https://www.bioworld.com/rss en-us Researchers from Chongqing Medical University have presented data regarding an antiviral compound, KM-10411, derived from a FUBP1 inhibitor (FUBP1-IN-1), as a potential approach to treat hepatitis B virus (HBV) infections. http://www.bioworld.com/articles/732551 Fri, 10 Jul 2026 09:00:00 -0400 https://www.bioworld.com/articles/732551-km-10411-shows-anti-hbv-effects-dependent-on-dusp5 Hepatitis B virus In a recent study, researchers from Kobe University Graduate School of Medicine and collaborators aimed to identify novel insulinotropic small molecules related to ion channel modulation. http://www.bioworld.com/articles/732456 Tue, 07 Jul 2026 09:00:00 -0400 https://www.bioworld.com/articles/732456-mdc-134-enhances-glucose-dependent-cell-insulin-secretion Glucose metabolism illustration Insulin allows the glucose channel to open, allowing glucose to enter the cell. Focal adhesion kinase (FAK), a key mediator of cell adhesion and migration, is frequently upregulated in glioblastoma (GBM), where its activity has been associated with increased tumor invasiveness and disease aggressiveness. http://www.bioworld.com/articles/732381 Fri, 03 Jul 2026 09:00:00 -0400 https://www.bioworld.com/articles/732381-fak-inhibitor-tested-in-glioblastoma-models Art concept for drug research Predominantly expressed in the striatum, a brain region involved in cognition, motivation and motor control, G protein-coupled receptor 52 (GPR52) regulates dopaminergic and glutamatergic signaling pathways implicated in psychiatric disorders. http://www.bioworld.com/articles/732309 Tue, 30 Jun 2026 09:00:00 -0400 https://www.bioworld.com/articles/732309-novel-gpr52-agonist-shows-antipsychotic-like-effects Receptor-interacting protein kinase 1 (RIPK1) acts as a central signaling node regulating apoptosis, necroptosis and inflammatory pathways. Researchers from China Pharmaceutical University reported the discovery and preclinical characterization of LT-1339-553, a novel RIPK1 inhibitor, in models of schistosomiasis-induced hepatic fibrosis. http://www.bioworld.com/articles/732192 Fri, 26 Jun 2026 09:00:00 -0400 https://www.bioworld.com/articles/732192-new-ripk1-inhibitor-protects-from-hepatic-fibrosis 3D molecular model illustration of RIPK1 RIPK1 Researchers from Bayer AG reported the discovery and preclinical characterization of BAY-439, a potent and selective hPLA2-G5 inhibitor, in models of pain. http://www.bioworld.com/articles/732114 Tue, 23 Jun 2026 09:00:00 -0400 https://www.bioworld.com/articles/732114-hpla2-g5-inhibition-exerts-analgesic-and-anti-inflammatory-effects Researchers from Zhejiang University of Technology and collaborators presented the discovery and preclinical characterization of YSA-64, a novel RBM39 degrader, in cancer models. http://www.bioworld.com/articles/731764 Tue, 09 Jun 2026 09:00:00 -0400 https://www.bioworld.com/articles/731764-rbm39-degraders-show-efficacy-in-ewing-sarcoma-tumors Concept art for targeting cancer Ubiquitin carboxyl-terminal hydrolase 1 (USP1) is a synthetic lethality target in cancers with high replication stress, such as tumors with BRCA gene mutations or homologous recombination deficiency (HRD). Targeting USP1 has emerged as a promising approach to overcome resistance observed in BRCA/HRD-driven tumors. Aigen Sciences Inc. developed and presented data for AIG-07025, a potent and selective USP1 inhibitor. BRCA gene mutations or homologous recombination deficiency (HRD). Targeting USP1 has emerged as a promising approach to overcome resistance observed in BRCA/HRD-driven tumors. Aigen Sciences Inc. developed and presented data for AIG-07025, a potent and selective USP1 inhibitor.]]> http://www.bioworld.com/articles/731143 Mon, 18 May 2026 09:00:00 -0400 https://www.bioworld.com/articles/731143-aigens-aig-07025-shows-potential-for-brca-hrd-driven-cancers Microscope with slide Werner syndrome helicase (WRN), belonging to the RecQ helicase family, represents a synthetic lethal vulnerability in MSI-H cancers, providing a strong rationale for therapeutic inhibition. Researchers from Simcere Zaiming Pharmaceutical Co. Ltd. reported the discovery and preclinical characterization of ZMS-4084, a novel WRN inhibitor. http://www.bioworld.com/articles/731128 Fri, 15 May 2026 09:00:00 -0400 https://www.bioworld.com/articles/731128-zms-4084-shows-robust-antitumor-efficacy-in-msi-h-cancer-models Cancer cells under magnifying glass Researchers from Sunshine Biopharma Inc. and the University of Arizona reported the discovery and preclinical characterization of MR-1-114, a noncovalent inhibitor of the SARS-CoV-2 papain-like protease (PLpro). http://www.bioworld.com/articles/731000 Mon, 11 May 2026 09:00:00 -0400 https://www.bioworld.com/articles/731000-next-generation-plpro-inhibitor-for-sars-cov-2-divulged Coronavirus punch Syracuse University recently presented a comprehensive preclinical program describing the rational design and optimization of peptide antagonists targeting the GDF15/GFRAL/RET receptor complex to mitigate nausea, emesis, anorexia and wasting associated with chemotherapy-induced stress signaling. http://www.bioworld.com/articles/730453 Fri, 17 Apr 2026 09:00:00 -0400 https://www.bioworld.com/articles/730453-peptide-gfral-ret-antagonists-against-gdf15-induced-effects-of-chemotherapy Art concept for drug research Mixed lineage kinase domain-like pseudokinase (MLKL), a key effector of necroptosis, is highly expressed in hepatocellular carcinoma (HCC), and its targeting may promote parthanatos-mediated immunogenic cell death. Researchers from the Chinese Academy of Sciences and collaborators described the discovery and preclinical characterization of C-116, a MLKL PROTAC degrader developed using AI-assisted rational drug discovery. http://www.bioworld.com/articles/730450 Fri, 17 Apr 2026 09:00:00 -0400 https://www.bioworld.com/articles/730450-targeted-mlkl-degradation-drives-parthanatos-in-hcc 3D representation of tumor Cisplatin is widely used in chemotherapy regimens for many solid tumors, yet its therapeutic benefit is counterbalanced by significant toxicity and immunologically related limitations. Researchers from Jiangxi University of Chinese Medicine described the preclinical efficacy of the PD-L1-targeted cisplatin prodrug MN42-81, designed to overcome these limitations. http://www.bioworld.com/articles/730449 Fri, 17 Apr 2026 09:00:00 -0400 https://www.bioworld.com/articles/730449-cisplatin-prodrug-enables-safe-pd-l1-targeted-chemo-immunotherapy Illustration of interaction between PD-1 and PD-L1 blocked by therapeutic antibodies Signal transducer and activator of transcription 3 (STAT3) is a central mediator of cytokine and growth factor signaling and is aberrantly activated in approximately 70% of human cancers. Persistent STAT3 signaling drives tumor proliferation, survival, metastasis, angiogenesis, immune evasion and inflammation. Researchers from the University of Michigan reported the discovery and preclinical characterization of SD-965, a selective STAT3 PROTAC degrader. http://www.bioworld.com/articles/730448 Fri, 17 Apr 2026 09:00:00 -0400 https://www.bioworld.com/articles/730448-selective-stat3-degrader-with-efficacy-in-hematological-cancer-models Microtubule-associated serine/threonine kinase-like protein (MASTL) is a key regulator of mitotic progression and cell-cycle control. Researchers from the Korea Institute of Radiological and Medical Sciences reported the preclinical efficacy of MKI-3, a selective MASTL inhibitor. http://www.bioworld.com/articles/730375 Wed, 15 Apr 2026 09:00:00 -0400 https://www.bioworld.com/articles/730375-mastl-inhibitor-shows-robust-antitumor-efficacy Cancer cell, dropper, test tubes Caspase-2-mediated cleavage of tau at Asp314 generates a neurotoxic fragment, Δtau314, that drives early synaptic dysfunction in Alzheimer’s disease (AD) and frontotemporal dementia (FTD). This fragment accumulates at synapses, disrupts glutamatergic signaling and contributes to cognitive impairment in vivo. http://www.bioworld.com/articles/730346 Tue, 14 Apr 2026 09:00:00 -0400 https://www.bioworld.com/articles/730346-novel-caspase-2-inhibitor-shows-in-vivo-neuroprotective-effects Retinoid X receptor γ (RXRγ) is a key nuclear receptor that sustains androgen receptor (AR) signaling. In castration-resistant prostate cancer (CRPC), RXRγ contributes to disease progression by maintaining adaptive transcriptional networks that promote therapy resistance and tumor cell survival. http://www.bioworld.com/articles/730328 Mon, 13 Apr 2026 09:00:00 -0400 https://www.bioworld.com/articles/730328-selective-rxr-degrader-shows-efficacy-in-prostate-cancer-models Photomicrograph of core biopsy of prostate gland showing histology of adenocarcinoma in patient with elevated PSA. Researchers from Syngenta AG and collaborators reported the preclinical characterization of CHNQD-01522, a microtubule-targeting agent designed based on the marine natural product penipanoid C, in hepatocellular carcinoma (HCC) models. http://www.bioworld.com/articles/730191 Wed, 08 Apr 2026 09:00:00 -0400 https://www.bioworld.com/articles/730191-chnqd-01522-microtubule-destabilizer-demonstrates-efficacy-in-hcc-models 3D rendering of microtubule: Minus-end, GDP-lattice and GTP-cap at plus-end Scientific structure of microtubule. Liver receptor homolog-1 (LRH-1) is a nuclear receptor that promotes the transcription of genes encoding key steroidogenic enzymes, thereby facilitating de novo androgen biosynthesis within the prostate tumor microenvironment. Researchers from Qilu Pharmaceutical Co. Ltd. reported the discovery and preclinical characterization of a series of novel LRH-1 antagonists. http://www.bioworld.com/articles/730171 Tue, 07 Apr 2026 09:00:00 -0400 https://www.bioworld.com/articles/730171-new-lrh-1-antagonists-exhibit-antitumor-activity-in-prostate-cancer-models 3D illustration showing tumor inside prostate gland and closeup view of cancer cells In both acute myeloid leukemia (AML) and synovial sarcoma (SS), targeting BRD9 disrupts oncogenic transcriptional programs, including MYC, leading to reduced proliferation and induction of apoptosis. Researchers from Pamplona Therapeutics (Shenzhen) Co. Ltd. reported the discovery and preclinical efficacy profile of XYD-270, a BRD9-targeting PROTAC, in models of SS and AML. http://www.bioworld.com/articles/730016 Mon, 30 Mar 2026 09:00:00 -0400 https://www.bioworld.com/articles/730016-brd9-protac-shows-efficacy-in-sarcoma-and-leukemia-models Art concept for hematologic cancer Researchers from the Chinese Academy of Sciences reported the design and preclinical characterization of YCH-3971, a selective PARP1 inhibitor developed for the treatment of BRCA-mutated tumors. http://www.bioworld.com/articles/729935 Thu, 26 Mar 2026 09:00:00 -0400 https://www.bioworld.com/articles/729935-selective-parp1-inhibitor-disclosed Illustration of cancer cell in crosshairs being destroyed Researchers from GSK plc and collaborators described the identification of MMV-1581361, a PfATP4 inhibitor, and its efficacy in models of malaria. The compound originates from MMV-020136, following structure-activity relationship studies to optimize antimalarial activity. PfATP4 inhibitor, and its efficacy in models of malaria. The compound originates from MMV-020136, following structure-activity relationship studies to optimize antimalarial activity.]]> http://www.bioworld.com/articles/729934 Thu, 26 Mar 2026 09:00:00 -0400 https://www.bioworld.com/articles/729934-mmv-1581361-combines-strong-antimalarial-efficacy-with-transmission-blockade Release of malaria parasites from red blood cell Atopic dermatitis (AD) is an inflammatory skin disease accompanied by pruritus, for which IL-13 and IL-31 are clinically validated targets. Earendil Labs Inc. has developed a bispecific antibody targeting both IL-13 and IL-31, HX-16108, with an extended half-life. http://www.bioworld.com/articles/729592 Wed, 11 Mar 2026 09:00:00 -0400 https://www.bioworld.com/articles/729592-hx-16108-holds-promise-for-treating-inflammatory-skin-diseases Skin irritation on hands Researchers in China reported the discovery and preclinical characterization of ZX-079, a novel BRD4/CBP PROTAC degrader. http://www.bioworld.com/articles/729325 Wed, 04 Mar 2026 08:00:00 -0500 https://www.bioworld.com/articles/729325-dual-degrader-shows-activity-in-acute-myeloid-leukemia-models Microscopic image of acute myeloid leukemia (AML) cells. Acute myeloid leukemia cells. Credit: Cincinnati Children's Researchers from Specally (Wuhan) Life Technology Co. Ltd. have disclosed the discovery and preclinical profile of WWZ-11-098, a non-palbociclib-based, selective cyclin-dependent kinase 6 (CDK6) degrader in models of leukemia. http://www.bioworld.com/articles/729154 Tue, 03 Mar 2026 08:00:00 -0500 https://www.bioworld.com/articles/729154-newly-described-selective-cdk6-degrader-exhibits-potential-in-leukemia-models Leukemia illustration Antimicrobial resistance (AMR) is increasingly compromising the effectiveness of essential antibiotics, resulting in higher global mortality and morbidity rates. Despite this urgent need, few new antibiotics, particularly against gram-negative bacteria, are in development. http://www.bioworld.com/articles/728921 Wed, 18 Feb 2026 08:00:00 -0500 https://www.bioworld.com/articles/728921-first-in-class-non-lactam-targeting-amr-gram-negative-pathogens Klebsiella pneumoniae colonies in petri dish Fibroblast growth factor receptor 2 (FGFR2) is a transmembrane tyrosine kinase that regulates signaling pathways controlling cell survival and proliferation. Dysregulation of FGFR2, through amplification or activating mutations, contributes to tumor development, making it an attractive target for therapeutic intervention in oncology. http://www.bioworld.com/articles/728919 Wed, 18 Feb 2026 08:00:00 -0500 https://www.bioworld.com/articles/728919-new-compound-against-tumors-with-aberrant-fgfr2-signaling Researchers from Fudan University reported the development of CZL-077, a p300/CBP bromodomain inhibitor. p300 and CREB-binding protein (CBP) are closely related histone acetyltransferases that play central roles in regulating gene expression. Dysregulation of these proteins has been implicated in tumorigenesis and the development of therapy resistance. http://www.bioworld.com/articles/728887 Mon, 16 Feb 2026 08:00:00 -0500 https://www.bioworld.com/articles/728887-czl-077-shows-robust-preclinical-antitumor-activity Vials, syringes, and pills Triple-negative breast cancer (TNBC) cells depend on the transcriptional kinases CDK12 and CDK13 to maintain DNA damage response gene expression and manage replication stress. Due to their functional overlap, inhibition of a single kinase may permit compensatory activity. http://www.bioworld.com/articles/728815 Thu, 12 Feb 2026 08:00:00 -0500 https://www.bioworld.com/articles/728815-new-cdk12-13-dual-degrader-for-tnbc Illustration of tumor in breast DNA polymerase θ (POLθ) is a specialized, error-prone DNA polymerase that promotes the repair of DNA double-strand breaks through theta-mediated end joining (TMEJ), an alternative pathway that operates independently of homologous recombination. http://www.bioworld.com/articles/728630 Thu, 05 Feb 2026 08:00:00 -0500 https://www.bioworld.com/articles/728630-sy-589-suppresses-hr-deficient-tumors-via-pol-inhibition