlich 1971 Alfred Burger. Authors' Comments. The CCK-8 assay enabled us to identify a novel compound, 14g, which strongly inhibited HepG2 and A549 cell growth with IC50 values of 0.54 and 0.47 μM, respectively. Whereas the configuration did not influence considerably the GluN2B-NMDA receptor binding, (1R)-configuration is crucial for elevated inhibitory activity. Scope . Editorial Board Members. Collectively, these data demonstrate that targeting GLP-1R and Y2-R with chimeric single peptides offers a route to new glucoregulatory treatments that are well-tolerated and have improved weight loss when compared directly to Ex-4. In particular, compound D12 showed excellent in vitro and in vivo synergistic antifungal efficacy with fluconazole to treat azole-resistant candidiasis. 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