Drug Discovery World

JULY 30, 2024

DDW’s Megan Thomas speaks to Khan about the work her team is doing to create the first map of the druggable transcriptome, which involves understanding RNA biology to discover small molecule drugs. Understanding how RNA structure is linked to function would open up entirely new target space for the small molecule modality.

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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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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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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

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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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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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

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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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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

Drug Discovery World

AUGUST 30, 2024

With the launch of an international clinical trial investigating BioNTech’s mRNA lung cancer vaccine announced this week, our news highlights focus on clinical trials, including studies of a monoclonal antibody and small molecule GLP-1 agonist for obesity, and a muscarinic M4 selective agonist for schizophrenia.

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Drug Discovery World

OCTOBER 4, 2024

The proceeds of the Series A financing will be primarily used to support the pre-clinical development and initial clinical studies of LoQus23’s lead programme, an allosteric small molecule MutSβ inhibitor. The company is hoping to enter the clinic in 2026.

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Disease Therapies Small Molecule DNA 147

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 73

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

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

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Small Molecule 40

Drug Discovery World

AUGUST 20, 2024

Mirit Eldor , Managing Director, Life Sciences Solutions, Elsevier, looks at how artificial intelligence (AI) can improve the hit-to-lead process for small molecules. Research shows that companies could shorten this cycle by up to 30 months 2 over the course of the small molecule drug discovery process by applying AI.

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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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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

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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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.

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Small Molecule RNA Clinical Trials Drugs 52

Drug Discovery World

NOVEMBER 15, 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. A first-in-class small molecule Protein CRMP2 is a key regulator of the Cav2.2

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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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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 84

Drug Discovery World

SEPTEMBER 2, 2024

With the launch of an international clinical trial investigating BioNTech’s mRNA lung cancer vaccine announced this week, our news highlights focus on clinical trials, including studies of a monoclonal antibody and small molecule GLP-1 agonist for obesity, and a muscarinic M4 selective agonist for schizophrenia.

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Small Molecule Clinical Trials Vaccine Trials 147

Drug Discovery World

SEPTEMBER 27, 2024

Their launch has been supported by Pfizer’s Pharmaceutical Sciences Small Molecule (PSSM) division, with contracts for work to build their initial viability and momentum. The new businesses are all contract research organisations (CROs), namely Biowaived, Matheus Engineering and Particology.

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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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Drug Discovery World

SEPTEMBER 2, 2024

With the launch of an international clinical trial investigating BioNTech’s mRNA lung cancer vaccine announced this week, our news highlights focus on clinical trials, including studies of a monoclonal antibody and small molecule GLP-1 agonist for obesity, and a muscarinic M4 selective agonist for schizophrenia.

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Small Molecule Clinical Trials Vaccine International 130

Drug Discovery World

SEPTEMBER 9, 2024

NRG Therapeutics has discovered a new class of small molecule mitochondrial permeability transition pore (mPTP) inhibitors that can block mitochondrial dysfunction. This project aims to evaluate NRG’s small molecule inhibitor, in a modified ALS TDP-43 mouse model that progresses more slowly.

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Small Molecule Clinical Trials Disease Trials 162

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

Drug Discovery World

AUGUST 8, 2023

Astex Pharmaceuticals and MSD (Merck & Co) have announced an exclusive worldwide research collaboration to identify small molecule candidates with activity towards a tumour suppressor protein for the treatment of cancer.

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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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Drug Discovery World

JULY 19, 2024

The proceeds from the financing will be used to further develop Draupnir’s risk-diversified preclinical pipeline of oral, small molecule protein degraders, which have been proven against targets that are validated and those that have been traditionally difficult to drug.

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Targeted Protein Degradation Small Molecule Research Government 130

Drug Discovery World

DECEMBER 12, 2023

EXN407 is a small molecule inhibitor of splice factor kinase SRPK1. Patients in the Phase Ib/IIa trial were treated twice a day for three months, with either EXN407 or placebo. billion, CAGR 6.4% 2023-2030 for diabetic retinopathy alone), the demand for a topical therapy is high.

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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.

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Small Molecule 52

Drug Discovery World

APRIL 19, 2023

Scientists at The Institute of Cancer Research, London, are teaming up with small molecule neoantigen immuno-oncology company NeoPhore to develop new potential cancer drugs.

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Drug Discovery World

AUGUST 27, 2024

“The first-generation CB1 inhibitor, rimonabant, was a small molecule that acted on the CNS. We believe that nimacimab’s positive safety and tolerability profile places Skye at a competitive advantage over small molecule CB1 inhibitors.”

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