51 articles for thisTarget
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Development of thieno- and benzopyrimidinone inhibitors of the Hedgehog signaling pathway reveals PDE4-dependent and PDE4-independent mechanisms of action.
Vanderbilt University School of Medicine
Discovery of 2-Indole-acylsulfonamide Myeloid Cell Leukemia 1 (Mcl-1) Inhibitors Using Fragment-Based Methods.
Vanderbilt University School of Medicine
Inhibition of human DNA topoisomerase IIa by two novel ellipticine derivatives.
Vanderbilt University School of Medicine
Discovery of tricyclic indoles that potently inhibit Mcl-1 using fragment-based methods and structure-based design.
Vanderbilt University School of Medicine
Diphenylpyrazoles as replication protein a inhibitors.
Vanderbilt University School of Medicine
Discovery of (S)-2-cyclopentyl-N-((1-isopropylpyrrolidin2-yl)-9-methyl-1-oxo-2,9-dihydro-1H-pyrrido[3,4-b]indole-4-carboxamide (VU0453379): a novel, CNS penetrant glucagon-like peptide 1 receptor (GLP-1R) positive allosteric modulator (PAM).
Vanderbilt University School of Medicine
Design of Fluorine-Containing 3,4-Diarylfuran-2(5H)-ones as Selective COX-1 Inhibitors.
Vanderbilt University School of Medicine
Fragment-based screening of the bromodomain of ATAD2.
Vanderbilt University School of Medicine
Discovery of a potent stapled helix peptide that binds to the 70N domain of replication protein A.
Vanderbilt University School of Medicine
Discovery of a potent inhibitor of replication protein a protein-protein interactions using a fragment-linking approach.
Vanderbilt University School of Medicine
Discovery of Protein-Protein Interaction Inhibitors of Replication Protein A.
Vanderbilt University School of Medicine
Development of potent and selective indomethacin analogues for the inhibition of AKR1C3 (Type 5 17ß-hydroxysteroid dehydrogenase/prostaglandin F synthase) in castrate-resistant prostate cancer.
Vanderbilt University School of Medicine
Discovery of potent myeloid cell leukemia 1 (Mcl-1) inhibitors using fragment-based methods and structure-based design.
Vanderbilt University School of Medicine
Development of an in vivo active, dual EP1 and EP3 selective antagonist based on a novel acyl sulfonamide bioisostere.
Vanderbilt University School of Medicine
Pharmacological inhibition of P-glycoprotein transport enhances the distribution of HIV-1 protease inhibitors into brain and testes.
Vanderbilt University School of Medicine
Mibefradil is a P-glycoprotein substrate and a potent inhibitor of both P-glycoprotein and CYP3A in vitro.
Vanderbilt University School of Medicine
Modulation by drugs of human hepatic sodium-dependent bile acid transporter (sodium taurocholate cotransporting polypeptide) activity.
Vanderbilt University School of Medicine
Further optimization of the K-Cl cotransporter KCC2 antagonist ML077: development of a highly selective and more potent in vitro probe.
Vanderbilt University School of Medicine
Generation of new protein kinase inhibitors utilizing cytochrome p450 mutant enzymes for indigoid synthesis.
Vanderbilt University School of Medicine
Podophyllotoxin analogues active versus Trypanosoma brucei.
Vanderbilt University School of Medicine
The influence of double bond geometry in the inhibition of cyclooxygenases by sulindac derivatives.
Vanderbilt University School of Medicine
Discovery of a Myeloid Cell Leukemia 1 (Mcl-1) Inhibitor That Demonstrates Potent In Vivo Activities in Mouse Models of Hematological and Solid Tumors.
Vanderbilt University School of Medicine
Substituent effects of N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides on positive allosteric modulation of the metabotropic glutamate-5 receptor in rat cortical astrocytes.
Vanderbilt University School of Medicine
Fragment-Based Discovery of Small Molecules Bound to T-Cell Immunoglobulin and Mucin Domain-Containing Molecule 3 (TIM-3).
Vanderbilt University School of Medicine
Discovery of a novel class of heteroaryl-pyrrolidinones as positive allosteric modulators of the muscarinic acetylcholine receptor M
Vanderbilt University School of Medicine
Harmaline Analogs as Substrate-Selective Cyclooxygenase-2 Inhibitors.
Vanderbilt University School of Medicine
Targeted Detection of Cyclooxygenase-1 in Ovarian Cancer.
Vanderbilt University School of Medicine
Enantiospecific, selective cyclooxygenase-2 inhibitors.
Vanderbilt University School of Medicine
Amide derivatives of meclofenamic acid as selective cyclooxygenase-2 inhibitors.
Vanderbilt University School of Medicine
Discovery of Sulfonamide-Derived Agonists of SOS1-Mediated Nucleotide Exchange on RAS Using Fragment-Based Methods.
Vanderbilt University School of Medicine
Multistep Binding of the Non-Steroidal Inhibitors Orteronel and Seviteronel to Human Cytochrome P450 17A1 and Relevance to Inhibition of Enzyme Activity.
Vanderbilt University School of Medicine
Discovery and SAR of a novel series of potent, CNS penetrant M4 PAMs based on a non-enolizable ketone core: Challenges in disposition.
Vanderbilt University School of Medicine
Ester and amide derivatives of the nonsteroidal antiinflammatory drug, indomethacin, as selective cyclooxygenase-2 inhibitors.
Vanderbilt University School of Medicine
Discovery of an Orally Bioavailable and Central Nervous System (CNS) Penetrant mGlu
Vanderbilt University School of Medicine
Discovery of Potent Myeloid Cell Leukemia-1 (Mcl-1) Inhibitors That Demonstrate in Vivo Activity in Mouse Xenograft Models of Human Cancer.
Vanderbilt University School of Medicine
Validation of Human Sterol 14α-Demethylase (CYP51) Druggability: Structure-Guided Design, Synthesis, and Evaluation of Stoichiometric, Functionally Irreversible Inhibitors.
Vanderbilt University School of Medicine
Discovery of Novel Central Nervous System Penetrant Metabotropic Glutamate Receptor Subtype 2 (mGlu
Vanderbilt University School of Medicine
Design, synthesis, and biochemical evaluation of N-substituted maleimides as inhibitors of prostaglandin endoperoxide synthases.
Vanderbilt University School of Medicine
Sterol 14α-Demethylase Structure-Based Optimization of Drug Candidates for Human Infections with the Protozoan Trypanosomatidae.
Vanderbilt University School of Medicine
Discovery of Quinazolines That Activate SOS1-Mediated Nucleotide Exchange on RAS.
Vanderbilt University School of Medicine
Sterol 14α-Demethylase Structure-Based Design of VNI (( R)- N-(1-(2,4-Dichlorophenyl)-2-(1 H-imidazol-1-yl)ethyl)-4-(5-phenyl-1,3,4-oxadiazol-2-yl)benzamide)) Derivatives To Target Fungal Infections: Synthesis, Biological Evaluation, and Crystallographic Analysis.
Vanderbilt University School of Medicine
Discovery and optimization of 3-(4-aryl/heteroarylsulfonyl)piperazin-1-yl)-6-(piperidin-1-yl)pyridazines as novel, CNS penetrant pan-muscarinic antagonists.
Vanderbilt University School of Medicine
Optimization of Potent and Selective Tricyclic Indole Diazepinone Myeloid Cell Leukemia-1 Inhibitors Using Structure-Based Design.
Vanderbilt University School of Medicine
Synthesis and evaluation of 4,6-disubstituted pyrimidines as CNS penetrant pan-muscarinic antagonists with a novel chemotype.
Vanderbilt University School of Medicine
