Biofront Ltd. has designed new proteolysis targeting chimeras (PROTACs) comprising an E3 ubiquitin ligase-binding moiety coupled to a mitogen-activated protein kinase kinase kinase kinase 1 (MAP4K1; HPK1; MEKKK1)-targeting moiety as HPK1 degradation inducers. They are described as potentially useful for the treatment of cancer.
Tyligand Bioscience Ltd. has reported new dual-drug antibody-drug conjugates comprising monoclonal antibodies covalently linked to stimulator of interferon genes protein (STING; TMEM173) agonist and a cytotoxic drug.
Aktis Oncology Inc. has obtained IND approvals from the FDA enabling the company to proceed to a phase Ib trial with AKY-2519, a miniprotein radioconjugate targeting B7-H3-expressing tumors, including prostate, lung and other solid tumors. Specifically, the IND clearances relate to [64Cu]Cu-AKY-2519 for imaging and [225Ac]Ac-AKY-2519 for therapeutic use.
Certain cancers, such as triple-negative breast cancer, produce antibodies that, although they help fight the tumor, can cross the blood-brain barrier and alter the function of NMDA receptors (NMDAR) in the brain, which are essential for neuronal signaling. Scientists at Cold Spring Harbor Laboratory (CSHL) have identified their origin and described how this process is linked to the maturation of these antibodies, which can activate or inhibit the receptor, causing neurological and psychiatric symptoms.
Introduced last year as a pilot program, the U.S. FDA Commissioner’s National Priority Voucher (CNPV) could be here to stay – at least for the duration of Marty Makary’s tenure as FDA commissioner. Since the FDA unveiled the CNPV last June, it has welcomed 18 products from 16 companies into the “game-changer” program for patients, as Makary described it. The goal is to provide an “ultrafast review pathway,” one to two months instead of the standard 10 to 12 months, for drugs and biologics of strategic national importance while maintaining the FDA’s scientific and regulatory standards, according to the agency.
Nanjing Sanhome Pharmaceutical Co. Ltd. has synthesized new Werner syndrome ATP-dependent helicase (WRN; RECQ3; RECQL2) inhibitors potentially useful for the treatment of cancer.
A University of Texas System patent describes new radiolabeled positron emission tomography (PET) imaging agents targeting receptor-interacting serine/threonine-protein kinase 1 (RIPK1; RIP-1). As such, they are potentially useful for the diagnosis of cancer, retinal and autoimmune diseases, neurological and inflammatory disorders.
Researchers from Blueprint Medicines Corp. and F. Hoffmann-La Roche Ltd. presented the preclinical characterization of BLU-852, a selective MAP4K1 inhibitor developed as a potential immunotherapeutic agent for cancer treatment.
Using Iambic Therapeutics’ AI/HTE platform, researchers at the company have engineered a next-generation HER2 inhibitor with superb selectivity for HER2, as well as broad mutant coverage and brain penetrance. The compound, IAM-1363, binds to HER2 in a type II DFG-out conformation, which represents the first reported type II HER2 tyrosine kinase inhibitor.
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.
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