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BioWorld - Sunday, December 21, 2025
Home » Topics » Small molecule, BioWorld Science

Small molecule, BioWorld Science
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Ischemic stroke
Cardiovascular

Esculetin promotes stroke rehabilitation by inhibiting CKLF1

Aug. 13, 2024
Esculetin, also known as 6,7-dihydroxycoumarin, is a coumarin-derived phytochemical that has shown effects against ischemic stroke. Additionally, chemokine-like factor 1 (CKLF1) has been revealed in previous findings to be a target for stroke when using coumarin-derived compounds. The effects of esculetin and the potential involvement of CKLF1 were tested in photothrombotic stroke in mice.
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Man holding hand up to ear
Ear, nose & throat

Piplartine counteracts antibiotic-induced hearing loss

Aug. 13, 2024
Piplartine, also called piperlongumine, had protective effects against hearing loss induced by aminoglycoside antibiotics in zebrafish and mouse models of kanamycin-induced hair cell loss. Kanamycin is a member of the aminoglycosides, a group of antibiotics that have broad-spectrum activity against gram-negative bacteria, including multidrug resistant strains.
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Doctor points at molecular structure
Cancer

Halda nabs $126M, publishes proof of concept

Aug. 12, 2024
Halda Therapeutics Inc. announced it has secured an additional $126 million in funding in a series B extension, bringing its total funding to date to $202 million. The company expects its lead molecule HLD-0915 to enter a phase I trial in the first half of 2025 for the treatment of patients with metastatic castration-resistant prostate cancer (mCRPC).
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3D illustration of a nerve cell
Neurology/psychiatric

Negative allosteric modulator of TrkA has efficacy in pain models

Aug. 9, 2024
Researchers from Alzecure Pharma AB presented preclinical data for ACD-137, a negative allosteric modulator (NAM) of tropomyosin receptor kinase A (TrkA), being developed for the treatment of pain.
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Drug R&D concept image.
Neurology/psychiatric

PIPE-791 is antinociceptive in peripheral neuropathy model

Aug. 9, 2024
Researchers from Contineum Therapeutics Inc. have presented preclinical data for the novel brain penetrant lysophosphatidic acid receptor 1 (LPAR1) antagonist, PIPE-791, being evaluated in models of neuropathic pain.
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Pipet, test tubes, chemical structures
Neurology/psychiatric

GABA-AT inhibitor OV-329 is analgesic in preclinical models

Aug. 8, 2024
Researchers from Indiana University have presented data from a study that aimed to assess the potential of suppressing GABA metabolism through inhibition of its degradation enzyme, GABA aminotransferase (GABA-AT), as novel analgesic strategy. The effect of next-generation GABA-AT inhibitor OV-329 was assessed in C57BL/6J mice that were intraperitoneally injected with paclitaxel to generate neuropathic nociception. Treatment with OV-329 attenuated the development and maintenance of paclitaxel-induced mechanical hypersensitivity.
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Scanning electron micrograph of MRSA interacting with a neutrophil
Infection

Vancomycin derivatives overcome multidrug resistance in S. aureus

Aug. 8, 2024
Researchers at Leiden University have synthesized semisynthetic guanidino lipoglycopeptides with in vitro and in vivo activity gram-positive bacteria, including methicillin-resistant and vancomycin-resistant Staphylococcus aureus.
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Neurology/psychiatric

Seed blooms with $1.5B Eisai deal

Aug. 7, 2024
By Lee Landenberger
Big pharma continues to invest heavily into molecular glue degraders. The latest deal has Eisai Co. Ltd. striking up a research collaboration that could bring Seed Therapeutics Inc. up to $1.5 billion in up-front and milestone payments. The two said they plan to discover, develop and commercialize MGDs for several undisclosed neurodegeneration and oncology targets.
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Cross section illustration of ion channel in cell membrane
Neurology/psychiatric

Nav1.8 inhibitor MSD-199 has activity in inflammatory, neuropathic pain models

Aug. 7, 2024
Researchers from Merck & Co Inc. have presented preclinical data for the novel Nav1.8 inhibitor MSD-199, being developed for the treatment of inflammatory and neuropathic pain.
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Multiple myeloma illustration
Cancer

Fibroblast growth factor traps have anti-myeloma activity

Aug. 6, 2024
Researchers from the University of Brescia have presented the discovery and preclinical characterization of novel fibroblast growth factor (FGF) trap small molecules, being developed for the treatment of multiple myeloma (MM).
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