Scientists at Beone Medicines I GmbH and Beone Pharmaceutical (Suzhou) Co. Ltd. have divulged histone acetyltransferase KAT6A (MOZ; MYST-3) and histone acetyltransferase KAT6B (MOZ2; MYST-4) inhibitors reported to be useful for the treatment of breast cancer.
Amphista Therapeutics Ltd. has nominated AMX-883, a selective and orally bioavailable degrader of BRD9, as its first clinical development candidate. AMX-883 is being advanced for the treatment of acute myeloid leukemia (AML), with an IND application planned for early next year.
Tumors suffer metabolic stress, such as oxygen and nutrient deficiency; as a result, altered metabolism is a common feature of tumors. Cancer cells enhance the production of energy and the synthesis of macromolecules to grow at pathologically increased rates. It is crucial to identify genes that modulate cellular fitness under these stressful scenarios.
Littdd Medicines Ltd. has described mTOR complex 1 (mTORC1) and/or mTOR complex 2 (mTORC2) inhibitors reported to be useful for the treatment of cancer, idiopathic pulmonary fibrosis, transplant rejection, autoimmune and metabolic diseases, Huntington’s disease, Parkinson’s disease and Alzheimer’s disease, among others.
Aurigene Oncology Ltd. has identified proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase protein binding moiety covalently linked to probable global transcription activator SNF2L2 (SMARCA2; BAF190B; SNF2-α) and/or transcription activator BRG1 (SMARCA4; BAF190A; SNF2-β) binding moieties through a linker reported to be useful for the treatment of cancer.
CXC chemokine receptor 4 (CXCR4) is a receptor overexpressed in several tumor types and associated with tumor aggressiveness and risk of metastasis, resistance and recurrence. A novel PET radiopharmaceutical tracer and CXCR4 ligand, [68Ga]NOTA-R-54, was developed and tested for potential use in the treatment of lung cancer.
Frontier Medicines Corp. has unveiled FMC-242 as its newest development candidate. FMC-242 is a covalent allosteric inhibitor that breaks the interaction between PI3Kα and RAS proteins to inhibit downstream effector signaling in tumors without impacting normal functions and while minimizing the toxicities commonly associated with the broader class of inhibitors.
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