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MMRi62, a Ferroptosis Inducer Targeting MDM2-MDM4

Louis Gilman December 28, 2022

MDM2 and MDM4 have established cancer drug targets. Additionally, they are also inhibitors of p53 activity and are amplified in many cancer types. In particular, the targeting of MDM2–p53 interactions…

Breast Cancer Lymphoma

MD-222 is a First-in-Class Highly Potent PROTAC Degrader of MDM2

Louis Gilman May 14, 2021

PROTACs are heterobifunctional molecules that connect a POI ligand to an E3 ubiquitin ligase recruiting ligand with an optimal linker. Researchers reported the discovery of MD-222. MD-222 is the first-in-class…

Acute Myeloid Leukemia Glioma

A-674563 is an Orally Active and Selective Akt1 Inhibitor

Louis Gilman May 5, 2021

Akt1 belongs to the Akt subfamily of serine/threonine kinases, which contains the SH2 (SRC homologous 2-like) domain. Specifically, Akt kinase is the central node of the signal transduction pathway, which…

Osteosarcoma

HLI373 is an Efficacious Hdm2 Inhibitor, with Antimalarial Activity

Louis Gilman July 4, 2020

Hdm2 is an ubiquitin-protein ligase. Hdm2 suppresses the transcriptional activity of the tumor suppressor p53 and promotes its degradation. HLI373 is an efficacious Hdm2 inhibitor. HLI373 is effective in inducing…

Leukemia

CMLD010509 is a Highly Specific Inhibitor of the Oncogenic MYC-Driven Translation Program

Louis Gilman December 10, 2019

Multiple myelomas (MM) is a hematological malignancy, it exhibits a clonal proliferation of plasma cells in the bone marrow micro-environment. MM remains a frequently incurable hematological malignancy until today. MYC…

Leukemia PROTAC

MD-224 is a First-in-Class and Highly Potent PROTAC Degrader of MDM2

Louis Gilman September 10, 2019

As previously introduced, the tumor suppressor p53 plays a critical role in the prevention of tumor development. While human, murine double minute 2 (MDM2) protein is a primary endogenous cellular…

Cancer

MI-1061 is an Orally Active MDM2 Inhibitor

Louis Gilman September 4, 2019

Inhibition of the MDM2-p53 protein-protein interaction is being actively pursued as a new anticancer therapeutic strategy. Our previous blogs have introduced typical MDM2 or MDM2-p53 inhibitors, including MI-773, RG7112, and…

Hematologic Neoplasms Leukemia Neoplasms Sarcoma Soft Tissue Tumor

RG7112 is the First Clinical and Orally Active MDM2-p53 Inhibitor

Louis Gilman August 28, 2019

Yesterday, I introduced AMG 232 as a potent, selective and orally available inhibitor of p53-MDM2 interaction. Additionally, we have known the significance of MDM2-p53 interaction in cancer development. Today, I’d…

Cancer

BI-0252 is an Orally Active Inhibitor of the MDM2-p53 Interaction

Louis Gilman August 2, 2019

The tumor protein p53 is a pivotal tumor suppressor protein and a mainstay of the body’s cellular anti-cancer defense system. As a potent transcription factor, TP53 regulates multiple downstream target…

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…

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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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