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Reliable, unbiased and up to date information in cancer research

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Reliable, unbiased and up to date information in cancer research

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Endometrial Cancer Uterine Serous Carcinoma

Alobresib is an Orally Active BET Bromodomain Inhibitor for Uterine Serous Carcinoma Treatment

Louis Gilman July 31, 2019

Uterine serous carcinoma is a rare and highly aggressive variant of endometrial cancer. Uterine serous carcinoma accounts for 10% of all endometrial cancer; however, it carries the poorest prognosis, with…

Chronic Lymphocytic Leukemia

MT-802 is a PROTAC Degrader of BTK for C481S Mutant CLL Treatment

Louis Gilman July 30, 2019

The irreversible inhibitor Ibrutinib for Bruton’s tyrosine kinase (BTK) has emerged as a transformative treatment option for patients with chronic lymphocytic leukemia (CLL) and other B-cell malignancies. However, more than…

Cancer

GSK3368715 is an Orally Active Type I PRMT Inhibitor

Louis Gilman July 29, 2019

GSK3368715 is an orally active type I PRMT inhibitor. Protein arginine methyltransferases (PRMTs) transfer a methyl group from S-adenosyl-L-methionine (SAM) to the substrate arginine side chain. All PRMTs can generate…

Cancer

MBM-55 is a Potent Nek2 Inhibitor for Cancer Therapy

Louis Gilman July 28, 2019

NIMA-related kinase 2 (Nek2) is a serine/threonine kinase. It serves as a key regulator of mitotic processes such as centrosome duplication and spindle assembly. Deregulation of mitotic processes can lead…

Gastric Adenocarcinoma

APG-115, an Orally Active MDM2 Inhibitor, Induces Cell-Cycle Arrest and Apoptosis in a p53-Dependent Manner

Louis Gilman July 27, 2019

The essential all human cancers compromises the tumor suppressor function of p53. In about half of human cancers, TP53, the gene encoding p53 protein, is mutated or deleted. This inactivates the…

Leukemia

M-89, a Specific Menin inhibitor, Has Potential to Treat MLL Leukemia

Louis Gilman July 26, 2019

Mixed lineage leukemia (MLL) protein is a histone methyltransferase and specifically methylates histone H3 lysine 4 residue (H3K4). MLL gene rearrangement accounts 5-10% in acute myeloid leukemia in adults and…

Cancer

GSK2643943A is a Novel DUB Inhibitor

Louis Gilman July 25, 2019

The ubiquitin proteasome system participates in a variety of biological functions including cell cycle progression, intracellular signaling and protein degradation. Therefore, it is not surprising to find many misregulation of…

Pancreas Cancer

FGTI-2734, a Dual FTase and GGTase Inhibitor, Has Potential to Treat KRAS-mutant Cancer

Louis Gilman July 24, 2019

The KRAS gene belongs to a class of genes known as oncogenes. When mutated, oncogenes have the potential to cause normal cells to become cancerous. The KRAS gene is in…

Melanoma

SAR-260301 is an Orally Active PI3Kβ Inhibitor for Melanoma Treatment

Louis Gilman July 23, 2019

The phosphoinositide 3-kinase (PI3K) pathway activation plays a major role in cancer. The PI3K-AKT pathway is one of the most important signaling networks in cancer. Activation of PI3K-AKT pathway plays…

Acute Lymphoblastic Leukemia

dBET6, an Orally Active PROTAC Degrader of BET, Has Potential to Treat ALL

Louis Gilman July 22, 2019

Development of drugs based on PROTAC is not new to us. We have mentioned the technology many times in our blogs. PROTAC is used to move the unwanted proteins to…

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  • INCB086550 is an Orally Active PD-L1 Inhibitor for Multiple Cancers Research
  • Panobinostat is a HDAC Inhibitor for Multiple Myeloma Research

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You Missed

Breast Cancer

BI 7446 is a STING Agonist for Immuno-oncology Research

Gastric Cancer Obesity

JNJ-38877605 is an Orally Active c-Met Inhibitor for Solid Tumour Research

Multiple Myeloma Myeloma

OATD-02 is an Orally Active Arginase 1/2 Inhibitor for Melanoma Research

autoimmune disease

INCB086550 is an Orally Active PD-L1 Inhibitor for Multiple Cancers Research

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