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 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.
On February 24, Russian army attacked Ukraine at the full scale of its military potential, and started the bloodiest war in the European continent since WWII. As it is unfolding, more and more shocking crimes are committed by Russian forces against Ukrainian civilians. What happened in the cities of Irpen and Bucha shocked not only Ukrainians, but the whole civilized world.
The launch of Enamine Charity Fund was the practical answer by our team to the increasing crisis in Ukraine, and we are thankful to everyone who contributed money to help us provide help to our fellow Ukrainians, including our colleagues and friends in Irpen and Bucha.
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.
Since our return to the labs 1 month ago, we have managed to restore and catch up with practically all our synthesis and stock operations. We are extremely grateful for your being with us during these difficult times. We were happy to receive your messages of strong support and orders, demonstrating your continuous trust in Enamine. It means a lot to all of us, and it helped our quick rebirth.
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.
We are happy to inform you that we have successfully completed the relocation of our entire collection of screening compounds and started weighing compound samples since yesterday. All 3.5 million vials with dry compounds have been safely moved to our new facility in Sokal, a town near Lviv with a population of 20 000 people in the West of Ukraine, close to the Polish border.
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).
As of today, 17 countries among which France, Italy, and Austria to name a few, along with the European Union have sent their diplomats back to Kyiv, reopening their embassies, a vote of confidence that the Russia’s assault against the Ukrainian capital city and its region is over. This important symbolic and solidarity step from our allies makes clear that the necessary safety in Kyiv is returning, while the Russians have decided to re-focus on the East of Ukraine.
From our side, we are continuing working at full throttle to contribute to restoring our beloved homeland and its economy. Over 350 chemists including 100 FTE’s in our clients’ research projects have been able to resume their programs in our laboratories in Kyiv. We appreciate tremendously your indefatigable support, commitment, and trust in us!
The situation in Kyiv keeps improving day by day, shops and restaurants are re-opening and people are returning to their homes in a continuous stream. More and more chemists come back to their labs and resume their projects at Enamine. Currently, over 300 chemists are already back to work, and we estimate this number to grow up to 400-500 colleagues within the next couple of weeks. We have restored the synthesis of building blocks, REAL Compounds, as well as custom synthesis, including FTE research projects in our Kyiv’s facility. Along with our absolute capacity to resynthesize building blocks in larger amounts as before, the resumption of the supplies from Ukraine has allowed us to return 2.5-, 5-, and 10-gram amounts to our building block catalogue. Following our contingency plan at the war outbreak, we completely switched to supplies from our warehouses in US and Latvia, both largely limited to the 1-gram batch size. Now, we are resuming supplies of the larger amounts from our Kyiv stock and via resynthesis! Please check our offer at https://enaminestore.com/.
The quick supply of the building blocks is crucial. Even though the infrastructure in Ukraine has been significantly damaged during the war and despite express courier services have been suspended for the time being, our logistics specialists have organized a 3-day ground transportation route from Kyiv to our EU-based site in Latvia. This means that delivery time from Ukraine to your lab will be cut down to around 7-10 days very soon. Delivery time from US and EU local stores is as always 1-2 days.
Dear Colleagues, Customers, and Friends,
It has been 43 days.
Forty-three days with thousands of bombs, shells, and missiles fired out at our cities and villages, thousands of destroyed buildings, bridges, streets, thousands of killed people. And there are to be feared thousands of victims yet to come as the war continues with a new focus to the East of our country, the war for democracy to prevail against dictatorship and tyranny, the war of the civilized world against the paranoiac barbarians, the war of good against evil. Russia commits genocide against Ukrainians, terrorizes the population, and engages in looting. Nowadays after the crimes in Chernihiv and Kharkiv, after the massacre in Bucha, Irpin and Borodyanka, everybody understands: the world appears to be once again black and white these days and one can see clearly who stands on the side of Ukraine.
In the last 10 days there have been no missile strikes on Kyiv and normal life settles down in the capital. Last week we reported on resuming operations with our main building block warehouse in Ukraine and today we are pleased to inform you that we are going to start delivering your orders for screening compounds since the middle of April. In the meantime, we are completing transfer of the entire stock of screening compounds to our new facility in the west of Ukraine, near the Polish border.
Enamine’s screening collection has over 3 million small molecular weight compounds and is the largest and most reputable commercial collection in the world. We are happy to continue providing our compounds for drug discovery worldwide!
Another good news is that we have resumed synthesis of REAL Compounds, re-opening access to over 20 billion new compounds. Very soon we will be starting to deliver your important hit-finding and hit exploration libraries synthesized in our labs.
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:
Russian aggression continues with more force and they continue killing civilians (at least 200 killed only today officially, and who knows how many more). Enamine is forced to adjust schedules of operations, please, support our fight for our lives.
As I already wrote in my previous post, we at Enamine are constantly working on extending our REAL concept (where REAL is for REadily AccessibLe compounds). Basically, this concept allows for the generation of a virtual chemical space based on the experimentally validated synthetic accessibility. Until now the REAL Space has comprised 15.5 billion make-on-demand molecules and is currently the largest offer of commercially available compounds. It was shown that this chemical space is especially useful in combination with high-throughput virtual screening techniques (see Nature 2019, 566, 224–229 and Nature 2020, 580, 663–668); there is also a number of other ways to access it.
A diastereoselective approach to cis- and trans-1,3-disubstituted bicyclo[2.1.0]pentanes (housanes) was recently reported by our chemists in The Journal of Organic Chemistry. The article included preparation of 35 derivatives on up to 100 g scale. Moreover, pKa’s and conformational features of selected examples of housanes (e.g. GABA analogues) were also studied and compared to that of the corresponding 1,3-disubstituted cyclopentanes. For an extended list of novel housanes check the Enamine Store page.
Things like gene editing, stem cells, immunotherapies and new types of biologics are now mega-trends in the pharmaceutical industry, widely covered in media, and I guess there is little doubt that biology is the next big thing in medicine. However, in this post I would like to outline several promising areas in small molecule drug discovery, suggesting a lot of untapped potential and investment prospects in this more “traditional” pharmaceutical research space.
1.Targeting ribonucleic acid (RNA)
The majority of existing marketed drugs out there are designed to somehow modulate proteins in the body, thereby disrupting a disease progression. However, going one step back and trying to disrupt a pathological process earlier -- right before a protein is actually made in the body -- seems a powerful concept. This can be achieved by influencing ribonucleic acid (RNA), a central actor molecule in the process of gene expression -- the one leading to the formation of proteins as instructed by the human genome.