Hematopoietic progenitor kinase 1 (HPK1) plays a relevant role in regulating T-cell, B-cell and dendritic cell function. As its inactivation both in vitro and in vivo contributes to tumor growth inhibition, HPK1 is considered a therapeutic target to explore in cancer immunotherapy.
Itheos Therapeutics Inc. recently presented the discovery of a first-in-class, potent and selective ENT1 inhibitor, EOS-984 (EOS-301984), for the treatment of solid tumors. Immune checkpoint inhibitors (ICIs) have become essential in treating solid tumors, but only a limited number of patients currently benefit from approved ICIs.
Aging is part of the life cycle and, although the effects are not manifest until after adulthood, it actually occurs from birth. The concept of senescence has traditionally been associated with aging. However, an embryo has senescent cells. In that case, what is aging, how can it be measured, and from what point in the life cycle?
Since the publication of The Hallmarks of Aging in 2013, aging research has exploded. The field now has more than 300,000 articles on the biological signals of the effect of time on the body. What would Marty McFly, the legendary character from the Back to the Future saga who traveled with his DeLorean time machine from the ‘80s to the ‘50s, think if he visited 2024 and saw laboratories experimenting with techniques to turn back the biological clocks of cells or increase the lifespan of rejuvenated mice?
Arcus Biosciences Inc. recently disclosed the chemical structure of AB-521 (casdatifan), an orally available small-molecule inhibitor of hypoxia-inducible factor 2α (HIF-2α) in early clinical development for the treatment of advanced solid tumors with a high prevalence of molecular alterations associated with pseudohypoxia, such as clear cell renal cell carcinoma (ccRCC).
Gilead Sciences Inc. recently disclosed details on the work that led to the discovery of elunonavir (GS-1156), an unboosted HIV protease inhibitor currently in phase I studies.
At the recently concluded ACS Fall meeting, Bristol Myers Squibb Co. reported the discovery of potent orally bioavailable B-cell lymphoma 6 protein (BCL6) ligand-directed degraders (LDDs).
In a presentation at the American Chemical Society meeting, Halda Therapeutics Inc. described its androgen receptor (AR)-targeting RIPTAC (regulated induced proximity targeting chimera) therapeutics as a new class of heterofunctional small molecules designed to selectively kill cancer cells that express tumor-specific targeting protein (TIP) into a stable intracellular ternary complex with a protein essential for cell survival for the treatment of prostate cancer.
Both casein kinase 1α (CK1α) and zinc finger protein Helios (IKZF2) are among the targets most recently evaluated for the treatment of acute myeloid leukemia (AML). A growing number of molecules against these targets acting as degraders or inhibitors are actively being investigated.
At the ongoing meeting of the American Chemical Society in Denver, F. Hoffmann-La Roche Ltd. has reported the discovery of an orally available and brain-penetrant irreversible asparagine-specific endopeptidase (AEP) inhibitor, RO-7542742, for the potential treatment of neurodegenerative diseases.
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