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Nanomaterials in Chemotherapy
Published in D. Sakthi Kumar, Aswathy Ravindran Girija, Bionanotechnology in Cancer, 2023
P. K. Hashim, Anjaneyulu Dirisala
A drug is defined as a natural or artificial pharmacologically active ingredient used for the detection, diagnosis, and treatment of a disease. A drug can be either hydrophobic (e.g., paclitaxel, cisplatin, and methotrexate) or hydrophilic (e.g., gemcitabine, L-asparaginase, and antibodies) depending on its aqueous solubility [1]. Also, a drug can be negatively charged (e.g., gene therapeutics such as DNA, messenger (m)RNA, and short interfering (si)RNA), positively charged (e.g., doxorubicin (DOX)), and neutral (e.g., cisplatin) based on the charged species present in the drug. A drug also can be a small molecule, which has a low molecular weight compound below 900 daltons (e.g., DOX and cisplatin), or a high molecular weight molecule (e.g., DNA, RNA, and proteins). The structural characteristics of drugs are often related to their functions. For instance, a small molecule drug usually binds to a target gene/protein as a first step in the complicated drug action mechanisms. Small molecule drugs often induce off-target adverse effects because of their lack of specificity. In contrast to small molecule drugs, macromolecule drugs (e.g., genes and proteins) typically bind to their target either expressed on the cell surface or intracellular component with high specificity, and correct or program the disease-causing elements. Advantageously, both small molecule- and macromolecule-drugs can be used for cancer therapy. Collectively, more than 150 anticancer drugs have been approved by the US Food and Drug Administration (FDA) for various types of cancer [2].
Appliance of Machine Learning Algorithms in Prudent Clinical Decision-Making Systems in the Healthcare Industry
Published in Ashish Mishra, G. Suseendran, Trung-Nghia Phung, Soft Computing Applications and Techniques in Healthcare, 2020
T. Venkat Narayana Rao, G. Akhila
The binding of drug molecules is made to be structurally similar native ligands (candidate keys). These are fake duplicate keys, close enough to fit the hole but not of the right shape to turn the block. Most of the current drugs are ‘small molecules’. Apart from that, other classes of medicines exist and are being developed, such as biologic drugs or therapeutic antibodies.
Active Nanoparticle Targeting: Current Status and Future Challenges
Published in Sandeep Nema, John D. Ludwig, Parenteral Medications, 2019
Siddharth Patel, Janni Mirosevich
Nanoparticle-based delivery of small-molecule drugs predominates the research literature and has shown the most progress in the clinical setting (Duncan and Vicent 2013; Sanna, Pala, and Sechi 2014). In recent years, nanotechnologies that deliver biologics such as nucleic acid (deoxyribonucleic acid [DNA], small interfering ribonucleic acid [siRNA], messenger ribonucleic acid, and aptamers) and peptide (peptides and proteins)-based therapeutics have also emerged with varying degrees of success (Kamaly et al. 2012). Both small molecules and biologics have their own distinct challenges, mechanism of action, and stability issues. Regardless of the cargo, a major biological barrier to any drug delivery system is the nonspecific uptake by the reticuloendothelial system (RES) (Chrastina, Massey, and Schnitzer 2011; Brannon-Peppas and Blanchette 2012). The RES consists of a host of cells that are designed to remove cellular debris and foreign particles from the bloodstream. Similar to viruses, synthetic nanoparticles are more adept at escaping RES detection by the nature of their size. In addition, the covalent attachment of polyethylene glycol (PEG) is a commonly used method to reduce opsonization and nonspecific RES uptake of small molecule, protein, and nanoparticulate drug carriers (Prencipe et al. 2009).
Synthesis and characterisation of formohydrazide derivatives as potential antimicrobial agents: molecular docking and DFT studies
Published in Molecular Physics, 2022
S. Gunavathi, R. Venkateswaramoorthi, K. Arulvani, S. Bharanidharan
For the synthesis of new drugs, small molecules have played an important role because they have low molecular weight, are easily ingestible, are immediately absorbed, easily penetrate cell membranes, and are capable of modulating biochemical processes [2]. Small molecule drugs include Isoniazid, Chloropromazine, Chloroquine, Chlorpromazine, Barbituric acid, Captopril, Diazepam and Azidothymidine have been continued to dominate in the pharmaceutical field [3] due to their structure, function, potency, medicinal usages, ease to make, and highly profitable. Nitrogen-containing small molecules, particularly hydrazones in DFT [4–8], Docking [9,10], Inhibition [11] and spectroscopic [12] studies were investigated and significant extensively used building blocks in pharmaceutical drug discovery systems such as Anticancer [13–15], Antihypertensive [16], Antileishmanial [17], Anti-inflammatory [18], Antituberculosis [19], Antimicrobial [20,21], Antioxidant [22,23], Anti proliferative [24,25], Antitumour [26] and Antiviral [27] activities. Hydrazones have functional diversity of C = N-N moiety and the structure shows nucleophilic imine, electrophilic and nucleophilic character carbon, the intrinsic nature of C = N bond and acetic NH proton and which are determined the physical and chemical properties of the corresponding biomolecules [28].