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In: Donev R, editor. Advances in protein chemistry and structural biology. UK: Swansea University; Maraviroc UK, , a potent, orally bioavailable, and selective small-molecule inhibitor of chemokine receptor CCR5 with broad-spectrum anti-human immunodeficiency virus type 1 activity. Antimicrob Agents Chemother.
Chemokines and Their Receptors in Drug Discovery
Big hopes ride on big rings. ACS Meeting News: constraining molecules in macrocyclic rings could help address challenges in drug discovery. Chem Eng News. The exploration of macrocycles for drug discovery — an underexploited structural class.
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Novel therapeutic strategy to inhibit growth of pancreatic cancer organoids using a rational combination of drugs to induce mitotic arrest and apoptosis. J Clin Oncol. Membranes as messengers in T cell adhesion signaling. Nat Immunol. Twenty years on: the impact of fragments on drug discovery. Discovery and characterization of a selective, nonpeptidyl thrombopoietin receptor agonist. Exp Hematol. Piece by Piece. Methylation of the first exon in the erythropoietin receptor gene does not correlate with its mRNA and protein level in cancer cells.
BMC Genet. Drug target protein-protein interaction networks: a systematic perspective. Biomed Res Int. Kinase inhibitors: the road ahead. Chemical space of DNA-encoded libraries. J Med Chem. Clin Cancer Res — Diversity-oriented synthesis as a tool for the discovery of novel biologically active small molecules. Nat Commun. An evidence-based review of obatoclax mesylate in the treatment of hematological malignancies. Core Evidence. Protein interactions and disease. PLoS Comput Biol. Allosteric inhibition of the protein-protein interaction between the leukemia-associated proteins Runx1 and CBFbeta.
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Angew Chem Int Ed. Receptor-receptor interactions as a widespread phenomenon: novel targets for drug development? Front Endocrinol. Drug discovery: a question of library design. Analysis of protein binding sites by computational solvent mapping. Methods Mol Biol. Allosteric inhibition of PTP1B activity by selective modification of a non-active site cysteine residue. Structure, function, and allosteric modulation of NMDA receptors. J Gen Physiol. Open Biol Chemokine receptor antagonists: overcoming developmental hurdles.
Tankyrase inhibition stabilizes axin and antagonizes Wnt signalling. The carcinogenic role of the notch signaling pathway in the development of hepatocellular carcinoma. J Cancer. Extracellular protein microarray technology for high throughput detection of low affinity receptor-ligand interactions. J Vis Exp. PPIMpred: a web server for high-throughput screening of small molecules targeting protein—protein interaction. R Soc Open Sci. Precision Oncology. Systematic analysis of helical protein interfaces reveals targets for synthetic inhibitors.
ACS Chem Biol. Mol Pharmacol. A prototype nonpeptidyl, hydrazone class, thrombopoietin receptor agonist, SB, is toxic to primary human myeloid leukemia cells. Nat Protoc. The novel tryptamine derivative JNJ induces wild-type p and E2F1-mediated apoptosis in acute myeloid and lymphoid leukemias. Mol Cancer Ther. Structural conservation of druggable hot spots in protein-protein interfaces.
Identification of hot spots within druggable binding regions by computational solvent mapping of proteins. Current screening methodologies in drug discovery for selected human diseases. Mar Drugs. Protein degradation by the ubiquitin—proteasome pathway in normal and disease states. J Am Soc Nephrol. J Org Chem — Thrombocytopenia caused by the development of antibodies to thrombopoietin. Drug discovery and natural products: end of an era or an endless frontier?
Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings. Adv Drug Deliv Rev. Diversity-oriented synthesis of bicyclic fragments containing privileged azines. The potential use of AKAP18delta as a drug target in heart failure patients. Expert Opin Biol Ther. Process of fragment-based lead discovery - a perspective from NMR. Med Microbiol Immunol. Nomad biosensors: a new multiplexed technology for the screening of GPCR ligands.
SLAS Technol. Discovery and characterization of nonpeptidyl agonists of the tissue-protective erythropoietin receptor. Marine invertebrate natural products that target microtubules. J Nat Prod. Approaches for differentiation and interconverting GPCR agonists and antagonists. Systematic targeting of protein-protein interactions. Trends Pharmacol Sci. The MDM2-p53 interaction. Mol Cancer Res. Hot spots - a review of the protein-protein interface determinant amino-acid residues. Natural products as sources of new drugs over the last 25 years. Towards the optimal screening collection: a synthesis strategy.
Angew Chem Int Ed Engl. An inhibitor of Bcl-2 family proteins induces regression of solid tumours. Computational identification of binding energy hot spots in protein-RNA complexes using an ensemble approach. Nucleic Acids Res. J Clin Med. Substantial susceptibility of chronic lymphocytic leukemia to BCL2 inhibition: results of a phase I study of Navitoclax in patients with relapsed or refractory disease.
Using peptidomimetics and constrained peptides as valuable tools for inhibiting protein—protein interactions. An integrated approach for fragment-based lead discovery: virtual, NMR, and high-throughput screening combined with structure-guided design. Application to the aspartyl protease renin. Fragment-based drug discovery lessons and outlook.
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Modulating the bcl-2 family of apoptosis suppressors for potential therapeutic benefit in cancer. De novo design of potent and selective mimics of IL-2 and IL Monoclonal antibodies mAbs : the latest dimension of modern therapeutics. Int J Curr Sci. Macrocyclic peptide inhibitors for the protein—protein interaction of Zaire Ebola virus protein 24 and karyopherin alpha 5. Org Biomol Chem. An inhibitor of NEDD8-activating enzyme as a new approach to treat cancer.
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Modulators of protein-protein interactions. Folia Medica Indonesiana. The integrins. Genome Biol. High throughput screen for inhibitors of protein-protein interactions in a reconstituted heat shock protein 70 Hsp70 complex. A small, nonpeptidyl mimic of granulocyte-colony-stimulating factor. ABT a potent and orally bioavailable Bcl-2 family inhibitor.
Biased agonism and allosteric modulation of metabotropic glutamate receptor 5. Clin Sci. Mechanisms of apoptosis in ovarian cancer: the small molecule targeting. Int J Med Med Sci. Varshavsky A. The ubiquitin system, autophagy, and regulated protein degradation. Annu Rev Biochem.
In vivo activation of the p53 pathway by small-molecule antagonists of MDM2.
Ultra performance liquid chromatographic method for simultaneous quantification of plerixafor and related substances in an injection formulation. Cogent Chemistry. Tuning the binding affinity and selectivity of perfluoroaryl-stapled peptides by cysteine-editing. Activation of apoptosis in vivo by a hydrocarbon-stapled BH3 helix. Accessed 24 Mar Wan H. An overall comparison of small molecules and large biologics in ADME testing.
Reaching for high-hanging fruit in drug discovery at protein—protein interfaces. From discovery to bedside: targeting the ubiquitin system. Cell Chem Biol. Curr Top Microbiol Immunol. Chemokine receptor CCR5 antagonist maraviroc: medicinal chemistry and clinical applications. Curr Top Med Chem. Exp Biol Med. Discovery of a novel B-cell lymphoma 6 BCL6 —corepressor interaction inhibitor by utilizing structure-based drug design.
Bioorg Med Chem. Nature — Identification of TNF-related apoptosis inducing ligand and other molecules that distinguish inflammatory from resident dendritic cells in patients with psoriasis. J Allergy Clin Immunol. Peptidomimetics targeting protein-protein interactions for therapeutic development. Protein Pept Lett. Stem Cells Int. Design, synthesis, and applications of DNA—macrocyclic host conjugates.
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Full Text. Agonist approved for idiopathic thrombocytopenic purpura; in Phase III trials in hepatitis. Antagonist; phase III, dry eye syndrome. Shipping Add to Cart. Further versions. Description Content Author information Chemokines are hormone-like signaling molecules secreted by cells to signal infection and guide the immune response. The editors are based at the Amsterdam Center for Drug Research, a cross-disciplinary center in the Dutch academic system, but with numerous ties to pharmaceutical companies.