Science Daily: Pharmacology News

FEBRUARY 22, 2024

A team of chemists has succeeded in synthesizing eight of the compounds for the first time using an approach that combines inventive chemical strategy with the latest technology in small molecule structure determination.

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Nvidia Developer: Drug Discovery

DECEMBER 3, 2024

Their specificity reduces the likelihood of off-target effects, making them safer and often more effective than small-molecule drugs for complex conditions. As a result… Source

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Covalent Modifiers

JANUARY 29, 2024

3c01835 Building on recent advances in peptide science, medicinal chemists have developed a hybrid class of bioconjugates, called peptide–drug conjugates, that demonstrate improved efficacy compared to peptides and small molecules independently. Moore Journal of Medicinal Chemistry 2024 DOI: 10.1021/acs.jmedchem.3c01835

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Small Molecule Drugs Science Disease 173

Covalent Modifiers

FEBRUARY 29, 2024

Gray ACS Central Science 2024 DOI: 10.1021/acscentsci.3c01245 Currently, all FDA-approved covalent small molecules feature one electrophile, leaving open a facile route to acquired resistance. Marto, Tinghu Zhang, Jianwei Che, and Nathanael S.

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Science Daily: Pharmacology News

MARCH 26, 2025

A small molecule shaped like a lasso may be a powerful tool in the fight against infectious diseases.

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DrugBaron

JULY 19, 2022

Despite the current hype around so called “advanced therapies”, which range from gene editing to cell therapies, and the inexorable advance of biologic therapeutics such as monoclonal antibodies, even in 2022 the majority of drugs in development and reaching patients are still small organic molecules.

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Small Molecule Drugs DNA Pharma Companies 100

Science Daily: Pharmacology News

NOVEMBER 13, 2023

The small molecule, which binds to an inner region of a calcium channel to indirectly regulate it, outperformed gabapentin without troublesome side effects, providing a promising candidate for treating pain.

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Small Molecule Regulations Drugs Research 222

Covalent Modifiers

JUNE 24, 2024

Rullo, Molecular Therapy: Oncology , 2024 , 200842, [link] Proximity-induction of cell-cell interactions via small molecules represents an emerging field in basic and translational sciences. The molecules, termed covalent immune recruiters (CIRs), were designed to affinity label and covalently engage SARs.

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Practical Cheminformatics

JANUARY 16, 2024

Following up on Part I and Part II, the third post in this series is a collection of review articles published in 2023 that I found helpful.

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Covalent Modifiers

SEPTEMBER 26, 2024

Changliu Wang, Zhenguang Zhao, Reem Ghadir, Dechun Yang, Zhenjia Zhang, Zhe Ding, Yuan Cao, Yuqing Li, Rosi Fassler, Dana Reichmann, Yujie Zhang, Yongli Zhao, Can Liu, Xiaobao Bi, Norman Metanis, and Junfeng Zhao ACS Central Science 2024 10 (9), 1742-1754 DOI: 10.1021/acscentsci.4c01148

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Covalent Modifiers

OCTOBER 25, 2024

We demonstrated the employability of ring-opening chemistry in isatoic anhydride as a drug delivery modality for the release of a small molecule and doxorubicin in cancer cells. Broadly, the tunable reactivity of isatoic anhydride could be leveraged for developing lysine-selective probes and drug delivery cargos.

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The Pharma Data

JULY 28, 2021

Novel small molecule drug candidates will target GPR75 to potentially address obesity and related co-morbidities. AstraZeneca has entered into a collaboration with Regeneron to research, develop and commercialise small molecule compounds directed against the GPR75 target with the potential to treat obesity and related co-morbidities.

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Covalent Modifiers

NOVEMBER 3, 2023

Rullo ACS Central Science 2023 DOI: 10.1021/acscentsci.3c01052 Strikingly, we observe chimeric molecules lacking an electrophile, which can only noncovalently bind the antibody, completely lack tumoricidal function. This is in stark contrast to previous work targeting small molecule hapten and peptide-specific antibodies.

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Small Molecule Science Drugs 173

The Pharma Data

NOVEMBER 17, 2020

Lead Pharma has entered into a collaboration and license agreement with Roche , hoping to lead the way in the development of oral small molecules for immune-mediated diseases like rheumatoid arthritis, psoriasis and inflammatory bowel diseases. .

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The ChEMBL-og

OCTOBER 23, 2024

This project builds upon the PDBeKnowledge Base (PDBe-KB) resource and combines structural, functional, and biochemical information for small molecules and their targets. By integrating CSD identifiers in UniChem, it is now easier to identify the availability of crystal structures that contain a specific molecule of interest.

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Broad Institute

OCTOBER 4, 2023

By Allessandra DiCorato October 4, 2023 Credit: AbbVie The new small molecule inhibitor (green) sits inside the PTPN2 protein, where acidic sites are marked in red and basic sites are marked in blue. A new small-molecule drug candidate being tested in an early-stage clinical trial aims to improve patient responses to immunotherapy.

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The Pharma Data

JULY 29, 2021

Loxo Oncology at Lilly, a research and development group of Eli Lilly and Company (NYSE: LLY), and Kumquat Biosciences today announced an exclusive collaboration focused on the discovery, development and commercialization of potential novel small molecules that stimulate tumor-specific immune responses.

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Broad Institute

MARCH 14, 2024

In one approach, they mark targeted proteins with “destroy me” tags that work with small molecules known as molecular glues to prompt the cell’s own protein-clearing machinery to gobble up the proteins. The new study appears in Science. Paper cited Mercer JAM, et al. March 14, 2024.

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Targeted Protein Degradation Small Molecule Medical Schools Science 141

Codon

FEBRUARY 13, 2025

A new paper , published today in Science , suggests a way forward. By training PLACER on structures stored in the Protein Data Bank, the team taught the model to predict atom arrangements that follow the physical and chemical rules governing protein-small molecule interactions.

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Drug Target Review

JUNE 15, 2023

In this article Drug Target Review’s Izzy Wood spoke to Sam Hasson, Director of Target Biology at Rgenta Therapeutics, a biotech firm in Massachusetts, US, that aims to develop small molecule therapeutics to target RNA processing. It is somewhat like how PROTACs have changed the perspective on what is a tractable therapeutic target.

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Drug Target Review

JULY 6, 2023

1 TPD is expected to challenge undruggable proteins, which are highly difficult to target by conventional small molecules. 1 The concept of TPD was first demonstrated with a heterobifunctional small molecule to degrader a protein of interest in the early 2000s.

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Drug Target Review

JULY 23, 2024

I studied Natural Sciences at the University of Cambridge, where I was exposed to a range of disciplines from chemistry to physiology, specialising in my last year in biochemistry. Pushing the boundaries of science always opens the door to new, impactful developments, although there are always challenges along the way.

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The Pharma Data

NOVEMBER 15, 2020

R&D collaboration building on Lead Pharma’s expertise in the discovery, design and optimization of small molecule treatments. Lead Pharma is headquartered at Pivot Park, the biopharmaceutical life sciences campus in Oss, the Netherlands. OSS, Netherlands , Nov. OSS, Netherlands , Nov.

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LifeSciVC

APRIL 2, 2024

The quality of science – and the ability to distinguish it from other approaches – was the entry ticket to serious engagement. The science presents an opportunity and a challenge for us at Sionna. We experienced strong enthusiasm for small molecule research in the investor community. That science resonates with investors.

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Drug Target Review

NOVEMBER 25, 2024

As the CEO of iOnctura, an innovative oncology biopharmaceutical company she co-founded in 2017, Catherine has played a key role in advancing the development of highly targeted small molecules aimed at revolutionising cancer treatment. I went on to complete my MBA and PhD at The Institute of Cancer Research (ICR) in drug development.

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Drug Target Review

JULY 13, 2023

They found that although the targets themselves may not be easily druggable due to their disordered nature, their ability to condense can be modulated using small molecules. By focusing on molecules that modulate the condensate formation, they identified tractable chemical matter that specifically impacted the target of interest.

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Disease Small Molecule Cell Biology Drugs 98

DrugBank

MAY 15, 2024

This method was more about serendipity than science. Today, we're able to identify and target specific molecules involved in disease processes—a method that's much more like using a sniper rifle than throwing darts blindfolded. One approach is to look beyond the traditional drug molecule.

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The Pharma Data

NOVEMBER 19, 2020

The Company is also aiming to leverage the highly conserved structure of the SARS-CoV-2 M pro protease as a basis for the design of novel oral small molecules against predicted future variants of SARS-CoV-2 and other related human viruses. Zhang, et al, Science (2020) DOI: 10.1126/science.abb3405. References. Hilgenfeld, Febs J.

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The Pharma Data

NOVEMBER 15, 2020

In a deal set to be finalized early in 2021, Urovant Sciences has agreed to be fully acquired by largest investor and close partner, Sumitovant Biopharma. Sumitovant is a global biopharmaceutical company with a pipeline similarly focused on uterine fibroids, advanced prostate cancer and endometriosis. .

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DrugBaron

JANUARY 31, 2024

After decades slowly developing in the shadows, featuring more often in science fiction novels than television news programs, the arrival of large language models, and ChatGPT in particular, thrust artificial intelligence into the national consciousness. The subservience of “the science” to other factors in the decision-making process.

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Drug Target Review

NOVEMBER 1, 2023

The mission of the CCDD is to discover novel small-molecule therapeutics for the treatment of cancer and progress them to hypothesis testing phase 1 clinical trials. We have several exciting projects in various stages of discovery, but a small-molecule drug that is causing a lot of excitement at the moment is Capivasertib.

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Drug Target Review

OCTOBER 4, 2023

Groundbreaking strategies like proteolysis-targeting chimeric molecules (PROTACs) are also being explored. 6 Combining the effect of payloads with different mechanisms of action – an approach that revolutionised small molecule chemotherapy – also holds the promise of enhanced therapeutic activity for ADCs. Chang, P. &

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NIH Director's Blog: Drug Development

OCTOBER 30, 2018

Now comes word of another absolutely incredible use of cryo-EM: determining with great ease and exquisite precision the structure of the smaller organic chemical compounds, or “small molecules,” that play such key roles in biological exploration and drug development. Also analyzed were eight less-familiar small molecules.

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LifeSciVC

JANUARY 16, 2024

Small molecule GLP1s? Small molecules are still in vogue despite IRA headwinds: We continue to hear optimism for the convenience of orals even in indications with high-commercial potential and enriched for CMS coverage (likely to fall in crosshairs of IRA).

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Drug Target Review

SEPTEMBER 25, 2024

Applying our technology has enabled us to develop a new small molecule, TT125-802, and to assign a new role to the epigenetic regulator CBP/p300 as a novel master regulator of non-oncogene resistance. This orally available small molecule binds to the bromodomain of CBP/p300 in a highly specific manner.

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Drug Target Review

NOVEMBER 6, 2023

These regimens frequently include one or two small molecule inhibitors and immuno-oncology (IO) therapies, such as monoclonal antibodies and T-cell engagers. To bring us closer to curing cancer, a combination of effective drugs with non-overlapping mechanisms of action is required. References Blood Cancer UK.

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Drug Target Review

OCTOBER 23, 2024

Technologies for the rapid and efficient testing of small molecules and biologics have greatly accelerated drug discovery. Intermediate-sized molecules such as macrocycles combining the beneficial properties of both small molecules and biologics may enable the targeting of currently undruggable targets.

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