Covalent Modifiers

SEPTEMBER 18, 2024

Overall, our findings highlight the potential of developing isoform-selective and cell-active JNK3 inhibitors by covalent drug design strategy targeting a conserved cysteine. This work not only provides a valuable chemical probe for JNK3-targeted investigations in vitro and in vivo but also opens new avenues for the treatment of PD.

Small Molecule 211

Small Molecule Disease Treatment Drugs 211

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 350

Small Molecule Engineering Drugs 350

Covalent Modifiers

SEPTEMBER 9, 2023

3c05161 The stabilization of protein–protein interactions (PPIs) has emerged as a promising strategy in chemical biology and drug discovery. 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.

Small Molecule 200

Small Molecule Biophysical Assays Production Drugs 200

Covalent Modifiers

MAY 7, 2025

5c01712 Covalent small molecule drugs have emerged as a crucial support in precision therapy due to their high selectivity and robust potency. Covalent DNA-encoded chemical library (CoDEL) technology is an advanced platform for covalent drug discovery.

DNA 147

DNA Small Molecule Therapies Drugs 147

Covalent Modifiers

JUNE 12, 2025

The modular structure of STAT3 nominates several of its protein domains as possible drug targets, but their exploitation with potential small-molecule inhibitors has been unevenly distributed so far, with past efforts highly favoring the conserved SH2 domain.

Small Molecule 130

Small Molecule Clinical Trials DNA Trials 130

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

Covalent Modifiers

APRIL 20, 2025

Its role as a potential drug target for combating tuberculosis (TB) has just begun to be substantiated in drug discovery research. The knockdown also remarkably heightened the mutant's sensitivity to ethionamide and meropenem, but not to many other TB drugs.

Small Molecule 147

Small Molecule Drugs Research 147

Chemical Biology and Drug Design

FEBRUARY 6, 2025

Analysis of prevalence of ring, nonring, sp 3 -, and sp 2 -hybridized oxygen in approved drugs. For the first time, analysis of distribution of different types of oxygen from center of mass of a molecule. In approved drugs, majority of oxygen atoms are present within 4 from the COM of the molecule.

FDA Approval 100

FDA Approval FDA Small Molecule Pharmacokinetics 100

Covalent Modifiers

FEBRUARY 6, 2024

Fibroblast growth factor receptor (FGFR) kinase inhibitors have been shown to be effective in the treatment of intrahepatic cholangiocarcinoma and other advanced solid tumors harboring FGFR2 alterations, but the toxicity of these drugs frequently leads to dose reduction or interruption of treatment such that maximum efficacy cannot be achieved.

Small Molecule 223

Small Molecule Treatment Science Therapies 223

Drug Hunter

APRIL 20, 2023

We asked the global drug discovery community to nominate and vote on their favorite molecule from 2022, and the results are in. Here, we highlight what makes deucravacitinib so impressive to the drug discovery community. Here, we highlight what makes deucravacitinib so impressive to the drug discovery community.

Small Molecule 130

Small Molecule Clinical Trials Trials Licensing 130

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

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 286

RNA Small Molecule Therapies Drugs 286

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.

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Small Molecule Drugs 330

Covalent Modifiers

MAY 18, 2025

However, the molecular basis for specific inhibition of USP30 by small molecules has remained elusive. Collectively, our work establishes a generalizable chimeric protein-engineering strategy to aid deubiquitinase crystallization and enables structure-based drug design with relevance to neurodegeneration.

Engineering 147

Engineering Regulations Small Molecule Clinical Trials 147

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 121

Small Molecule Disease Drugs Science 121

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. It explores SARs, binding modes, and challenges in developing selective Clk4 inhibitors, offering insights for future therapeutic strategies.

Small Molecule 100

Small Molecule Disease Drugs 100

Chemical Biology and Drug Design

APRIL 4, 2025

At present, there are few studies on the drug resistance of mIDH1 inhibitors. It is found that a significant cause for drug resistance is that IDH1 has mutation at the second site. Isocitrate dehydrogenase (IDH) is a key metabolic enzyme that catalyzes the conversion of isocitrate to -ketoglutaric acid (-KG).

Small Molecule 100

Small Molecule Drugs DNA Treatment 100

Science Daily: Pharmacology News

NOVEMBER 13, 2023

A compound -- one of 27 million screened in a library of potential new drugs -- reversed four types of chronic pain in animal studies, according to new research.

Small Molecule 226

Small Molecule Drugs Regulations Research 226

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 Drugs 246

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

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

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 post ACS Fall 2023 First Disclosures appeared first on Drug Hunter. Stay tuned!

Small Molecule 238

Small Molecule Drugs 238

ASPET

OCTOBER 8, 2024

However, drug resistance and side effects, particularly those affecting hemostasis, continue to pose significant challenges for TKI therapies. imatinib and nilotinib), and second-generation ABL inhibitors including ponatinib and bosutinib designed to mitigate drug resistance. Our study included standard-of-care agents (e.g.,

Small Molecule 100

Small Molecule Therapies Drugs 100

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 171

Small Molecule Disease Drugs 171

Chemical Biology and Drug Design

MAY 10, 2025

Although it is currently only used in veterinary therapy, carprofen proves to be a molecule with a versatile therapeutic potential for human pharmacotherapy. Moreover, the molecule is a target in the drug discovery process for the development of new bioactive compounds.

Small Molecule 100

Small Molecule Drug Development Science Therapies 100

PPD

NOVEMBER 11, 2024

It is hard to ignore some of the most pressing, long-term trends driving the push to accelerate innovation and progress in drug development. As a result, biopharma and biotech companies working to bring their drug pipelines to the market require deep expertise from trusted partners to help deliver critical therapies for their patients.

Drug Development 97

Drug Development Clinical Trials Drugs Small Molecule 97

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

Drug Target Review

JUNE 6, 2025

As antibody-drug conjugates (ADCs) gain traction across oncology and begin to expand into other therapeutic areas, a persistent challenge remains: the design and optimisation of payloads. The ADC itself is not necessarily a large molecule – it’s a small molecule with aspects of a large molecule, and vice versa.

Small Molecule 52

Small Molecule Pharmacokinetics Packaging Drugs 52

Drug Target Review

DECEMBER 4, 2024

G protein-coupled receptors (GPCRs) represent a cornerstone of modern drug discovery due to their crucial role in regulating human physiology and their involvement in numerous diseases. In the early days, each GPCR target required its own structure-modulating ConfoBody to be identified before starting any drug discovery.

Small Molecule 122

Small Molecule Pharmacokinetics Therapies Immune Response 122

Drug Hunter

AUGUST 15, 2023

LRRK2 has been a hotly pursued drug target for Parkinson’s Disease based on human genetics. Drug Hunter Premium is drug discovery, distilled, so you can quickly catch up and make informed decisions based on industry examples. appeared first on Drug Hunter. Get ahead now by requesting a trial. already a member?

Small Molecule 229

Small Molecule Trials Treatment Disease 229

Covalent Modifiers

FEBRUARY 1, 2024

link] Proteins labelled site-specifically with small molecules are valuable assets for chemical biology and drug development. Nat Commun 15 , 859 (2024). The unique reactivity profile of the 1,2-aminothiol moiety of N -terminal cysteines ( N -Cys) of proteins renders it highly attractive for regioselective protein labelling.

Biophysical Assays 200

Biophysical Assays Small Molecule Drug Development Production 200

Drug Target Review

JUNE 16, 2025

G protein-coupled receptors (GPCRs) are a highly validated drug target family – accounting for 30-35 percent of all approved drugs. Despite this, the therapeutic potential of targeting most GPCRs remains untapped, as only 10 percent of GPCRs have been drugged.

Disease 59

Disease Therapies Small Molecule Immune Response 59

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

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

Drug Target Review

JULY 4, 2023

Over the last two decades, an increasing number of Antibody Drug Conjugate (ADC) therapeutics have been approved for oncology indications. These therapies have broadened treatment options for patients to expand beyond the more traditional small molecule drug alternatives. 3D rendering of Antibody Drug Conjugate Molecules.

Small Molecule 145

Small Molecule Drugs Clinical Pharmacology Trials 145

Covalent Modifiers

FEBRUARY 29, 2024

Currently, all FDA-approved covalent small molecules feature one electrophile, leaving open a facile route to acquired resistance. Therefore, molecular bidents represent a new pharmacological modality with the potential for improved selectivity, potency, and drug resistance profile.

Small Molecule 217

Small Molecule FDA Approval FDA Science 217

Covalent Modifiers

NOVEMBER 9, 2023

Baggelaar bioRxiv 2023.10.19.562725; doi: [link] Comparative, dose-dependent analysis of interactions between small molecule drugs and their targets, as well as off-targets, in complex proteomes is crucial for selecting optimal drug candidates.

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Small Molecule Drugs 147