GLOSSARY |
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The technology platform invented by Professor David Liu at Harvard University that uses the specific formation of double stranded DNA to control chemical reactions. |
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Epidermal Growth Factor (EGF) Receptor. See also ERBB |
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A proprietary class of drug candidate molecules that have been developed by Ensemble Discovery. Ensemblin libraries comprise sets of synthetic macrocycles (ring size mainly 18—25 atoms) that have been produced using DNA-programmed chemistry. |
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A family of receptor tyrosine kinases (RTKs) related to the EGF Receptor (see EGFR), members of which include ERBB1 (EGFR), ERBB2 (HER2), ERBB3 and ERBB4. These receptors are important in cell-cell communication controlling the growth of cells and tissues, and are important targets of new anti-cancer drugs such as Herceptin®. |
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See Trastuzumab. |
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A set of guidelines devised by Dr. Chris Lipinski that indicate the preferred physicochemical properties of drug molecules that influence compound solubility and cell permeability. |
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A class of organic compounds that contain as a central feature a ring structure, usually of 14—30 atoms in size. Macrocyclic rings are prevalent in many naturally occurring compounds including natural product drugs. The presence of the macrocyclic ring confers important and beneficial biophysical properties on such molecules which enable their utility as drug molecules (reviewed in Driggers et al., 2008). |
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The natural physiological process of cell suicide, involved in controlling development and cell numbers. This process is often inhibited in cancer cells, leading to the growth of tumors and resistance to anti-cancer drugs. |
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A class of valuable drug discovery targets that comprise a pair of proteins which interact under physiological conditions to form a complex with a biological function. Examples include: interaction of many growth factors (or cytokines) with their receptors; intracellular complexes of protein pairs involved in cell signaling. Formation of the complex can induce a conformational change in one or both proteins and this change alters their interaction with other cellular proteins thereby transmitting a signal within the cell. As many protein-protein interactions have roles in disease it is important to find drugs that can prevent their formation. Such drug discovery targets have been historically difficult to address with small molecules, and success with biologic drugs can be limited owing to difficulty accessing their tissue location or intracellular location. |
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A class of enzymes that removes phosphate groups from tyrosine residues of proteins. The activity of these enzymes is generally the reverse of tyrosine kinases. Tyrosine kinases and phosphatases together regulate the structure and function of proteins via the phosphorylation state of the protein’s tyrosine residues. |
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A class of cell surface transmembrane receptors that signal via their cytoplasmic kinase domains. Many respond to extracellular signals from growth factors such as epidermal growth factor and platelet-derived growth factor, translating the extracellular signal from these ligands into an intracellular kinase signaling cascade. |
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Structure-Activity Relationship. Used by medicinal chemists and pharmacologists to describe the relationship between variations in chemical structure and a specific biochemical or physiological activity of a molecule such as its binding affinity for a target or its inhibitory activity on an enzyme. |
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Tumor Necrosis Factor is a key cytokine involved in systemic inflammation. The primary role of TNF is in the regulation of cells of the immune system, but its dysregulation has been implicated in a variety of human diseases, particulary inflammatory diseases, as well as cancer. Thus, it has been a significant target for the biopharmaceutical industry with a number of marketed biologic drugs against it. |
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Generic name for Herceptin®, an inhibitory humanized monoclonal antibody targeted to the extracellular domain of ERBB2. |
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