Covalent Modifiers

SEPTEMBER 9, 2023

Here, we show the structure-based optimization of the nonselective fragment toward selective and highly potent small-molecule stabilizers of the 14-3-3σ/ERα complex. We have previously identified a disulfide fragment that stabilized the hub protein 14-3-3σ bound to several of its clients, including ERα and C-RAF.

Small Molecule 200

Small Molecule Biophysical Assays Production Drugs 200

Covalent Modifiers

FEBRUARY 15, 2024

Herein, we use afatinib as a lead to undertake a structure-based drug design approach, aided by mass-spectrometry and x-ray crystallography, to develop DHC-156, a small molecule that more selectively binds brachyury and downmodulates it as potently as afatinib.

Small Molecule 162

Small Molecule FDA Approval FDA Therapies 162

Chemical Biology and Drug Design

JANUARY 20, 2025

ABSTRACT Drug targeting strategies, such as peptidedrug conjugates (PDCs), have arisen to combat the issue of off-target toxicity that is commonly associated with chemotherapeutic small molecule drugs.

Small Molecule 187

Small Molecule Drugs International Therapies 187

Covalent Modifiers

APRIL 20, 2025

Our findings indicate that small-molecule inhibitors targeting ClpP1P2, when used alongside existing TB medications, could represent novel therapeutic strategies. Subsequent evaluation confirmed the synergistic activity of GDI-5755 when combined with the TB drugs to inhibit mycobacterial growth.

Small Molecule 147

Small Molecule Drugs Research 147

Drug Hunter

APRIL 20, 2023

Through a series of structure-based design, ADME and solubility optimization, LP0200 was shown to exhibit high potency and safety comparable to approved IL-17A and IL-17RA targeting mAbs (more in our report of first disclosures from the EFMC-ISMC and this article on small molecule immunomodulators ). LP0200 has completed a Ph.

Small Molecule 130

Small Molecule Clinical Trials Trials Licensing 130

Collaborative Drug

SEPTEMBER 23, 2024

Upcoming Webinar 9-26-24: Generative Chemistry, Deep Learning and Traditional Models - Practical Insights and Emerging Technologies

Small Molecule 277

Small Molecule 277

Covalent Modifiers

NOVEMBER 26, 2023

While small molecule inhibitors for the G12C mutant have been successfully developed, allele-specific inhibition for other KRAS hotspot mutants remains challenging. Shokat Journal of the American Chemical Society 2022 144 (35), 15916-15921 DOI: 10.1021/jacs.2c05377

Small Molecule 130

Small Molecule Therapies Production 130

Science Daily: Pharmacology News

APRIL 10, 2024

In a new breakthrough that could revolutionise medical and material engineering, scientists have developed a first-of-its-kind molecular device that controls the release of multiple small molecules using force.

Small Molecule 347

Small Molecule Engineering Drugs 347

Covalent Modifiers

FEBRUARY 6, 2024

Schönherr, H.; Taylor, A. Casaletto, J. Moustakas, D. Hudson, B. Valverde, R.; O’Hearn, P. Sharon, D. Garfinkle, S.; Giordanetto, F.; Lescarbeau, A.; Kurukulasuriya, R.; Gerami-Moayed, N.; Bruderek, K.; Gunaydin, H.; Boezio, A. McLean, T. Shaw, D.

Small Molecule 223

Small Molecule Treatment Science Therapies 223

BioPharma Drive: Drug Pricing

JANUARY 6, 2025

The startup is developing a kind of macrocyles, which share strengths of both small molecules and biologics, as oral medicines against “validated blockbuster biologic targets.”

Small Molecule 301

Small Molecule 301

Science Daily: Pharmacology News

NOVEMBER 30, 2023

Researchers have succeeded in restoring lost brain function in mouse models of stroke using small molecules that in the future could potentially be developed into a stroke recovery therapy.

Small Molecule 325

Small Molecule Therapies Research 325

BioPharma Drive: Drug Pricing

AUGUST 28, 2024

Under a collaboration with NextRNA Therapeutics, Bayer will access the biotech’s platform to target long, non-coding RNA interactions with small molecule drugs.

RNA 293

RNA Small Molecule Therapies Drugs 293

Chemical Biology and Drug Design

MARCH 17, 2025

This review highlights recent advancements in small molecule inhibitors targeting Cdc2-like kinase 4 (Clk4), emphasizing their potential in treating cancers and neurodegenerative diseases. This review highlights recent advancements in Clk4 inhibitors, covering both natural, and synthetic compounds.

Small Molecule 100

Small Molecule Disease Drugs 100

Forbes: Drug Truths

MARCH 6, 2024

There is another aspect of this provision of the IRA that is starting to be felt – "the small molecule penalty"

Small Molecule 296

Small Molecule Drugs 296

Science Daily: Pharmacology News

APRIL 8, 2025

Experimental drug NU-9 -- a small molecule compound approved by the U.S. Food and Drug Administration (FDA) for clinical trials for the treatment of amyotrophic lateral sclerosis (ALS) -- improves neuron health in animal models of Alzheimer's disease, according to a new study.

Small Molecule 241

Small Molecule Disease Clinical Trials Drugs 241

Science Daily: Pharmacology News

APRIL 5, 2024

The active ingredient in many drugs is what's known as a small molecule: bigger than water, much smaller than an antibody and mainly made of carbon. It's tough, however, to make these molecules if they require a quaternary carbon -- a carbon atom bonded to four other carbon atoms.

Small Molecule 294

Small Molecule Drugs 294

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.

Small Molecule 311

Small Molecule Laboratories 311

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

Small Molecule 113

Small Molecule Disease Drugs Science 113

ASPET

OCTOBER 8, 2024

Significance Statement This study examines the effects of clinically relevant small molecule BCR-ABL tyrosine kinase inhibitors (TKIs) on platelet activity. Overall, these new insights around the effects of ABL TKIs on platelet function could inform the development of targeted therapies with reduced hematologic toxicities.

Small Molecule 100

Small Molecule Therapies Drugs 100

Collaborative Drug

AUGUST 29, 2023

a new Italian incubator dedicated to the discovery and development of small molecule-based treatments for neurodegenerative diseases, announced today that it has adopted Collaborative Drug Discovery’s CDD Vault as its platform of choice for managing drug discovery data.

Small Molecule 246

Small Molecule Treatment Disease Research 246

Covalent Modifiers

AUGUST 14, 2024

Rullo Molecular Therapy 2024 DOI: [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.

Small Molecule 182

Small Molecule Engineering Science Therapies 182

Covalent Modifiers

JUNE 6, 2023

Cravatt, B.; Hayward, R.; DeMeester, K.; Ogasawara, D.; Schreiber, S.; Melillo, B. ChemRxiv 2023 [link] Covalent chemistry is a versatile approach for expanding the ligandability of the human proteome.

Small Molecule 130

Small Molecule 130

Drug Hunter

AUGUST 18, 2023

The First Disclosures sessions at the 2023 ACS Fall Meeting in San Francisco, organized by Nikki Goodwin , presented a variety of new orally available small molecules. The standing room-only sessions were so highly attended that many attendees were unfortunately kicked out due to the fire code.

Small Molecule 238

Small Molecule Drugs 238

Chemical Biology and Drug Design

FEBRUARY 6, 2025

The study examines the frequency, distribution, prevalence, and diversity of oxygen atoms in a dataset of 2049 small molecules approved by the FDA and other agencies. This work presents a comprehensive analysis of oxygen atoms in approved drugs, aiming to streamline drug design and discovery efforts.

FDA Approval 100

FDA Approval FDA Small Molecule Pharmacokinetics 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

Chemical Biology and Drug Design

APRIL 4, 2025

Currently, the FDA has granted approval for the use of the small molecule inhibitor Ivosidenib (AG-120) in the treatment of IDH1-mutated AML and cholangiocarcinoma. Although AG-120 has benefited patients clinically, drug resistance has gradually emerged and has become a major problem in the treatment of mutant IDH1 (mIDH1) diseases.

Small Molecule 100

Small Molecule Drugs DNA Treatment 100

Covalent Modifiers

OCTOBER 3, 2023

3c06622 Targeted protein degradation relies on small molecules that induce new protein–protein interactions between targets and the cellular protein degradation machinery. Most of these small molecules feature specific ligands for ubiquitin ligases.

Targeted Protein Degradation 182

Targeted Protein Degradation Small Molecule Drugs 182

Covalent Modifiers

OCTOBER 10, 2023

Ebert, Nathanael Gray bioRxiv 2023 [link] Small molecules that can induce protein degradation by inducing proximity between a desired target and an E3 ligase have the potential to greatly expand the number of proteins that can be manipulated pharmacologically. Rutter, Cyrus Y. Jin, Michelle Y. Wang, Shawn Xu, Anna M.

Targeted Protein Degradation 208

Targeted Protein Degradation Small Molecule 208

Covalent Modifiers

MARCH 1, 2024

The range of small molecules explored by chemical proteomics has, however, been limited. Our findings show the utility of photo-stereoprobes for expanding the ligandable proteome, furnishing target engagement assays, and discovering and characterizing bioactive small molecules by cell-based screening.

Small Molecule 195

Small Molecule 195

Chemical Biology and Drug Design

JANUARY 29, 2024

Knowledge of the molecular interactions acquired from such structures would greatly aid the discovery of small molecule inhibitors of sPLA 2 s for the treatment of snakebite envenoming. In addition, the complex of the sPLA 2 inhibitor, varespladib, with a Lys49-PLA 2 -like snake venom toxin is also discussed.

Small Molecule 100

Small Molecule Immune Response Treatment Disease 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.

Small Molecule 222

Small Molecule Regulations Drugs Research 222

Covalent Modifiers

SEPTEMBER 9, 2023

3c00297 Falling in between traditional small molecules and antibodies in size, peptides are emerging as a privileged therapeutic modality, one that can harness the benefits of both small molecule and antibody drugs. Mengmeng Zheng and Jianmin Gao ACS Chemical Biology 2023 DOI: 10.1021/acschembio.3c00297

Small Molecule 195

Small Molecule International Drugs 195

Covalent Modifiers

FEBRUARY 1, 2024

link] Proteins labelled site-specifically with small molecules are valuable assets for chemical biology and drug development. By using this approach in tandem with BHoPAL, we generate dually labelled protein bioconjugates appended with different labels at two distinct specific sites on a single protein molecule.

Biophysical Assays 200

Biophysical Assays Small Molecule Drug Development Production 200

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

Small Molecule 173

Small Molecule Drugs Science Disease 173

Chemical Biology and Drug Design

SEPTEMBER 28, 2023

The assay design is to discover bioactive small molecules that restore proliferation in T. brucei We hypothesized that chemically disrupting the SLiM-binding pocket would restore proliferation in T. brucei brucei , overproducing PCNA orthologs. Testing this hypothesis is the proof-of-concept for a T. brucei-

Small Molecule 100

Small Molecule DNA Regulations Research 100

Covalent Modifiers

MARCH 22, 2024

This capability becomes particularly valuable in addressing challenges such as the low affinity frequently encountered between therapeutic proteins and their targets, as well as the limited availability of small molecules for specific protein targets.

Small Molecule 237

Small Molecule Engineering Treatment Drugs 237

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.

Small Molecule 165

Small Molecule Disease Drugs 165