Covalent Modifiers

MARCH 22, 2024

2023.09.004 Recent years have seen a remarkable growth in the field of protein-based medical treatments. Zhang Han Xiao C ell Chemical Biology, 2024 Volume 31, 3, 428 - 445 [link] j. As a result, proximity-induced chemistry is reshaping the field of protein drug preparation and propelling the revolution in novel protein therapeutics.

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Small Molecule Engineering Treatment Drugs 237

Chemical Biology and Drug Design

JANUARY 27, 2025

This study investigates the effects and mechanisms of combining Polyphyllin VII (PPVII) with Docetaxel (DTX) in the treatment of prostate cancer (Pca). This study reveals the synergistic effects of combining PPVII with DTX and provides a reference for overcoming DTX resistance in clinical Pca treatment.

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Chemical Biology and Drug Design

JANUARY 29, 2024

sPLA 2 inhibitors have been developed for the treatment of inflammatory and other conditions such as cardiovascular disease, arteriosclerosis and rheumatoid arthritis. Due to their roles in inflammation, the sPLA 2 enzymes are of much medicinal interest.

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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

Drug Target Review

NOVEMBER 25, 2024

As the CEO of iOnctura, an innovative oncology biopharmaceutical company she co-founded in 2017, Catherine has played a key role in advancing the development of highly targeted small molecules aimed at revolutionising cancer treatment. This is exciting because often resistance builds up to these other treatments.

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Treatment Small Molecule Clinical Trials Trials 52

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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Covalent Modifiers

JULY 25, 2024

We have integrated structural and quantitative proteomics with biochemical assays to decipher the mode of action of covalent USP30 inhibition by a small molecule containing a cyanopyrrolidine reactive group, USP30-I-1.

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Biochemical Assays Small Molecule Treatment Disease 182

Drug Target Review

OCTOBER 11, 2023

Most of these conditions are genetic in origin and the majority have no effective treatment. That includes countless rare peripheral diseases, including many for which there are currently no treatments. Autophagy boosters, in contrast, are conventional small molecule drugs.

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Disease Treatment Small Molecule Therapies 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. ADCs have the potential to redress the poor balance between safety and efficacy seen with traditional cancer treatment options. 3D rendering of Antibody Drug Conjugate Molecules.

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Small Molecule Drugs Clinical Pharmacology Trials 145

PPD

NOVEMBER 11, 2024

However, getting essential treatments to patients quickly and safely requires more than just technological innovation. A global network with local expertise To ensure the delivery of treatments to patients worldwide, biotech and biopharma companies also need partners that can provide comprehensive solutions from a geographic perspective.

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Drug Development Clinical Trials Drugs Small Molecule 97

Covalent Modifiers

OCTOBER 7, 2023

Zhang, Han Xiao, Cell Chemical Biology , 2023 [link] Recent years have seen a remarkable growth in the field of protein-based medical treatments. Linqi Cheng, Yixian Wang, Yiming Guo, Sophie S.

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Small Molecule Engineering Treatment Drugs 162

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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Small Molecule FDA Approval FDA Pharmacokinetics 59

Chemical Biology and Drug Design

OCTOBER 20, 2023

Details about the enzyme sequence and structural properties make a compelling case for designing small molecule inhibitors that are specific to the amoebae and would not affect the host enzyme. Unfortunately, the efficacy of these can be limited, driving the need for the discovery of new treatments.

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Treatment Small Molecule Drug Development Drugs 100

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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Small Molecule FDA Approval FDA Pharmacokinetics 52

Metabolite Tales Blog

APRIL 4, 2023

Metabolism of 2022 FDA approved small molecule drugs part 2 Mixing it Up By Julia Shanu-Wilson In Part 1 of this topic we looked at metabolism of the small molecule drugs approved by the FDA in 2022 that were mediated by CYP3A4. Dermavant’s tapinarof is one such friend. 8 This is not the only point of interest.

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Small Molecule FDA Approval FDA Drugs 52

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. . Our ambition is to develop life-changing treatments for patients.

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Small Molecule Disease Immune Response Licensing 52

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

Drug Target Review

APRIL 7, 2025

Susceptibility or risk biomarkers can detect the likelihood of a patient developing a disease or medical condition, which is crucial for treatments that are most effective before the onset of symptoms. A biomarker is a measurable indicator of a biological process, disease state, or response to a treatment.

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Clinical Development Clinical Trials Clinical Pharmacology Trials 69

ASPET

AUGUST 5, 2024

The ability of small molecule lipophilic ligands to function as exogenous chaperones was examined using receptor-selective antagonists. Long term treatment leads to increases in receptor abundance and activity with no changes in mRNA supporting a role as pharmacological chaperones.

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Small Molecule Regulations Treatment 100

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

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

DrugBank

JULY 24, 2024

These multifunctional small molecules are like tiny spies, hijacking the body’s natural protein degradation system to remove unwanted proteins. Similarly, PROTACs can target and degrade overexpressed proteins, offering a way to overcome drug resistance, a common issue in cancer treatment.

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Small Molecule Drugs Clinical Trials Therapies 98

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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Drug Target Review

JULY 12, 2023

Molecular-level biochemical assays like transcriptomics, genomics and proteomics have emerged as valuable tools for identifying potential targets in cancer treatment through deep cyclic inhibition (DCI). How does the DCI mechanism compare to the design of other drugs for cancer treatment?

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Biochemical Assays Treatment Bioinformatics Disease 98

ASPET

OCTOBER 12, 2023

Supramolecular nanostructured based delivery systems are emerging as a meaningful approach in treatment of cancer, offering controlled drug release and improved therapeutic efficacy. These structures can improve the solubility and stability of drugs having low aqueous solubility by encapsulating and protecting them from degradation.

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Therapies Small Molecule Treatment Drugs 100

Drug Hunter

JUNE 26, 2023

This article compiles recent high-profile clinical readouts and related news with small molecules of general interest and structures where they are available. Sepiapterin (synthetic) is a precursor of tetrahydrobiopterin (BH 4 ), which is essential for degradation of phenylalanine.

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DrugBank

MAY 22, 2024

Consider aminergic GPCRs and kinases —while many drugs hit these proteins, they often affect more than one target, a phenomenon known as polypharmacology, leading to complex treatment profiles and side effects. Many cancer treatments target DNA, but often these can cause collateral damage, leading to severe side effects.

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Small Molecule RNA DNA Pharmaceutical Companies 96

Drug Target Review

OCTOBER 6, 2023

This interview explores how CoRegen’s innovative techniques are not only transforming cancer treatment but also hold promise for a wide range of medical applications, all while minimising the side effects often associated with traditional therapies. For what indications can this approach be used?

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Small Molecule Engineering Protein Expression Therapies 111

Drug Target Review

SEPTEMBER 25, 2024

4 Another related and well described non-oncogene resistance mechanism is the histological transformation of EGFR-mutated non-small cell lung cancer (NSCLC) to small-cell lung cancer upon treatment with an EGFR inhibitor. This orally available small molecule binds to the bromodomain of CBP/p300 in a highly specific manner.

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Small Molecule Therapies Regulations Treatment 105

Chemical Biology and Drug Design

MAY 11, 2023

Abstract Proprotein convertase subtilisin/kexin type 9 (PCSK9) has emerged as a promising therapeutic target for the treatment of hyperlipidemia. In discovery of novel small molecules that interfere PCSK9/LDLR protein–protein interaction (PPI), structural modification was performed based on our previously derived compounds.

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Olympian Clinical Research

MAY 6, 2024

The journey toward effective treatments has been long and evolving, with recent breakthroughs offering new hope to those living with this challenging condition. From Coal Tar to Biologics: A Historical Perspective The history of psoriasis treatment is as old as the condition itself, with records dating back to ancient times.

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Treatment Small Molecule Clinical Research Immune Response 52

Chemical Biology and Drug Design

JUNE 7, 2023

Our MD simulation results also revealed that the 5-hydroxy-4H-thioxen-4-one group and terminal carboxyl group were critical groups responsible for interaction of small molecules with SIRT7. In our study, we demonstrated that targeting SIRT7 may offer novel therapeutic options for cancer treatment.

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Drug Target Review

JULY 23, 2024

This laid the groundwork for my career in drug discovery using novel modalities like small molecule inhibitors, antibodies, RNA interference (RNAi) and, currently, small molecule protein degraders – which are opportunities to change how we think about medicines.

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Small Molecule Targeted Protein Degradation Science Disease 116

Drug Target Review

APRIL 7, 2025

Advancements in screening technologies for small-molecule drug discovery including cellular assays, computational screening, and biophysics-based methods enhanced by structural biology breakthroughs have improved screening hit rates and facilitated the identification of drug candidates for previously undruggable targets.

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Fragment Screening Drugs Small Molecule Biophysical Assays 52

ASPET

SEPTEMBER 7, 2023

Alglucosidase alfa, a recombinant human acid α-glucosidase, was the first approved treatment for Pompe disease, but its uptake into skeletal muscle via the cation-independent mannose-6-phosphate (M6P) receptor (CIMPR) is limited. These results further substantiate the crucial role of CIMPR binding in lysosomal targeting of ERTs.

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Chemical Biology and Drug Design

JULY 27, 2023

Abstract The small molecule, isatin, is a well-known reversible inhibitor of the monoamine oxidase (MAO) enzymes with IC 50 values of 12.3 This study investigated the SARs of MAO inhibition by isatin analogues and discovered five compounds with IC 50  < 1 μM. μM for MAO-A and MAO-B, respectively.

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