Molecular Enzymology and Drug Targets

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Mini Review - (2022) Volume 8, Issue 6

A Short Note on Molecular Drug Targets and its Types

Iysha Mariyam*
Department of Molecular Biology and Biochemistry, University of California, Irvine Irvine, CA 92697-2025, USA
*Correspondence: Iysha Mariyam, Department of Molecular Biology and Biochemistry, University of California, Irvine Irvine, CA 92697-2025, USA, Email:

Received: 01-Dec-2022, Manuscript No. Ipmedt-22-13337; Editor assigned: 05-Dec-2022, Pre QC No. Ipmedt-22-13337; Reviewed: 19-Dec-2022, QC No. Ipmedt-22-13337; Revised: 26-Dec-2022, Manuscript No. Ipmedt-22-13337; Published: 30-Dec-2022, DOI: 2572-5475- 08.06-119


The outcome of instrument put together medication revelation depends with respect to the meaning of the medication target. As we try to connect drug response to genetic variation, comprehend stratified clinical efficacy and safety, explain the differences between drugs in the same therapeutic class, and predict drug utility in patient subgroups, this definition takes on even greater significance. However, the literature frequently provides inadequate definitions of drug targets, both for currently being developed therapeutic agents and for drugs that have already been approved for use. An updated and comprehensive map of approved drugs' molecular targets is presented here. Information that can lead to an avalanche of therapeutic targets can be obtained through access to the complete sequences of pathogenic organisms and the human genome. One of the first methods used in drug design is structure-based design. Finding and enhancing the 3D structure (binding and/or active site) of a target molecule, such as a receptor protein, is specifically referred to as structure-based design. This review aims to provide an overview of studies in the field of structure-based drug design that have aided in drug discovery. Comparative and homology modeling will be the primary focus. We curate 893 biomolecules derived from humans and pathogens, which are used in 1,578 US FDA-approved drugs. These biomolecules include 667 proteins that are derived from the human genome and are the targets of drugs that treat human disease. The analysis of these drug targets reveals not only the expansion of novel first-in-class mechanisms, particularly in oncology, but also the continued dominance of privileged target families across disease areas. We investigate the presence of orthologues between human and animal models, as well as between pathogen and human genomes, as well as the connections between bioactivity class and clinical success. Through the cooperation of three autonomous groups, we feature a portion of the continuous difficulties in precisely characterizing the objectives of sub-atomic therapeutics and present shows for deconvoluting the intricacies of atomic pharmacology and medication viability.


Drug targets; Protein modeling; Ligands; Design


All small molecules and biologics that are currently approved (or have previously been approved) by the US FDA (before June 2015) to enhance human health, in addition to antimalarial drugs that are approved elsewhere in the world, are included in this definition of a "drug," which only includes therapeutic ingredients. Imaging agents, nutritional supplements, sunscreens, and vaccines are not considered drugs [1]. In addition, the numbers presented in the paper are for parent compounds after pharmaceutical salts have been removed. Due to the variety of required information sources and the number of different regulatory agencies involved, it is extremely difficult to identify a complete set of drugs that have been approved anywhere in the world. Additionally, the lack of information presents a problem; For instance, the European Medicines Agency does not have data on drug approvals prior to 1995, and the Japan Pharmaceutical and Medical Devices Agency has only published lists of drug approvals in English since 2004 (see Additional information). However, we also identified a group of more than 1,200 drugs that have been approved by other agencies but have not yet been approved by the FDA [2]. The novel targets in this group are discussed separately. With the discovery of the three-dimensional structures of globins, enzymes, and polypeptide hormones, discussions of the application of structural biology in drug discovery began more than 35 years ago. The chemical modification of insulins to increase half-lives in circulation, the design of inhibitors of serine proteases to control blood clotting, and the use of 3D structures to guide the synthesis of ligands of haemoglobin to decrease sickling or improve blood storage were among the earliest ideas in circulation. The UK Wellcome Foundation's 1975 program on haemoglobin structures was an early and daring initiative. However, X-ray crystallography required a lot of time and money. This method could not be brought "in-house" into industrial laboratories, and the pharmaceutical industry initially did not really embrace it. Over time, drug design was informed by understanding the 3D structures of target proteins [3]. Comparative models based on homologues began to be utilized in lead optimization in the 1980s, despite the fact that the relevant drug targets' structures were rarely accessible directly from X-ray crystallography in the early days. A model was the utilization of aspartic protease designs to display renin, an objective for antihypertensive.

Types of drug targets

Drug Target

The development of genomics, proteomics, and metabolomics has opened the door to biologically driven processes, which has resulted in an abundance of drug targets. The rundown of potential medication targets encoded in a genome incorporates generally normal decision of destructive qualities and speciesexplicit qualities [4].

Species-Specific Genes as Drug Targets

The first insights into the approaches that will be used in the near future for drug discovery are provided by comparing the complete genome sequences of bacterial pathogens that are available in the public databases. Bork and colleagues have proposed the differential genome display, an intriguing method for predicting potential drug targets. The fact that parasitic microorganism genomes are typically much smaller and encode for fewer proteins than those of free-living organisms is the foundation of this strategy. As a result, the genes that are found in the genome of a parasitic bacterium but not in the genome of a free-living bacterium are likely to be important for pathogenecity and could be targets for drug [5, 6]

Nucleic Acid as Drug Targets

Nucleic acids are the repository of genetic information. DNA itself has been shown to be the receptor for many drugs used in cancer and other diseases [7]. These work through a variety of mechanisms including chemical modification and cross linking of DNA (cisplatin) or cleavage of the DNA (bleomycin). Much work either by intercalation of a polyaromatic ring system into the double stranded helix (actinomycin D, ethidium) or by binding to the major and minor grooves of DNA has been reported.

RNA as drug target

New opportunities that will have a significant impact on the pharmaceutical industry have emerged as a result of recent advancements in the investigation of RNA structure and function. It was thought that RNA, which communicates with proteins and DNA among other things, was a completely flexible molecule with little structural complexity. However, recent research has demonstrated a surprising complexity in the structure of RNA. The pharmaceutical industry now has new opportunities to target RNA with small molecules thanks to this observation. More importantly, drugs that bind to RNA may have effects that drugs that bind to proteins can't have [8, 9].

Membranes as drug targets

Membranes are important structural components because they not only help define a cell's boundaries but also provide interior compartments within the cell that are associated with particular functions. Cell layers themselves can likewise go about as focuses for atomic acknowledgment. Drug molecules with improved permeation characteristics or specific membrane effects may benefit from an understanding of the structural and dynamic functions of membranes, such as plasma membranes and intercellular membranes. When dissolved in membranes, many general anesthetics are thought to work by their physical effects.

Proteins as drug targets

The pharmaceutical and biotechnology industries continue to pay a lot of attention to proteins as a useful source of potential drug targets. Proteins are the key to understanding fundamental biological processes like disease pathology, diagnosis, and treatment because they provide the crucial link between genes and disease. Over 700 products are currently in various stages of development, and researchers have discovered numerous potential therapeutic targets. However, there are significant obstacles in converting protein research into validated drug targets. Genome arrangements teach cells on how and when to make proteins. The cell's active players are, in turn, the proteins. Proteins control an organism's growth or death, enable cells to communicate with one another, and form the machinery of cells [10].


With a focus on the trends and shifts that have occurred over the past ten years7, we have provided an enhanced and updated perspective on the current diversity of approved drugs and their targets in this article. It is not an easy task to compile a comprehensive list of drug efficacy targets, but with the help of three teams, we have demonstrated some of the practical obstacles and made significant progress toward this objective. These difficulties include determining the non-trivial relationship between a drug target and a gene, assigning the target, and finally establishing a method for counting final effective molecular targets that takes into account complexes, subunits, splice variants, and protein isoforms a major reason why the number of protein targets increased to 667 from 324 in our previous study7.

Analyzing the variety of existing drugs and targets in light of their disease coverage requires all of this. These annotations, on the other hand, will need to be updated on a regular basis due to the constant evolution of drug mechanism of action knowledge in the literature.

As a result, research in biotechnology and pharmaceuticals has undergone significant change. The industry's search for new drug targets has traditionally been hampered by a lack of biological data. Bioinformatics now offers a number of methods for predicting the structure and function of proteins based on similarities in sequence and structure thanks to the release of the human genome's sequence. Rational drug design is now possible thanks to impressive technological advancements in computer science, molecular biology, and structural characterization of bio macromolecules.



Conflict of Interest



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Citation: Mariyam I (2021) A Short Note on Molecular Drug Targets and its Types. Mol Enzy Drug Targ, Vol. 8 No. 6: 119.