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  • inhibitors
  • In the intensifying efforts to discover new, hopefully more therapeutically efficacious HDAC inhibitors, molecular modeling-based rational drug design has played an important role in identifying potential inhibitors that vary in molecular structures and properties. (mdpi.com)
  • Negative correlations between 7-ethoxycoumarin O -deethylation and cell line chemosensitivity to a group of topoisomerase inhibitors were also seen, again suggesting P450-dependent drug inactivation. (aspetjournals.org)
  • chemotherapy drugs
  • Because of the effect on immune cells (especially lymphocytes), chemotherapy drugs often find use in a host of diseases that result from harmful overactivity of the immune system against self (so-called autoimmunity). (wikipedia.org)
  • efficacy
  • Once a small molecule is discovered that selectively and potently alters a target with potential therapeutic importance, it can be modified by medicinal chemists to overcome the pharmacodynamic, pharmacokinetic, toxicity, and efficacy hurdles necessary for bringing a drug to market. (aacrjournals.org)
  • Such tests, along with the discovery of new biological markers for response to drug therapy, or approaches to increase the compound's efficacy (e.g. via siRNA-mediated knock-down of cytoprotective genes) will assist NKUA-CRG members and collaborating pharmaceutical companies in deciding whether a "drug candidate" has scientific merit for further development as an investigational new drug. (uoa.gr)
  • toxicity
  • however, use of these drugs is often associated with patient toxicity and poor tumor delivery. (hindawi.com)
  • With this award, he obtained his PhD in Medicinal Chemistry from the University of Washington in 2005, investigating the molecular mechanisms of specific drug-induced liver toxicity (under the mentorship of Prof Sid Nelson). (nus.edu.sg)
  • In July 2009, he started his assistant professorship at NUS, and began building his own research program focusing on drug-induced liver toxicity, as well as exploring new drug targets for liver cancer. (nus.edu.sg)
  • Also, the drugs can often be used at lower doses, reducing toxicity. (wikipedia.org)
  • development
  • The cancer drug development process has become increasingly costly and inefficient resulting in few new highly effective drugs reaching the market yearly ( 1 ). (aacrjournals.org)
  • The special properties of the small molecules described above are important in drug development. (aacrjournals.org)
  • For the past two decades, marine pharmaceutics has been a developing field in the antitumor drug development arena. (mdpi.com)
  • they play a leading role in the discovery and development of drugs, for disease treatment. (hindawi.com)
  • Natural health products (NHPs) and natural products (NPs) play a leading role in the discovery and the development of drugs for the treatment of human diseases. (hindawi.com)
  • The overall goal of the lab is to improve the management of liver disorders such as liver cancer and drug-induced liver disease (DILI) through understanding the molecular mechanisms leading to their development and progression. (nus.edu.sg)
  • Notable kinases are being evaluated for their suitability as drug targets for chemotherapeutic development. (nus.edu.sg)
  • The techniques we employ include but are not limited to high-throughput sequencing, mutation analysis, immunoassays and other biochemical assay development. (nus.edu.sg)
  • I run a testing service as part of the Drug Development Unit in NUS for in-house lead discoveries. (nus.edu.sg)
  • He also directs a toxicology division within a newly founded Drug Development Unit in NUS and is a young member of the NGS program. (nus.edu.sg)
  • targets
  • The pharmaceutical industry has successfully exploited the ability of small molecules to serve as drugs by focusing on a relatively small number of biological targets, a subset of the so-called "druggable genome" ( 6 ). (aacrjournals.org)
  • synthesis
  • Due to the improvement on methods for isolation, identification, and synthesis during the last century, many drugs have arisen from natural sources. (hindawi.com)
  • unmet
  • We ultimately assess the value for antioxidants as neuroprotective drugs and provide our comments on the unmet needs. (mdpi.com)
  • tightly
  • The ICG is a public-access research facility consisting of a tightly integrated team of synthetic and analytical chemists, assay developers, high-throughput screening and automation engineers, computational scientists, and software developers. (aacrjournals.org)
  • Based on the natural high affinity of folate for the folate receptor protein (FR), which is commonly expressed on the surface of many human cancers, folate-drug conjugates also bind tightly to the FR and trigger cellular uptake via endocytosis. (wikipedia.org)
  • metabolism
  • The cytochrome P450s are a superfamily of hemeprotein monooxygenases that catalyze the oxidative metabolism of a large number of drugs, environmental carcinogens, as well as steroids and other endobiotics. (aspetjournals.org)
  • P450 enzymes are highly expressed in human liver and in certain extrahepatic tissues and have been studied extensively with respect to their roles in drug metabolism ( Rendic and Di Carlo, 1997 ). (aspetjournals.org)
  • Work includes mechanistic studies on drug distribution and metabolism, and the consequential generation and accumulation of toxic metabolites. (nus.edu.sg)
  • therapeutic
  • An ideal delivery system should be composed of biocompatible and biodegradable materials, reproducibly assemble into the desired size range, encapsulate a wide range of drugs and drug classes, maintain particle size in biological media, have the ability to attach cell-specific targeting groups, and release the therapeutic at the site of disease. (hindawi.com)
  • chemically
  • Some have utilized the approach of chemically conjugating the active drug to a polymer to potentially improve stability. (hindawi.com)
  • cell
  • From a mechanistic perspective, the FR functions to concentrate exogenous ligands (e.g. folates and folate-drug conjugates) into the cell cytosol by endocytosis. (wikipedia.org)
  • biological
  • High-throughput screening (HTS), a mainstay of the drug industry, is well suited for this process because it is designed to handle hundreds of thousands of biological measurements per day. (aacrjournals.org)
  • research
  • All chemistry and screening data are deposited into the ChemBank web site ( http://chembank.broad.harvard.edu/ ) and are available to the entire research community within a year of generation. (aacrjournals.org)
  • This report outlines how the ICG functions, how researchers can take advantage of its screening, chemistry and informatic capabilities, and provides a brief summary of some of the many important research findings. (aacrjournals.org)
  • specific
  • Targeted drug therapy is advantageous because it deposits the drug at the specific location where it can be most useful in treating the disease. (wikipedia.org)