Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes–7

Breakthroughs in Medicinal Chemistry [...].

[1]  Laura M Luh,et al.  Prey for the Proteasome: Targeted Protein Degradation—A Medicinal Chemist's Perspective , 2020, Angewandte Chemie.

[2]  R. Bonomo,et al.  A γ-Lactam Siderophore Antibiotic Effective Against Multidrug-Resistant Gram-Negative Bacilli. , 2020, Journal of medicinal chemistry.

[3]  Kuo Zhang,et al.  Peptide-Based Nanoparticles Mimic Fibrillogenesis of Laminin in Tumor Vessel for Precise Embolization. , 2020, ACS nano.

[4]  S. Sarafianos,et al.  Chemical profiling of HIV-1 capsid-targeting antiviral PF74. , 2020, European journal of medicinal chemistry.

[5]  K. Matsui,et al.  Stalobacin: Discovery of Novel Lipopeptide Antibiotics with Potent Antibacterial Activity against Multidrug-resistant Bacteria. , 2020, Journal of medicinal chemistry.

[6]  Mai Moaaz,et al.  The novel role of IL-37 to enhance the anti-inflammatory response of regulatory T cells in patients with peripheral atherosclerosis , 2020, Vascular.

[7]  H. Briem,et al.  Treating Cancer by Spindle Assembly Checkpoint Abrogation: Discovery of Two Clinical Candidates, BAY 1161909 and BAY 1217389, Targeting MPS1 Kinase. , 2020, Journal of medicinal chemistry.

[8]  J. Elisseeff,et al.  Using proteolysis-targeting chimera technology to reduce navitoclax platelet toxicity and improve its senolytic activity , 2020, Nature Communications.

[9]  Hualiang Jiang,et al.  Structure of Mpro from SARS-CoV-2 and discovery of its inhibitors , 2020, Nature.

[10]  T. Liang,et al.  Discovery of Peptide Boronate Derivatives as Histone Deacetylase (HDAC) and Proteasome Dual Inhibitors for Overcoming Bortezomib Resistance of Multiple Myeloma. , 2020, Journal of medicinal chemistry.

[11]  A. Brasier,et al.  Discovery of Orally Bioavailable Chromone Derivatives as Potent and Selective BRD4 Inhibitors: Scaffolding Hopping, Optimization and Pharmacological Evaluation. , 2020, Journal of medicinal chemistry.

[12]  Xiaotao Lu,et al.  An orally bioavailable broad-spectrum antiviral inhibits SARS-CoV-2 in human airway epithelial cell cultures and multiple coronaviruses in mice , 2020, Science Translational Medicine.

[13]  Matthew R. Lee,et al.  Discovery of Selective Small Molecule Degraders of BRAF-V600E. , 2020, Journal of medicinal chemistry.

[14]  C. Supuran,et al.  Tellurides Bearing Sulfonamides as Novel Inhibitors of Leishmanial Carbonic Anhydrase with Potent Antileishmanial Activity. , 2020, Journal of medicinal chemistry.

[15]  R. Hilgenfeld,et al.  Crystal structure of SARS-CoV-2 main protease provides a basis for design of improved α-ketoamide inhibitors , 2020, Science.

[16]  Tomohiko Hayashi,et al.  Development and structural determination of an anti-PrPC aptamer that blocks pathological conformational conversion of prion protein , 2020, Scientific Reports.

[17]  A. Zelikin,et al.  Molecular, macromolecular, and supramolecular glucuronide prodrugs: an unexpected lead identified for anticancer prodrug monotherapy. , 2020, Angewandte Chemie.

[18]  Yi-Wei Chang Bacteria suit up with virus armor , 2020, Proceedings of the National Academy of Sciences.

[19]  A. Walls,et al.  Structure, Function, and Antigenicity of the SARS-CoV-2 Spike Glycoprotein , 2020, Cell.

[20]  J. Turnbull,et al.  The 2019 coronavirus (SARS-CoV-2) surface protein (Spike) S1 Receptor Binding Domain undergoes conformational change upon heparin binding , 2020, bioRxiv.

[21]  Reid H. J. Olsen,et al.  Nanobody-enabled monitoring of kappa opioid receptor states , 2020, Nature Communications.

[22]  C. Biot,et al.  Structure‐Based Design and Synthesis of Piperidinol‐Containing Molecules as New Mycobacterium abscessus Inhibitors , 2020, ChemistryOpen.

[23]  Jiang Xia,et al.  Safeguarding intestine cells against enteropathogenic Escherichia coli by intracellular protein reaction, a preventive antibacterial mechanism , 2020, Proceedings of the National Academy of Sciences.

[24]  W. Chiu,et al.  Ultra-thermostable RNA nanoparticles for solubilizing and high-yield loading of paclitaxel for breast cancer therapy , 2020, Nature Communications.

[25]  A. Zelikin,et al.  Molecular, macromolecular, and supramolecular glucuronide prodrugs: an unexpected lead identified for anticancer prodrug monotherapy. , 2020, Angewandte Chemie.

[26]  H. Schwalbe,et al.  In situ formation of transcriptional modulators using non-canonical DNA i-motifs† †This work is dedicated to Professor Hans-Ulrich Reissig on the occasion of his 70th birthday. ‡ ‡Electronic supplementary information (ESI) available. See DOI: 10.1039/d0sc00514b , 2020, Chemical science.

[27]  Ulrike Schulze,et al.  Phage liquid crystalline droplets form occlusive sheaths that encapsulate and protect infectious rod-shaped bacteria , 2020, Proceedings of the National Academy of Sciences.

[28]  R. Hilgenfeld,et al.  α-Ketoamides as Broad-Spectrum Inhibitors of Coronavirus and Enterovirus Replication: Structure-Based Design, Synthesis, and Activity Assessment , 2020, Journal of medicinal chemistry.

[29]  C. Supuran,et al.  Drug Screening in Human Cells by NMR Spectroscopy Allows the Early Assessment of Drug Potency , 2020, Angewandte Chemie.

[30]  Doyle J Cassar,et al.  Structure-based design and pharmacokinetic optimization of covalent allosteric inhibitors of the mutant GTPase KRASG12C. , 2020, Journal of medicinal chemistry.

[31]  Emma J. Chory,et al.  A Deep Learning Approach to Antibiotic Discovery , 2020, Cell.

[32]  I. Trougakos,et al.  Biological Evaluation and In Silico Study of Benzoic Acid Derivatives from Bjerkandera adusta Targeting Proteostasis Network Modules , 2020, Molecules.

[33]  I. Sancho-Martinez,et al.  Nidufexor (LMB763), a Novel FXR Modulator for the Treatment of Nonalcoholic Steatohepatitis (NASH). , 2020, Journal of medicinal chemistry.

[34]  C. Kang,et al.  Identification and structural characterization of small molecule fragments targeting Zika virus NS2B-NS3 protease. , 2020, Antiviral research.

[35]  Janez Konc,et al.  Stereoselective Activity of 1-Propargyl-4-styrylpiperidine-like Analogues That Can Discriminate between Monoamine Oxidase Isoforms A and B , 2020, Journal of medicinal chemistry.

[36]  A. Rojas,et al.  Potent, selective, water soluble, brain-permeable EP2 receptor antagonist for use in central nervous system disease models. , 2020, Journal of medicinal chemistry.

[37]  Samuel T. Jones,et al.  Modified cyclodextrins as broad-spectrum antivirals , 2020, Science Advances.

[38]  Davide Risso,et al.  Rapid non-uniform adaptation to conformation-specific KRAS(G12C) inhibition , 2020, Nature.

[39]  M. Cheng,et al.  Design, synthesis, biological evaluation and molecular docking study of novel thieno[3,2-d]pyrimidine derivatives as potent FAK inhibitors. , 2019, European journal of medicinal chemistry.

[40]  F. Tay,et al.  Considerations and Caveats in Combating ESKAPE Pathogens against Nosocomial Infections , 2019, Advanced science.

[41]  E. Eisenmesser,et al.  Short‐term interleukin‐37 treatment improves vascular endothelial function, endurance exercise capacity, and whole‐body glucose metabolism in old mice , 2019, Aging cell.

[42]  T. Blundell,et al.  Fragment-Based Design of Mycobacterium tuberculosis InhA Inhibitors , 2019, Journal of medicinal chemistry.

[43]  Y. Pommier,et al.  Novel deazaflavin tyrosyl-DNA phosphodiesterase 2 (TDP2) inhibitors. , 2019, DNA repair.

[44]  Wei Wu,et al.  Targeting Oncogenic BRAF: Past, Present, and Future , 2019, Cancers.

[45]  Judith Weber,et al.  ThX – A next-generation probe for the early detection of amyloid aggregates , 2019, bioRxiv.

[46]  Esther Kellenberger,et al.  A bright future for fragment-based drug discovery: what does it hold? , 2019, Expert opinion on drug discovery.

[47]  M. Hipp,et al.  The proteostasis network and its decline in ageing , 2019, Nature Reviews Molecular Cell Biology.

[48]  Wolfgang Jahnke,et al.  Fragment-Based Drug Discovery: Advancing Fragments in the Absence of Crystal Structures. , 2019, Cell chemical biology.

[49]  C. Supuran,et al.  Are Carbonic Anhydrases Suitable Targets to Fight Protozoan Parasitic Diseases? , 2019, Current medicinal chemistry.

[50]  Bryan L Roth,et al.  Discovery of new GPCR ligands to illuminate new biology. , 2017, Nature chemical biology.

[51]  I. Schalk,et al.  Bacterial Iron Uptake Pathways: Gates for the Import of Bactericide Compounds. , 2017, Journal of medicinal chemistry.

[52]  W. Parks,et al.  Filamentous Bacteriophage Produced by Pseudomonas aeruginosa Alters the Inflammatory Response and Promotes Noninvasive Infection In Vivo , 2016, Infection and Immunity.

[53]  M. Willmann,et al.  Human commensals producing a novel antibiotic impair pathogen colonization , 2016, Nature.

[54]  L. Henry,et al.  Epidemiology of Nonalcoholic Fatty Liver Disease and Nonalcoholic Steatohepatitis in the United States and the Rest of the World. , 2016, Clinics in liver disease.

[55]  K. Lewis,et al.  A new antibiotic kills pathogens without detectable resistance , 2015, Nature.

[56]  C. Jack,et al.  Hypothetical model of dynamic biomarkers of the Alzheimer's pathological cascade , 2010, The Lancet Neurology.

[57]  J. Hardy,et al.  The Amyloid Hypothesis of Alzheimer ’ s Disease : Progress and Problems on the Road to Therapeutics , 2009 .