Solute carriers (SLCs) have often been overshadowed by more prominent protein families in drug discovery, such as kinases and G protein-coupled receptors. However, SLC proteins hold significant therapeutic potential due to their role in various diseases. Among them, the high-affinity norepinephrine transporter (NET/SLC6A2) has received considerable attention, but the limited chemical diversity of known ligands presents a challenge for identifying novel compounds. The new article published in Journal of Chemical Information and Modeling explores a computational screening pipeline developed to discover new NET inhibitors, utilizing a data-driven approach to expand known chemical space and optimize target selection.
Preparation of the screening libraries from the stock in dry powders always takes extra time and, in many cases is uneconomical due to compound waste.
Enamine’s Liquid Stock collection backed with our state-of-the-art compound management provides time- and cost-effective solution for design of the bespoke libraries easily customizable in terms of both composition and format. This collection currently consists of more than 296,000 compounds stored as 10 mM DMSO solutions available for cherry-picking.
No doubt Fluorine is an extremely important element for Medicinal chemistry. There are tons of reviews with numerous examples of cases when the introduction of Fluorine or fluorinated groups led to the improvement of activity, selectivity, ADME-properties of the molecules therefore every year we commonly see many fluorinated molecules among FDA-approved drugs.
Dear Customers, Dear Colleagues, Dear Friends.
This morning, russia carried out another act of aggression, firing dozens of rockets at peaceful cities in Ukraine, including Kyiv. Another act of barbarian terrorism. Despite it, we stand firm and resilient.
All our employees are safe, and all our facilities are intact. The work has been postponed for today, but it will be resumed tomorrow with the support of our local authorities and government. At Enamine, we are acting according to our internal contingency plan. Once the air raid alarm starts, all the laboratory activity is stopped, and our staff is evacuated to the specially equipped shelters.
Deucravacitinib(FDA-approved on September 9, 2022)
A week ago, FDA-approved TYK2 inhibitor deucravacitinib (trade name Sotyktu) for moderate-to-severe plaque psoriasis and there are several reasons which make the news remarkable.
Last week there was news that is remarkable for the Ukrainian chemical community. Kyiv administration agreed on the renaming of Murmanska street. Now this street will be named after Academician Valery Kukhar.
Such a renaming is a part of the huge campaign in Kyiv and other Ukrainian cities aiming to remove the names of Russian-related names of streets, squares and other objects and give them actual names.
The interest of pharmaceutical companies in DNA-encoded chemical libraries (DEL) technology has been growing over the years, with numerous organizations now having their own screening programs using DELs, or outsourcing capabilities from specialized DEL providers.
There are not so much info in the media about this story however I suppose it is remarkable. And while it is not completely my topic, I suppose it is worth sharing, because it obviously demonstrates how innovative products of biotech can help Ukraine today.
Time for the Enamine Store update
We are excited to announce that despite all the difficulties we faced with the Russian Invasion of Ukraine we are launching an all-new user interface for our web store.
Our team has been working tirelessly to upgrade our enaminestore.com over the past year. We believe that our reimagined design will help you enjoy your experience and make our services easier to use.
Visit new web store
Structures of first DUBTACs (from Nature Chemical Biology volume 18, pages 412–421, 2022)
Few weeks ago a new biotech appeared on the map: Vicinitas Therapeutics launched with $65 Million in Series A. The company is focused on developing small-molecule drugs that stop the degradation of specific proteins to restore their levels for therapeutic benefit. The main value and basis of the biotech is the research of Daniel Nomura’s lab at UC Berkeley on so-called Deubiquitinase-targeting chimeras (or DUBTACs) for targeted protein stabilization.
Dear Colleagues, Customers, and Friends,
More than four months from the beginning of the full-scale Russian invasion and it is not clear when it will be over. The world is getting used to the Russian-Ukrainian war. At the same time, I suppose Ukraine should not exit from the focus of the whole world while Russia continues its aggression.
Image credit:Dilok Klaisataporn, iStock.
Proteins are essential components of living matter – they function as building blocks for cells and tissues, as well as participate in signaling and practically all biochemical activities. However, each protein operates correctly only for a limited amount of time and is eliminated by molecular machinery after it has reached its “functional shelflife”. To maintain a healthy and functional proteome, cells tightly control protein turnover processes, ensuring that misfolded, damaged, and old proteins exit the game in a timely manner. This sophisticated mechanism of degradation was recently hijacked by the drug discovery industry to develop new small molecule therapies — protein degraders.
Because of the war I’ve missed the news about the death of Sidney Altman on April 5, 2022. Altman is outstanding researcher, who first discovered the catalytical properties of RNA. He shared the Nobel prize in Chemisry with Thomas Cech in 1989. Their research results seem even more important nowadays when RNA-targeted drugs becomes reality.
Three months of the full-scale ruzzian invasion are over however it’s still really heartwarming for as at Enamine to get more and more words and signs of support from our customers and partners. The recent example is our joint letter to Science journal initiated by our friends from UCSF John J. Irwin and Brian K. Shoichet.
We are glad to inform you that we have fully restored the scope of our building block catalog as it was before the 24th of February war outbreak. The catalog lists over 238,000 off-the-shelf products. Such items are again offered in the various batch sizes reaching up to 100 grams in many cases to give you full scale of choice for your projects. Please visit https://enaminestore.com/catalog to make structure searches and order online.
Image credit: Orhan Turan, iStock by Getti Images.
Drug discovery is a long and challenging process, which may take up to fifteen years of experimentation and clinical trials, and several billion dollars in various expenses to bring a successful drug to patients. The process can be roughly divided into three stages: 1) biology research and early drug discovery; 2) preclinical drug development; and 3) clinical trials.
In order to start a drug discovery program, at the first stage, scientists study biological processes to come up with proper understanding of the underlying causes of a particular disease. Once drivers of the disease are known, scientists can select specific biological targets -- typically proteins involved in a disease-causing biological process.
I decided to write this post because I needed to share my feelings for the last 56 days. Of course, I did not experience as much as those who were in the hot areas or took the arms to defend Ukraine, but possibly my personal story might still be interesting to the readers (sorry for the long read with a little bit too much personal touch).
We, at Enamine, have united to resist at our level the Russian invasion. We help to acquire non-lethal military aid to enhance the defense of Ukraine, provide medical supplies to the hospitals, provide sponsorship for science and education in Ukraine, and help our employees scattered by war across Ukraine and abroad. Our own funds are limited as we have had to put on hold most of our projects and we will greatly appreciate your donations, which we will immediately use for the urgent needs of today! This is the most direct help to Ukraine.
Dear Customers, Dear Colleagues, Dear Friends,
The war in our country lasts more than 10 days. We have put on hold most of our operations in Kyiv and ask our customers to wait until this situation is resolved. We thank all of you for your patience. During this time, we have been able to estimate our resources, capabilities, and plan next steps to be done. Now I would like to highlight some of them: