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High Throughput Screening (HTS) is a powerful and automated scientific method used in various fields, particularly in drug discovery, materials science, and biological research.
It involves the rapid testing of a large number of diverse compounds or samples for specific biological or chemical activities.
The primary goal of high throughput screening is to identify potential hits or leads that exhibit desired properties, such as the ability to interact with a target molecule, inhibit a biological process, or display certain characteristics.
The process of high throughput screening generally follows these steps:
High throughput screening has revolutionized the drug discovery process by significantly increasing the speed and efficiency of identifying potential drug candidates.
It has found applications in various other fields, such as identifying catalysts in materials science, characterizing protein interactions, and uncovering potential therapeutic agents in personalized medicine.
In summary, high throughput screening is a cutting-edge approach that allows researchers to quickly sift through vast numbers of compounds or samples, pinpointing those with desired properties for further development, thereby accelerating scientific discovery and innovation.
These days you can get everything tailormade.
If it’s shoes or if it’s jewelery or even a car.
You can design things and customise each and every spec.
Well, the same concept of customization can be done to molecules. This is what custom synthesis is all about.
Custom synthesis refers to the tailored production of specific chemical compounds, molecules, or materials based on unique requirements provided by a client or researcher.
Instead of using readily available chemicals, custom synthesis involves designing and producing compounds that may not be readily accessible in the commercial market.
This process typically involves specialized chemical reactions, techniques, and equipment to create the desired compounds.
Custom synthesis can be employed in various industries, including pharmaceuticals, biotechnology, materials science, and research, where researchers or companies require compounds for specific purposes that are not easily obtainable through standard methods.
The custom synthesis process typically involves the following steps:
If looking for these special molecules one would collaborate with specialized laboratories or contract research organizations with expertise in organic chemistry.
The chemists in these labs would design & perform a series of intricate chemical reactions to synthesize the exact compound they need.
This involves selecting the appropriate starting materials, developing reaction pathways, and optimizing conditions to yield the desired compound efficiently and with high purity.
In essence, custom synthesis offers a bespoke approach to chemical production, allowing researchers and industries to obtain the precise compounds they need for their projects, even if those compounds are not available through off-the-shelf sources.
It is a tool to help scientists and researchers shape a healthier future.
In the Biotech or Pharma industry you hear the phrase ‘hit to lead’ a lot.
But what does it mean?
In the pharmaceutical and biotech fields, the “hit to lead” concept refers to the process of refining and optimizing a potential drug candidate from a pool of initial “hits” – compounds that exhibit some level of biological activity against a target, such as a disease-causing protein.
Hit to lead is a stage in early drug discovery.
Imagine you’re searching for a key to unlock a door.
The “hits” are like different keys you’ve found that might work, but they’re not perfect fits yet.
And now imagine that you have 100000 to a million keys.
The “hit to lead” process involves taking these initial hits and carefully modifying their chemical structures
to enhance their potency, selectivity, and safety profile.
Scientists analyze the hits’ interactions with the target, test variations of the chemical structure, and perform experiments to ensure that the modified compounds maintain or improve their effectiveness while inimizing negative side effects.
“hit to lead” is a crucial step in drug discovery.
It transforms these early potential drug candidates into more advanced “lead compounds” that have higher chances of success in becoming safe and effective medicines.
The process involves a blend of chemistry, biology, and data analysis to iteratively improve the properties of the compounds, setting the stage for further development and testing in the journey toward a new drug.
In wrapping up our exploration of the “hit to lead” process, we’ve witnessed the conversion of scientific potential into concrete advancement.
From initial hits to refined lead compounds, this journey highlights researchers’ dedication to creating impactful medicines.
“Hit to lead” serves as a pivotal step, propelling us toward innovative treatments that can make a real difference in healthcare.
It embodies collaboration, creativity, and a relentless drive to shape a healthier future.
In the dynamic journey of drug discovery, lead optimization is a pivotal phase that propels a promising compound towards its full therapeutic potential.
Imagine identifying a lead compound—like finding a key that unlocks the door to a potential breakthrough drug.
This is where lead optimization steps in, serving as a critical refining process, much like sculpting a raw gem into a polished jewel.
When placing Lead Optimization in the drug discovery pipeline It can be placed right after Hit to Lead and before Phase One of the Clinical trials.
The amount of compounds in this phase lies at 10 to 100.
Lead optimization is about fine-tuning the chemical structure of the lead compound to enhance its effectiveness, safety, and overall suitability for becoming a successful therapeutic drug.
Medicinal chemists lead this process, strategically modifying the molecular architecture to boost the compound’s potency against the targeted disease, while minimizing any unwanted side effects.
These chemists explore a realm of possibilities, employing computational tools to predict the impact of structural changes.
The goals are clear:
Once this refining process is complete, the optimized lead compound moves on to the next stages of preclinical development, undergoing rigorous testing to assess its safety and efficacy.
In essence, lead optimization is the bridge between discovery and development, transforming a promising lead compound into a well-crafted candidate ready for the challenges of preclinical and clinical trials.
It’s the art and science of turning a potential breakthrough into a tangible solution that holds the promise of improving lives.
Medicinal chemistry is a scientific discipline at the intersection of chemistry, pharmacology, and biology.
It involves the design, development, and study of compounds (chemical substances) with the potential to become pharmaceutical drugs.
Medicinal chemists work to create new drugs or improve existing ones by understanding the molecular and chemical aspects of how drugs interact with the human body.
The primary goals of medicinal chemistry include:
Medicinal chemists are high in demand these days, especially in the biotech and pharma industry, due to constant Need for New Drugs, Complex Diseases and Health Challenges, Advancements in Personalized Medicine, Global Health Challenges Technological Advancements and Retirement & Skill Gap.
Medicinal chemists utilize principles of chemistry, biochemistry, molecular biology, and pharmacology to design and synthesize molecules that can effectively treat diseases while minimizing adverse effects.
These professionals play a crucial role in advancing the field of medicine and improving the quality of healthcare by creating more effective and safe pharmaceuticals.
Biotechnology, often abbreviated as biotech, is a broad field that involves the use of living organisms, cells, and biological systems to develop new products and technologies for various applications.
It merges biology and technology to create innovative solutions that impact multiple industries including medicine, agriculture, food production, and environmental management.
Key areas within biotechnology are:
Here are 3 notable Biotech companies yu should know:
Amgen Inc.: Amgen is a multinational biopharmaceutical company known for its focus on developing and manufacturing therapies for serious illnesses, including cancer, cardiovascular disease, and autoimmune disorders.
Gi-leed Sciences, Inc.: Gi-leed is recognized for its work in antiviral drugs and has played a significant role in the development of treatments for HIV/AIDS and hepatitis C.
Genentech (Rosh Group): Genentech, a subsidiary of Rosh, is a leading biotechnology company specializing in the development of drugs for oncology, immunology, and other therapeutic areas.
Biotechnological processes often involve genetic engineering, where the DNA of living organisms is manipulated to achieve specific outcomes.
This may include the insertion, deletion, or modification of genes to confer desired characteristics or functions.
In conclusion one can describe Biotechnology as a dynamic field driven by scientific discoveries and technological advancements.
It addresses global challenges through genetic engineering, creating solutions for disease therapies, sustainable agriculture, and eco-friendly industrial processes.
Taros compound library designs target underpopulated druglike chemical space.
High quality compound libraries require chemical creativity and profound high throughput synthesis knowledge to achieve the highest possible molecular
diversity.
This commitment is mirrored in our efficient production processes, which leverage parallel synthesis and high-throughput purification techniques.
By optimizing these processes, Taros effectively reduces costs per compound, ensuring affordability without compromising quality.
Our track record speaks volumes about our capabilities. The leadership role in initiatives like the European Lead Factory ELF highlight our success in designing,
synthesizing, and delivering over 40,000 screening compounds from a vast array of chemical scaffolds.
As an executive member and head of the chemistry consortium within ELF, we led a collaborative effort involving seven companies and ten academic groups
throughout Europe, resulting in the development of the ELF public compound collection comprising more than 300,000 novel and lead-like screening compounds.
One of our flagship offerings is our unique library of 30,000 novel compounds, characterized by drug-like physico-chemical properties and relevance to medicinal chemistry.
Our library designs feature a remarkably lower c-logP, an increased number of chiral atoms, and a balanced ratio of hydrogen bond acceptors and donors.
Unlike commercially available options, our libraries prioritize 3D character directly engineered into the scaffolds, enhancing their drug-likeness.
Guided by our experienced medicinal chemists, our libraries are adorned with chemical building blocks of utmost medicinal chemistry relevance, ensuring
rapid lead identification.
Taros compound libraries embody a harmonious blend of innovation, efficiency, and quality, making us a trusted partner in the journey of drug discovery.
Nitrosamines are a group of chemical compounds that contain the nitroso functional group. They are organic compounds that are characterized by the presence of a nitric oxide group which is attached to an organic moiety . Nitrosamines can also include other atoms and functional groups attached to the nitrogen atom, leading to a of different nitrosamine compounds.
So, why are nitrosamines a concern in APIs?
During the manufacturing process, nitrosamines can form under specific conditions, such as high temperatures, acidic environments, or in the presence of certain catalysts and solvents.
Nitrosamines are chemical compounds, most of which are classified as probable human carcinogens and their presence in pharmaceuticals is a significant issue for both drug manufacturers and regulators.
A recent challenge for the biotech and pharmaceutical industries has been that the presence of nitrosamine impurities in pharmaceuticals has led to recalls of several medications. Biotech and pharmaceutical companies need to implement robust quality assurance measures to detect and prevent the presence and formation of nitrosamines in their drugs, ensuring patient safety and maintaining the integrity of their brands.
This includes engaging in extensive analytical testing to detect and quantify nitrosamine impurities in products and focusing on developing new and improved manufacturing processes that avoid the formation of nitrosamine impurities.
It’s important to note that not all nitrosamines are necessarily harmful, and the risk they pose to health can depend on factors like the specific nitrosamine compound, the level of exposure, and an individual’s susceptibility. Nonetheless, efforts are made to minimize exposure to potentially carcinogenic nitrosamines in various products to protect public health.
TPD isn’t just another method; it revolutionizes our
approach by eliminating malfunctioning proteins, which are often at the root of diseases.
This innovative technology uses Pro-tacs, or Proteolysis
Targeting Chimeras, which are specially designed to target and destroy disease-causing proteins. The power of Pro-tacs lies in their selectivity, engineered to target specific proteins, ensuring minimal side effects while tackling diseases.
One standout example is ARV110, a Pro-tac in Phase-2 clinical trials, which selectively degrades the Androgen receptor among 4000 similar targets. The architecture of Pro-tacs is key. They consist of two main parts: one binds to the target protein, and the other to an E3 ubiquitin ligase, connected by a linker.
Researchers are exploring various E3 ligases and the role of Pro-tac linkers, based on flexibility and diversity, which are crucial in determining the stability and specificity of the degradation process.
Globally, the biotech and pharmaceutical sectors are heavily investing in TPD research, driven by its potential to address complex diseases like cancer, neurodegenerative disorders, HIV, and resistant bacterial infections. Several clinical trials are currently assessing the efficacy of Protacs, with promising results that may soon revolutionize therapeutic approaches.
Through the power of TPD, we are entering a new era of drug discovery, where we don’t just manage diseases – we aim to end them.
