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

BioPharma Drive: Drug Pricing

JUNE 21, 2023

Empress Therapeutics claims its technology allows it to identify chemical drug candidates faster and more reliably. It has $50 million from Flagship to prove it can.

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Small Molecule Drugs 119

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-

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Small Molecule DNA Regulations Research 100

Drug Hunter

AUGUST 15, 2023

Clinical advancement of LRRK2 inhibitors was initially stalled by concerns about on-target lung findings in primates, but these were ameliorated by a Merck/Genentech/Pfizer/MJFF study showing that these lung changes were reversible, and Biogen/Denali has currently a small molecule (BIIB122/DNL151) in Ph. I ( NCT04557800 ).

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Small Molecule Trials Treatment Disease 229

Metabolite Tales Blog

APRIL 10, 2024

Table 1: Small molecule drugs approved by the FDA in 2023 with reported involvement of phase II mechanisms In vitro : In vivo differences Incubation of the SGLT2 (sodium-glucose co-transporter-2) inhibitor bexagliflozin in human liver microsomes points to metabolism through both oxidation and glucuronidation to 6 main metabolites.

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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.

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Small Molecule FDA Approval FDA Therapies 64

Covalent Modifiers

SEPTEMBER 18, 2024

Liang Ouyang, Wen Shuai, Panpan Yang, Huan Xiao, Yumeng Zhu, Faqian Bu, Aoxue Wang, Qiu Sun, Guan Wang Angewandte Chemie 2024 e202411037 [link] c-Jun N-terminal kinases (JNKs) including JNK1/2/3 are key members of mitogen-activated protein kinase family.

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Small Molecule Disease Treatment Drugs 84

Covalent Modifiers

OCTOBER 15, 2024

Our findings reveal a striking plasticity underpinning the pioneering function of FOXA1 that can be controlled by small molecules. Motif analysis supports a mechanism where the ligands relax the canonical DNA-binding preference of FOXA1 by strengthening interactions with suboptimal sequences in predicted proximity to C258.

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ASPET

JULY 13, 2023

Dynasore and dyngo-4a, small molecules developed to inhibit the GTPase activity of classic dynamins DNM1, DNM2 and DNM3, but not mdivi-1, a specific inhibitor of DNM1L, protect corneal epithelial cells exposed to the oxidant tert-butyl hydroperoxide (tBHP).

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Small Molecule Treatment 100

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.

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Small Molecule Biophysical Assays Production Drugs 80

Metabolite Tales Blog

JANUARY 23, 2024

Metabolism of 2023 FDA Approved Small Molecules – PART 1 By Julia Shanu-Wilson 2023 was a fruitful year for drug approvals by the FDA, with a crop of 34 small molecules out of a total of 55 new drugs [1]. References [1] 2023 Novel Small Molecule FDA Drug Approvals.

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Drug Hunter

JUNE 29, 2023

The talk covered: Theoretical advantages of targeted protein degradation over traditional small molecules Recent highlights throughout the industry illustrating these advantages Areas to watch in targeted protein degradation on the horizon Some of the highlights mentioned in the talk include: IV STAT3 degraders from Kymera Therapeutics (e.g.

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Targeted Protein Degradation Small Molecule Drugs 221

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.

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Small Molecule Engineering Drugs 140

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.

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Small Molecule Treatment Science Therapies 89

Drug Hunter

MAY 31, 2023

This article compiles 20+ recent small molecules of general interest in the news in April 2023, with structures where they are available.

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Small Molecule Clinical Trials Trials Drugs 196

Practical Cheminformatics

JANUARY 16, 2024

Property Prediction Machine Learning Methods for Small Data Challenges in Molecular Science [link] Practical guidelines for the use of gradient boosting for molecular property prediction [link] Application of message passing neural networks for molecular property prediction [link] Molecular Similarity Molecular Similarity: Theory, Applications, and (..)

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Targeted Protein Degradation Small Molecule Computational Chemistry Bioinformatics 140

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

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Small Molecule Therapies Production 52

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 132

Drug Target Review

JULY 4, 2023

These therapies have broadened treatment options for patients to expand beyond the more traditional small molecule drug alternatives. 2 However, when dosed at the MTD, ADCs display improved efficacy over small molecules in oncology trials. 3D rendering of Antibody Drug Conjugate Molecules.

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Small Molecule Drugs Clinical Pharmacology Trials 145

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.

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RNA Small Molecule Therapies Drugs 119

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.

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Chemical Biology and Drug Design

NOVEMBER 20, 2023

We employed a combined strategy involving molecular docking-based virtual screening, molecular dynamics (MD) simulation, and MM/GBSA free energy calculation on existing FDA-approved drugs. Sorafenib and glimepiride simultaneously downregulated c-Maf protein expression to induce G1 phase arrest and apoptosis in myeloma cells.

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Small Molecule Protein Expression FDA Approval FDA 100

Collaborative Drug

SEPTEMBER 23, 2024

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

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Small Molecule 102

Alta Sciences

JULY 28, 2023

Miniature Swine: Changing the Bias for Nonclinical Studies on Small Molecules and Biologics pmjackson Fri, 07/28/2023 - 16:07 Miniature swine have been widely used for research studies since the 1960s—most commonly within the scope of dermal testing due to similarities of their integument to humans.

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Small Molecule Pharmaceutical Companies Research FDA 52

Alta Sciences

JULY 28, 2023

Miniature Swine: Changing the Bias for Nonclinical Studies on Small Molecules and Biologics pmjackson Fri, 07/28/2023 - 16:07 Miniature swine have been widely used for research studies since the 1960s—most commonly within the scope of dermal testing due to similarities of their integument to humans.

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Small Molecule Pharmaceutical Companies Research FDA 52

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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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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Small Molecule Drugs Research Science 117

Drug Discovery Today

APRIL 20, 2023

Global integrated drug discovery company, Sygnature Discovery and global healthcare group Daewoong Pharmaceutical, have entered into a research collaboration agreement to accelerate the discovery of a novel small molecule to target autoimmune disease.

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Small Molecule Research Drugs Pharmaceuticals 113

ASPET

AUGUST 5, 2024

The ability of small molecule lipophilic ligands to function as exogenous chaperones was examined using receptor-selective antagonists. Finally, the effect of cannabidiol (CBD), a small molecule ligand and a major active component of Cannabis, on receptor abundance and activity in mice was examined.

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Small Molecule Regulations Treatment 100

ASPET

JULY 19, 2024

Here we design an assay to screen a compound library of small molecules inhibitors. Four compounds were identified as potential small molecule inhibitors one of which, BM-8372, demonstrated significant effect in platelet aggregation assays.

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Small Molecule Disease Research 100

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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Small Molecule Clinical Trials Engineering Trials 128

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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Small Molecule Disease Drugs Science 96

Chemical Biology and Drug Design

DECEMBER 15, 2023

In an effort to identify new lead compounds with potential anticancer properties for further optimization, in vitro assays combined with in-silico target fishing and docking studies have been used to identify and further map out the antiproliferative and potential mode of action of molecules from a small library of compounds previously prepared in (..)

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Small Molecule Protein Expression Laboratories Research 100

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. Liu is also a Howard Hughes Medical Institute investigator and a professor at Harvard University.

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Targeted Protein Degradation Small Molecule Medical Schools Science 141

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

JANUARY 10, 2024

Both are a focus for exciting new small-molecule drug therapeutics that target cancers and autoimmune disorders. There is extensive crosstalk between the DNA damage response (DDR) and innate immune pathways.

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DNA Biochemical Assays Small Molecule Drugs 104

Zobio

AUGUST 26, 2024

Het bericht Innovative NMR strategy provides structure of first-in-class small molecule inhibitors of the dual-specificity kinase MKK4 (MKK4i) verscheen eerst op ZoBio - Drug Discovery Technology.

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Small Molecule International Drugs 40