Drug discovery today
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Drug discovery today · Mar 2017
ReviewTargeting tuberculosis using structure-guided fragment-based drug design.
Fragment-based drug discovery is now widely used in academia and industry to obtain small molecule inhibitors for a given target and is established for many fields of research including antimicrobials and oncology. Many molecules derived from fragment-based approaches are already in clinical trials and two - vemurafenib and venetoclax - are on the market, but the approach has been used sparsely in the tuberculosis field. Here, we describe the progress of our group and others, and examine the most recent successes and challenges in developing compounds with antimycobacterial activity.
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The term 'prodrug' was first introduced by Albert in 1958. Generally, prodrugs can be utilized for improving active drug solubility and bioavailability, increasing drug permeability and absorption, modifying the distribution profile, preventing fast metabolism and excretion, and reducing toxicity. ⋯ Most antitubercular agents are defined as 'prodrugs', including isoniazid and ethionamide. Thus, the prodrug approach could provide novel targets for the rational design of more effective treatments for tuberculosis (TB).
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Drug discovery today · Dec 2016
What will the crowd fund? Preferences of prospective donors for drug development fundraising campaigns.
Biomedical researchers are increasingly turning to project-based online fundraising (i.e., crowdfunding) as a complementary source of research funding. To help inform the fundraising strategies adopted by researchers who take this approach, we conducted an online survey of prospective donors in North America. Respondents indicated not only an overwhelming preference for donating to projects conducted by nonprofit research organizations, but also an openness to donating to companies that have a 'for-benefit' corporate structure. They also showed a strong preference for projects that have alternate sources of funding, that have the potential to yield a curative therapy, and that focus on common and pediatric diseases.
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Drug discovery today · Nov 2016
ReviewTriple inhaled therapy for chronic obstructive pulmonary disease.
Combining individual drugs in a single inhaler is the most convenient way to deliver triple therapy. A long-acting muscarinic receptor antagonist (LAMA) added to an inhaled corticosteroid (ICS)/long-acting β2-adrenoceptor agonist (LABA) fixed-dose combination (FDC) can improve efficacy of pharmacological treatment of patients with chronic obstructive pulmonary disease (COPD). ⋯ Triple inhaled therapy might be particularly useful in patients with severe to very severe COPD, above all in those with peripheral blood or sputum eosinophilia, asthma-COPD overlap syndrome (ACOS) or frequent exacerbators. Future prospective studies should assess efficacy and safety of triple ICS/LABA/LAMA therapy in selected COPD phenotypes.