The Role of the Medicinal Chemist in the Drug Discovery

Medicinal chemistry is amongst the most stimulating fields of science. Acting as a link between several disciplines (synthetic organic chemistry, pharmacology, and other biological sciences) it allows the collaboration of scientists from various fields to research, discover and develop new drugs.

A recent study revealed that the average cost to develop a new drug from scratch can take anywhere between $800 million to $1 billion. Hence, the process of drug discovery and development is amongst the most complex and expensive procedures of the pharmaceutical industry.

Over the past several years, the process of drug discovery has undergone several changes. However, its goal has remained unchanged- to develop safe and effective drugs for the treatment of diseases. Since drug discovery plays a crucial role in the pharmaceutical industry, it must be ensured that the person responsible for it possesses the necessary skills and knowledge. In this case, the key person is the medicinal chemist.

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Undertaking the responsibility of isolating the medicinal agents from plants and the creation of new synthetic drug compounds, the medicinal chemistry services offer several vital aids to optimize discovery process. Here are a few of them:

1. Target identification and validation

Medicinal chemists play a significant role in the process of drug discovery as they ensure that the target identification and validation step is executed properly. Target identification refers to the process of identifying a biological target that is ‘druggable’- to confirm whether its behavior or function can get altered through a therapeutic. On the other hand, target validation refers to the process of demonstrating the functional role of the identified target.

2. Discovery of molecules

Discovery of molecules is the fundamental role of every medicinal chemist, as it is a crucial part of drug discovery. Over a period, technology has changed the way of how the drug discovery companies conduct the discovery of molecules. It is because of these technologies the process of drug discovery has accelerated. A few of these technologies are as follows:

• Combinatorial chemistry– This consists of several chemical synthetic methods that allow the preparation of a large number of compounds (tens of thousands to millions) within a single procedure. Through this method, large libraries of molecules can get created within a short period of time.
• High-Throughput Screening (HTS)– It is another method of drug discovery that enables the automated testing of a large number of biological compounds for a particular biological target. Extensively used by medicinal chemists, they are a cost-effective way of screening huge compound libraries.

Apart from these two methods, Microwave Assisted Organic Synthesis (MAOS) is also used by medicinal chemists for the discovery of molecules.

3. Taking part in Hit-To-Lead studies

After the hits are identified from High-Throughput Screening (HTS) or from any other method, the medicinal chemist gets involved in Hit-To-Lead studies. Through these studies, the hits are screened effectively and scrutinized carefully so that they can get used in the form of lead compounds. Hence, the primary goal to carry out this study is to identify several promising hits that can serve as drug candidates.

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Asides from these roles and responsibilities, the chemist would also be counted upon for purification and proper characterization of the new chemicals. Moreover, he/she would also be responsible for developing in vivo activity for the hit compound in a suitable animal model.

Hence, the modern medicinal chemist plays a vital role in the early stages of drug discovery. The medicinal chemist would help in shaping the hypothesis for the new drug project. The hypothesis would further get used for establishing the objectives of the new drug project.

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