Innovative approaches to expand medicinal chemistry space

نویسنده

  • Gérard Rossé
چکیده

Drug discovery proceeds as a multi-stage process, from the identification of a potential therapeutic target through lead generation, lead optimization, preclinical evaluation to clinical testing, before a new medicine is marketed. Uniting synthetically accessible chemical space with disease relevant biological space represents a significant challenge. Industrial chemical biology approaches have been recognized by pharmaceutical companies as a novel strategy in drug discovery. It encompasses an organizational structure composed of dedicated, specialized teams, thereby enabling a detailed analysis and an optimal use of the chemical and biological space of target classes. The benefits of an industrial chemical biology approaches in combination with automated parallel synthesis and purification will be discussed. A case study for the discovery of novel GPCRs ligands with a focus on the therapeutic areas of Inflammation and Neurobiology will also be presented.

برای دانلود رایگان متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

ثبت نام

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

منابع مشابه

Expanding medicinal chemistry space.

Clinically useful drugs target a relatively small number of proteins that lie within a clearly defined and chemically accessible space. However, many high value biological targets lie outside this chemical space, and an ability to access such 'intractable' targets not amenable to traditional small molecule intervention would expand treatment options and be a major boost for patients and the pha...

متن کامل

Medicinal chemistry research in India.

The beginning of modern drug research in India can be traced to early part of the twentieth century. Dr Upendra Nath Brahmachari worked on drugs for kala-azar at the Campbell Medical College, Calcutta. Colonel Ram Nath Chopra organized an active centre of research on the Indian medicinal plants at the School of Tropical Medicine, Calcutta. The lead given by Chopra led to start of investigations...

متن کامل

Information extraction in the life sciences: perspectives for medicinal chemistry, pharmacology and toxicology.

Information extraction approaches have been successfully applied to mine the scientific literature in biology and medicine. So far, the main focus of research and development in this domain was on the recognition and extraction of gene and protein names in the context of molecular biology and genome research and on disease names and other medical terms in the context of clinical research. Simil...

متن کامل

Preparation and activities of macromolecule conjugates of the CCR5 antagonist Maraviroc.

CCR5 antagonists are among the most advanced approaches in HIV therapy and may also be relevant to treatment of graft-versus-host disease and Staphylococcus aureus infection. To expand the potential of the only approved CCR5 antagonist, Maraviroc, we studied derivatives that would enable functional linkage of Maraviroc to long-lived carriers. Through targeted synthesis, we discovered an effecti...

متن کامل

Chemogenomics approaches for receptor deorphanization and extensions of the chemogenomics concept to phenotypic space.

Chemogenomic approaches, which link ligand chemistry to bioactivity against targets (and, by extension, to phenotypes) are becoming more and more important due to the increasing number of bioactivity data available both in proprietary databases as well as in the public domain. In this article we review chemogenomics approaches applied in four different domains: Firstly, due to the relationship ...

متن کامل

ذخیره در منابع من


  با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید

عنوان ژورنال:

دوره   شماره 

صفحات  -

تاریخ انتشار 2013