Chemical Biology and Drug Design

SEPTEMBER 28, 2023

Abstract Proliferating cell nuclear antigen (PCNA) is a homo-trimeric protein complex that clamps around DNA to tether DNA polymerases to the template during replication and serves as a hub for many other interacting proteins. The assay design is to discover bioactive small molecules that restore proliferation in T. brucei

Small Molecule 100

Small Molecule DNA Regulations Research 100

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.

Small Molecule 100

Small Molecule Drugs DNA Pharma Companies 100

Covalent Modifiers

MAY 25, 2024

Complementary to genetic approaches, small-molecule probes have emerged as useful tools for modulating caspase activity. However, due to the high sequence and structure homology of all 12 human caspases, achieving selectivity remains a central challenge for caspase-directed small-molecule inhibitor development efforts.

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Small Molecule DNA Virus Regulations 162

Covalent Modifiers

DECEMBER 11, 2023

Covalent ligands are a promising strategy to pharmacologically target nuclear proteins, such as transcription factors, which lack ordered small-molecule binding pockets. To identify nuclear cysteines that are susceptible to covalent liganding, we couple proximity labeling (PL), using a histone H3.3-TurboID

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Small Molecule DNA Regulations Disease 162

Covalent Modifiers

MAY 29, 2023

We further show that members of our nucleophilic fragment library can impair functional protein–protein interactions involved in nuclear oncoprotein transport and DNA damage repair.

Small Molecule 130

Small Molecule DNA 130

Codon

FEBRUARY 13, 2025

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. They synthesized DNA encoding each protein variant, expressed the proteins in E.

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Small Molecule Engineering Production DNA 139

Dark Matter Blog

APRIL 4, 2023

The bulk of my nearly three decades of experience up to that point was with drugging protein targets using a variety of modalities, but principally small molecules. And unproductive interactions between the RNA target and the DNA barcodes complicated DEL screening. Screening to Set a Course Screening brings its own challenges.

Small Molecule 52

Small Molecule RNA Fragment Screening DNA 52

Covalent Modifiers

AUGUST 14, 2023

For both cancer and healthy genomes, we find that cysteine acquisition is a ubiquitous consequence of genetic variation that is further elevated in the context of decreased DNA repair.

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Small Molecule RNA DNA Therapies 130

DrugBank

MAY 22, 2024

Molecular dynamics (MD) simulations and other computational methods are vital tools in our arsenal , helping us peek into the atomic-level interactions and movements within the protein, helping reveal potential new binding sites induced by small molecule interactions. DNA and RNA are also key players, each bringing unique challenges.

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Small Molecule RNA DNA Pharmaceutical Companies 96

DrugBank

JULY 24, 2024

These multifunctional small molecules are like tiny spies, hijacking the body’s natural protein degradation system to remove unwanted proteins. Multifunctional Small Molecules and Peptides Beyond PROTACs, there are other exciting tools in the new drug discovery toolbox.

Small Molecule 98

Small Molecule Drugs Clinical Trials Therapies 98

Drug Hunter

MAY 18, 2023

researching DNA photoproducts related to skin cancer. As the ADC team moved toward a greater emphasis on development, Dian felt the pull to return to her “research mindset” and switched paths again, this time delving into DMPK, particularly small molecules and peptides. “I Proteomics!

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Small Molecule DNA Pharmacokinetics Engineering 131

DrugBank

MAY 15, 2024

One approach is to look beyond the traditional drug molecule. Researchers are experimenting with biologics—larger biological molecules that can do things small molecules can't, like targeting larger, more complex structures on cell surfaces or even inside cells.

Small Molecule 98

Small Molecule Molecular Biology Drugs Disease 98

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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Small Molecule DNA Drugs Pharmaceuticals 65

NIH Director's Blog: Drug Discovery

MARCH 8, 2016

Instead of the black, printed stripes of the Universal Product Codes (UPCs) that we see on everything from package deliveries to clothing tags, they used short, unique snippets of DNA to label cells. DNA barcoding has already empowered single-cell analysis, including for nerve cells in the brain. PRISM consists of two key components.

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DNA Drugs Small Molecule FDA Approval 52

DrugBaron

FEBRUARY 7, 2022

Finding small molecule drugs is much harder than finding a needle in a haystack – discovering the right arrangement of atoms to bind precisely to a protein target to elicit a particular response is a problem of vast dimensionality. Yet the situation with small molecules is even worse.

Small Molecule 100

Small Molecule Synthetic Chemistry Pharma Companies Pharmacokinetics 100

Codon

JUNE 11, 2024

And unlike traditional DNA sequencers, which parse genetic material by breaking it up into fragments and interpreting it chunk-by-chunk, a nanopore device unspools a long strand of DNA and reads it all at once. A scientist can isolate DNA and load up a flow cell in fifteen minutes. Nanopore devices work incredibly fast.

DNA 99

DNA Engineering RNA Small Molecule 99

Drug Target Review

JULY 31, 2023

For my PhD project, I chose an advisor who worked on DNA and I started working with her on the physical properties of DNA. I worked with Jackie Barton in the early days of what’s now called DNA-mediated electron transfer. And that was a very controversial idea. And my answer to that has changed over the years.

DNA 98

DNA Science Small Molecule Cell Biology 98

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.

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Small Molecule Therapies Treatment Disease 111

The Pharma Data

JANUARY 5, 2021

Durham, North Carolina-based Ribometrix announced a strategic collaboration deal with Genentech , a Roche company, to identify and advance novel RNA-targeted small molecule therapeutics. This is because many proteins do not have small-molecule binding sites. This is not the first deal for RNA therapeutics for Genentech.

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RNA Small Molecule DNA Licensing 52

DrugBank

OCTOBER 17, 2024

By utilizing high-resolution protein structures obtained through X-ray crystallography, researchers could design small molecules that potently inhibit the SARS-CoV-2 main protease, a key enzyme essential for viral replication.

Drug Development 98

Drug Development Metabolic Stability Clinical Trials Drugs 98

KIF1A

JANUARY 27, 2024

Drugs that treat symptoms in other HSP types could inform treatments for similar symptoms in KAND, so we’re always on the lookout for small molecule or technological interventions that work in other SPGs. Simran Kaur’s 2023 conference talk briefly describes the KIF1A mini-gene approach.

Therapies 111

Therapies Small Molecule Treatment DNA 111

Sygnature Discovery

JUNE 17, 2024

Our in-house SPR equipment comprises: 2x Biacore TM 8K+ 3x Biacore TM 8K 1x Biacore TM T200 This covers mM binders, such as fragments, through to sub pM interactions (such as late stage small molecules or very high affinity biological interactions, Tollenaere et al 2023 [link] ). This technology measures affinities from mM to nM.

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Small Molecule Fragment Screening DNA Science 52

Drug Target Review

JUNE 19, 2024

The other powerful benefit is that our cell lines can become any of the cell types of the human body – these cells have within their DNA the capability to become any of the more than 200 human cell types which you might want to manufacture. Just like small molecules and antibodies, cell therapies are changing how we treat patients.

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Therapies Small Molecule Pharmaceutical Companies Molecular Biology 84

Dark Matter Blog

AUGUST 31, 2020

The majority of small molecule drugs induce their therapeutic effects by seeking out and binding to their intended target while avoiding most other molecules in the dense milieu of the cell interior. Our overall mission at Arrakis is to expand the set of “druggable” targets for small-molecule medicines to include RNA.

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RNA Small Molecule Bioinformatics Computational Chemistry 52

Drug Target Review

DECEMBER 7, 2023

In an infected animal, cGAS senses viral DNA in cytoplasm whilst in an uninfected organism, DNA is confined in the nucleus. Bacteria must take a different approach as they do not have nuclei and if CBASS reacted to the presence of DNA, it would cause autoimmunity or the bacterium to attack itself, Banh said. But what, exactly?”

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RNA Immune Response DNA Molecular Biology 59

LifeSciVC

AUGUST 5, 2024

The genomic capabilities that were brought online for drug discovery (cheaper & faster next-gen DNA sequencing) did not diminish the need for biologists and translational scientists in target and patient selection, respectively. One final parallel to 2001.

Molecular Biology 97

Molecular Biology Production Drug Development Small Molecule 97

Nvidia Developer: Drug Discovery

MARCH 21, 2023

New supercomputing-scale large language models (LLMs) that understand biology and chemistry text are helping scientists understand proteins, small molecules, DNA, and biomedical text. These state-of-the-art AI models help generate de novo proteins and molecules and predict the 3D structures of proteins.

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Small Molecule Drugs Clinical Trials DNA 52

Dark Matter Blog

JULY 16, 2021

As soon as I learned about DNA and RNA, I wanted to be a molecular biologist. Last stops at RNA My last roles in biotech were where my original passion began: DNA and RNA. My last stop at Arrakis Therapeutics is with a company targeting RNA with small molecules. I wanted to use molecular biology to create drugs.

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Small Molecule RNA Clinical Trials DNA 52

The Premier Consulting Blog

JULY 9, 2023

During the development of new small molecule drug products, developers must conduct impurity and degradant evaluation at several points in the program and to varying degrees. In addition, this guidance focuses on DNA reactive substances that could potentially cause cancer. Global regulatory agencies, including the U.S.

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Small Molecule DNA Drugs Clinical Development 52

Metabolite Tales Blog

OCTOBER 5, 2023

Trapping agents are described for reactive metabolites that could ordinarily be overlooked due to quenching with endogenous small molecules and protein nucleophiles.

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Small Molecule DNA Drug Development Drugs 52

LifeSciVC

DECEMBER 6, 2022

These hair clip-like molecules clamp onto DNA, thereby turning many genes on and off. As Darnell observed, the prospect of being able to regulate Transcription Factor function holds the potential to reframe the way we treat disease but achieving that goal with traditional small molecule screening approaches is impossible.

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Small Molecule DNA Regulations Science 40

The Pharma Data

JUNE 28, 2021

Broadens company’s oncology platform of Targeted Alpha Therapies / Acquisition includes actinium-225 labeled differentiated PSMA small molecule for the treatment of prostate cancer. It has been demonstrated to inflict difficult to repair damage to tumor cells by inducing DNA double strand breaks.

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Small Molecule Licensing Licensing Therapies 52

The Pharma Data

MAY 15, 2023

Through the acquisition, Gilead gains rights to a portfolio of small molecule inhibitors targeting PARP1 for oncology and MK2 for inflammatory diseases that could enter clinical trials later this year. Executive Vice President, Research, Gilead Sciences. The company was founded in 2021 by Stephen Kaldor, Ph.D., Qing Dong, Ph.D.,

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Small Molecule DNA Immune Response Science 40

Drug Target Review

JULY 18, 2023

I think it is astonishing that The Human Genome Project was completed exactly 20 years ago and DNA was discovered by Franklin and published by Watson and Crick exactly 70 years ago, yet that 10 percent success rate has still not improved. This means that we are not doing something right.

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Drug Development Drugs Clinical Development Pharmaceutical Companies 98

The Pharma Data

NOVEMBER 18, 2020

The company’s novel first-in-class AKR1C3 targeted therapy is OBI-3424 (small-molecule prodrug) that selectively releases a potent DNA alkylating agent in the presence of the aldo-keto reductase 1C3 (AKR1C3) enzyme. Additional information can be found at www.obipharma.com. Forward-Looking Statements.

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Vaccine Small Molecule Immune Response Hospitals 52

LifeSciVC

MARCH 1, 2023

Augustin et al summarized how novel platforms have more recently been applied to try to solve this question including CRISPR genome editing combined with adoptive cell therapy, siRNA knockdown, DNA encoded library approaches and machine learning algorithms.

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Small Molecule Immune Response DNA Therapies 52

Molecule Blog

AUGUST 13, 2021

This program focuses on testing and developing three of these small molecules as possible interventions in ageing. These molecules target the longevity field with the aim of letting everyone live healthier, happier and longer lives. He now runs one of the largest research programmes in Europe focusing on aging.

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FDA Approval DNA Small Molecule FDA 52