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Reliable, unbiased and up to date information in cancer research

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Colon Cancer

COH000 is an Allosteric, Covalent and Irreversible Inhibitor of SUMO-Activating Enzyme

Louis Gilman April 8, 2019

Aberrations in post-translational modifications by ubiquitin or ubiquitin-like proteins (Ubl), such as the small ubiquitin-like modifiers (SUMO) relate to the pathogenesis of lifethreatening diseases, such as cancer, neurodegenerative disorders, and…

Prostate Cancer

A Cyclin G-associated kinase (GAK) Inhibitor SGC-GAK-1

Louis Gilman April 7, 2019

Cyclin G-associated kinase (GAK) is a 160 kDa serine/threonine kinase. Importantly, GAK features high homology outside its kinase domain with auxilin. GAK regulates receptor tyrosine kinases, such as the EGF…

Breast Cancer PROTAC

A Lead PROTAC BRD9 Chemical Degrader

Louis Gilman April 6, 2019

The bromodomain-containing protein BRD9, a recently identified mSWI/SNF subunit, is a novel complex configuration distinct from BAF and PBAF. The mSWI/SNF (BAF) complex comprises at least 15 subunits of ~2…

Cancer

BR351 is a Brain Penetrant MMP Inhibitor

Louis Gilman April 5, 2019

Matrix metalloproteinases (MMPs) are a family of zinc- and calcium-dependent endopeptidases. They are responsible for the degradation of most extracellular matrix proteins during organogenesis, growth and normal tissue turnover. Elevated…

Gastrointestinal Stromal Tumor

AZD3229 is a Potent Pan-KIT Mutant Inhibitor

Louis Gilman April 4, 2019

Gastrointestinal stromal tumors (GISTs) are the most common mesenchymal neoplasms of the gastrointestinal tract. While the application of targeted tyrosine kinase inhibitors has revolutionized the treatment of gastrointestinal stromal tumors…

Breast Cancer

H3B-5942, a Selective Estrogen Receptor Covalent Antagonist for ERα Breast Cancer Treatment

Louis Gilman April 3, 2019

  Estrogen receptor is a nuclear receptor activated by estrogen, existing inside cells. The receptor contains two types, ERα and ERβ. The former is always expressed in breast cancer, which…

Lung Cancer

CCB02, a Tubulin Binder Inhibits Cancer Cells with Extra Centrosomes

Louis Gilman April 2, 2019

Centrosome is an important organelle. It acts as the main microtubule organizing center (MTOC), regulates cell-cycle progression in mammalian cells. In normal cells, centrosome duplication occurs in the early phase…

Acute Lymphoblastic Leukemia Acute Myeloid Leukemia

Optimization of HJB97 for The Design of PROTAC Degraders of BET Proteins

Louis Gilman April 1, 2019

The Bromodomain and Extra-Terminal Domain (BET) family of proteins comprises BRD2, BRD3, BRD4, and BRDT. The BET proteins are epigenetic readers and play a key role in the regulation of…

Acute Leukemia Breast Cancer

CF53, a Potent and Orally Active BET Inhibitor

Louis Gilman March 31, 2019

Bromodomain and extra-terminal (BET) family is a well-known member of bromodomain family. Proteins of this family include BRD2, BRD3, BRD4 and a testis-specific protein, BRDT. BET proteins act as important…

Pancreas Cancer

A Novel and Efficacious RAF Inhibitor RAF709

Louis Gilman March 30, 2019

The mitogen-activated protein kinase pathway regulates lots of multiple biological functions. In addition, RAF inhibitors activate the MAPK pathway. Interestingly, the MAPK pathway in turn induces the RAS proteins to…

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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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