drug target Articles
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Triiodophenyl acrylate–based microbeads find important use in the medical field
Preparation of polymeric micro– and nanoparticles has significantly become an effective approach for achieving efficient drug targeting to tumour tissues. A promising solution could be the use of a radio–opaque polymeric system carrying iodine groups. In this context, radio–opaque polymeric microparticles based on methyl methacrylate (MMA) and an 2,4,6–triiodophenyl acrylate (TIPA) were ...
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Challenges in Small Molecule Targeted Drug Development
The classical mode of action of small molecule drugs is "occupancy-driven". Since the FDA approved the first oral small molecule targeted therapy for tumors-tamoxifen targeting the estrogen receptor (ER)-in 1977 for the treatment of breast cancer, small molecule drug development has typically focused on screening for high-affinity inhibitors. Small molecule inhibitors can bind to the active sites ...
By BOC Sciences
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Finalists for AstraZenca Cosolve
Kumuda was selected as a Finalist awardee for AstraZeneca’s (AZN) Open Innovation CoSolve 2! The proposal is entitled “Systems-based druggability identifies potential drugs and targets to modulate Class B G-protein-coupled receptors (GPCRs).” ...
By Kumuda
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The Protein Data Bank has Over 200,000 Structures
Structural biology is an important field in drug discovery as it helps researchers understand the three-dimensional structure of proteins and how they interact with other molecules. This knowledge is crucial in developing new drugs as it allows scientists to target specific proteins and understand how they contribute to diseases. One of the most important resources in structural biology is the ...
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G Protein-Coupled Receptors targeted by antibodies raised against three dimensional epitopes
Why target GPCRs with antibodies? The G Protein-coupled receptor (GPCR) superfamily represents the largest and single most important family of human drug targets. GPCRs play a central role in a plethora of biological processes and are linked to a wide range of therapeutic areas including cancer, diabetes, inflammation, cardiovascular diseases, and chronic pain. Expressed in every type of cell in ...
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Drug Discovery: Unraveling the Mysteries of Therapeutic Agents
In the vast and ever-evolving field of medicine, the discovery of new drugs has been a critical pursuit, offering hope and relief to countless individuals suffering from various ailments. The process of drug discovery is a complex and multifaceted endeavor, involving the integration of diverse scientific disciplines, including biology, chemistry, and computational science. At the heart of this ...
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Co-Immunoprecipitation (Co-IP): A Comprehensive Guide
Introduction Co-immunoprecipitation (Co-IP) is a versatile and powerful laboratory technique employed to elucidate protein-protein interactions. It is particularly valuable for identifying and characterizing protein complexes involved in various cellular processes. The technique relies on the specificity of antibodies to selectively capture a protein of interest (bait) from a complex mixture, ...
By Profacgen
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Nanoparticulate systems for oral drug delivery to the colon
A review of oral drug delivery to the colon is a difficult but desirable method of administration. In order to target the colon the dosage form must overcome the barriers presented by the gastrointestinal tract including the steep pH gradient, binding to the mucus layer, premature clearance, and premature cellular uptake. Nanoparticles have been fabricated via a number of methods and designed ...
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Nanogenomics for medicine: emerging strategies to overcome bottlenecks in siRNA-based therapy of human diseases
Silencing of gene expression by siRNA holds a promise both for a drug target discovery and as a therapy. Major bottlenecks of siRNA technology include 'off-target' silencing effects and problems with siRNA degradation before delivery. We propose a two-fold approach aimed at curtailing described shortcomings. First, before pre-clinical tests each siRNA shall be matched to comprehensive redundancy ...
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The linker matters in antibody-drug conjugates - Case Study
It was Paul Ehrlich who first brought up the idea of creating a magic bullet that selectively delivers drugs to malicious tissues while sparing the healthy parts. Roughly a century later, researchers started to attach cytotoxic compounds through linkers to antibodies for a targeted drug delivery approach, given the highly selective binding properties of antibodies. It turned out though that ...
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Unlocking the secrets of cellular uptake: paving the way for new cancer and disease treatments
Drug development is a balancing act between ensuring that the drug is suitable for the target and that the drug can penetrate the cell membrane to reach the target. Typically, research into drugs that can cross cell membranes has focused on small, rigid molecules with nonpolar chemical structures. However, new therapeutic strategies break traditional drug design rules by using larger, flexibly ...
By Profacgen
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Understanding Drug-Disease Relationship Analysis: A Key to Drug Discovery
In the realm of modern medicine, the quest for new and effective drugs to combat various diseases is a continuous journey. Drug discovery, the process of identifying compounds that can potentially treat diseases, has seen a significant transformation in recent years, thanks to advancements in computational biology and artificial intelligence (AI). In this article, we will delve into the ...
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Non–covalent surface integration: optimising a novel technique for preparing targeted polymeric nanoparticles for cancer therapeutics
Targeting anticancer drugs to their specific molecular targets is a major challenge in cancer therapy. However, advances in biomedical and protein engineering have led to novel nanoparticle targeting approaches. In this study, we used a novel non–covalent insertion of a homo–bifunctional spacer for targeted delivery of drugs to various cancer cells. Functionalised blank nanoparticles for antibody ...
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Function of heterologous mycobacterium tuberculosis inha, a type 2 fatty acid synthase enzyme involved in extending c20 fatty acids to c60-to-c90 mycolic acids, during de novo lipoic acid synthesis in saccharomyces cerevisiae
We describe the physiological function of heterologously expressed Mycobacterium tuberculosis InhA during de novo lipoic acid synthesis in yeast (Saccharomyces cerevisiae) mitochondria. InhA, representing 2-trans-enoyl-acyl carrier protein reductase and the target for the front-line antituberculous drug isoniazid, is involved in the activity of dissociative type 2 fatty acid synthase (FASII) that ...
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Abalone conservation in the presence of drug use and corruption: implications for its management in South Africa
The illegal exploitation of wild abalone in South Africa has been escalating since 1994, despite increased enforcement, leading to collapse in some sections of its range. South Africa banned all wild abalone fishing in 2008 but controversially reopened the fishery in 2010. This paper formulates a poacher's model, taking into account the realities of the abalone terrain in South Africa - the ...
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Rationalising fixed dose combinations for tuberculosis and acquired immunodeficiency syndrome therapy
Poorly managed healthcare can be directly attributed to extensive drug regimens. Numerous chronic illnesses and epidemics such as HIV/AIDS and tuberculosis require elaborate drug regimens for efficacious therapeutic outcomes. Various drug delivery systems have been developed to simplify their regimental drug therapy. However, more effective and innovative drug delivery technologies are required ...
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Four Well-Established Strategies Used in Hit Identification
The major preclinical phases of peptide drug discovery encompass initial target identification and validation, hit identification, high throughput screening, lead optimization, etc. Among them, hit identification is one of the most critical steps in identifying peptides that can interact with well-validated targets. Hit identification (HI) follows the process of target validation, in which the ...
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Biomedical applications of organically modified bioconjugated silica nanoparticles
Nanoparticles are one of the most important prominent areas in the field of nanotechnology, with a broad significant role in current life sciences and human healthcare applications. Among the nanoparticles silica nanoparticles are explored in many biological applications because their size dependent novel properties and functions differ drastically from those of the bulk materials. In biomedical ...
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Lipidomics in Microbial Research
Lipids are a class of metabolites with diverse chemical structures. More than just components of cell membranes and energy storage substances, lipids can perform a variety of important biological functions in life activities. The structural diversity of lipids endows them with a variety of important biological functions: (1) they constitute an important component of the cell membrane. Many ...
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Decoding Protein Structure Modeling: Unlocking the Key to Life's Mysteries
Proteins are among the most vital molecules in living organisms, playing crucial roles in cell function, signal transduction, and drug development, to name just a few. However, directly observing and studying the three-dimensional structures of proteins is not an easy task. Fortunately, the development of protein structure modeling technology has provided us with a powerful tool to unravel the ...
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