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 52

Small Molecule Therapies Production 52

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

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

Metabolite Tales Blog

JANUARY 26, 2023

Metabolism of 2022 FDA approved small molecule drugs – Part 1 Does CYP3A4 still rule? By Julia Shanu-Wilson It won’t come as much surprise to learn that of the 17 small molecules* approved by the FDA in 2022, CYP3A4 was the major player in drug metabolism. References Iversen et al., Front Pharmacol.,

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Small Molecule FDA Approval FDA Drugs 52

Alta Sciences

SEPTEMBER 14, 2023

PBSS—Human PK and Dose Prediction for Small Molecules lperez Thu, 09/14/2023 - 19:16 Image GettyImages-1075448458.jpg jpg Tags Preclinical Research URL [link] Event End Date Fri, 10/06/2023 - 12:00 Event Start Date Fri, 10/06/2023 - 12:00 Weight 1

Small Molecule 40

Small Molecule Research 40

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.

Small Molecule 52

Small Molecule Pharmaceutical Companies Research FDA 52

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

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"

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Small Molecule Drugs 296

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).

Small Molecule 100

Small Molecule Treatment 100

Alta Sciences

DECEMBER 29, 2023

PBSS—ADME/DMPK Studies for IND and NDA Filing for Small Molecules: Nuts, Bolts and Best Practices lperez Fri, 12/29/2023 - 16:20 Image GettyImages-1075448458.jpg jpg Synopsis Foster City, CA URL [link] Event End Date Fri, 01/19/2024 - 12:00 Event Start Date Fri, 01/19/2024 - 12:00 Weight 1

Small Molecule 40

Small Molecule 40

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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Small Molecule Research Science Disease 52

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 117

Dark Matter Blog

AUGUST 27, 2020

A few years ago, at Arrakis Therapeutics, we set out to conquer a strange new territory, drugging RNA structures with small molecules. Dramatic discoveries of small molecules targeting SMN2 Prior to those outstanding therapeutic achievements, in 2015, a group from Novartis published an important paper in Nature Chemical Biology.

Small Molecule 52

Small Molecule RNA Clinical Trials Drugs 52

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

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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Small Molecule Disease Immune Response Licensing 52

The Pharma Data

JANUARY 19, 2021

Precision medicine developer Kura Oncology is positioned to make a meaningful difference in the treatment of cancer in the next few years with its two, wholly-owned, small molecule compounds. Photo courtesy of Kura. It’s in the spotlight, the data is stunning, and it has a lot of promise,” Troy Wilson, Ph.D., CEO, told BioSpace.

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Small Molecule Therapies FDA Approval Trials 52

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.

Small Molecule 100

Small Molecule Protein Expression FDA Approval FDA 100

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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Small Molecule Immune Response Research Laboratories Laboratories 52

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.

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Small Molecule Drugs 238

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.

Small Molecule 100

Small Molecule Regulations Treatment 100

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 117

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 86

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.

Small Molecule 100

Small Molecule Disease Research 100

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 52

Small Molecule 52

ASPET

SEPTEMBER 16, 2024

We previously identified a small molecule, UM101, predicted to bind to the substrate-binding groove of p38aMitogen-activated Protein Kinase (MAPK) near the binding site of its proinflammatory substrate, MAPK-activated protein kinase (MK2). UM101 exhibited anti-inflammatory, endothelial-stabilizing, and lung-protective effects.

Small Molecule 100

Small Molecule Drugs 100

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.

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Small Molecule Engineering Science Therapies 72

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 133

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 (..)

Small Molecule 100

Small Molecule Protein Expression Laboratories Research 100

Drug Hunter

JUNE 11, 2023

Small molecule drugs make up most of the drugs we take conveniently as pills, including painkillers like ibuprofen (Advil), antibiotics like penicillin and amoxicillin, or cholesterol-lowering drugs like atorvastatin (Lipitor). The small molecules drugs of today look nothing like the molecules of the 1970s.

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Small Molecule Treatment Engineering Pharmaceuticals 147

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

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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Small Molecule Therapies Research 125

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 141

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.

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Small Molecule Clinical Trials Drugs Therapies 82

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.

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Small Molecule 78

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

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