Category: Breast Cancer

Senaparib is a Selective and Orally Active PARP1/2 Inhibitor

Poly(ADP-ribose) polymerase (PARP) is an important protein in DNA repair pathways especially the base excision repair. . PARP proteins compose of two ribose moieties and two phosphates per unit polymer. PARP inhibitors represent a successful example of precision medicine as the first drugs targeting DNA damage response to have...

AZ9482 is a Triple PARP1/2/6 Inhibitor

PARPs are implicated in a variety of cellular metabolic processes including DNA-damage repair and mitotic spindle formation. In particular, PARP1 is essential in repairing DNA single- and double-strand breaks. For example, PARP1 Inhibitor Olaparib is an effective synthetic lethal strategy in cancer. Recently, scientists reported a triple PARP1/2/6 inhibitor,...

PND-1186 is a Highly-Specific FAK Inhibitor and Induces Apoptosis

Focal adhesion kinase (FAK) is a tyrosine kinase overexpressed in cancer cells. Especially, FAK plays an important role in the progression of tumors to a malignant phenotype. FAK associates with integrins and modulates various cellular processes including growth, survival, and migration. In particular, PND-1186 is a substituted pyridine reversible...

ADPM06 is a Novel Nonporphyrin Photodynamic Therapeutic (PDT) Sensitizer and Induces Apoptosis

Photodynamic therapeutic (PDT) is an established treatment modality for cancer. It utilizes a photosensitive compound accompanied by low-energy light of a specific wavelength. The combination of these two independently nontoxic components produces extensive cellular, vascular, and tissue damage in an oxygen-dependent manner, via reactive oxygen species (ROS) generation, resulting in...

H3B-6545 is an Orally Active and Selective ER Covalent Antagonist (SERCA)

Breast cancer is the second leading cause of cancer mortality among women worldwide. Estrogen receptor alpha (ERα) is a key hormone-regulated transcription factor for normal and malignant breast cells. Moreover, tumors that are ER-positive are much more likely to respond to treatments that block estrogen in ER-positive/HER2 negative breast...

Giredestrant is an Orally Active and Selective ER Antagonist

Estrogen receptor (ERs) is a group of proteins found in cells and is activated by estrogen. Specifically, ERs are typical members of the nuclear receptor superfamily, including receptors that mediate steroid hormones, thyroid hormones, vitamin A and vitamin D, and many orphan receptors. Besides, once ER is activated, estrogen...

AZD-9833 is an Orally Active Estrogen Receptor (ER) Antagonist

Estrogens participate in numerous physiological processes such as cell growth, reproduction, and differentiation. In females, the ovaries are the major site of estrogen synthesis producing the predominant estrogen 17b-estradiol (E2). In addition to effects by E2 on normal physiology, estrogens also play an important role in several pathological processes...