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Targefrin is a Potent EphA2 Antagonist with Antitumor Activity

Louis Gilman December 7, 2022

EphA2, a transmembrane glycoprotein, is a type of Ephrin receptors (Eph) which is the most important class of receptor tyrosine kinases. EphA2 can be detected in most epithelial cells. In common…

Cancer Lung Cancer Pancreas Cancer

Reversin 121, a P-glycoprotein Inhibitor, Reverses P-glycoprotein-Mediated Multidrug Resistance

Louis Gilman December 1, 2022

Nowadays, how to overcome the resistance of tumor cells to multiple drugs is still a serious problem. Various mechanisms can cause Multidrug resistance (MDR), including cell cycle alterations, increased repair…

Colorectal Cancer Lung Cancer Non-Small Cell Lung Cancer Pancreas Cancer

G12Si-5 is a K-Ras G12S Mutant Covalent Inhibitor

Louis Gilman September 20, 2022

KRAS (Kirsten rat sarcoma virus) is one of the most commonly altered oncogenes in human cancers. Recurrent oncogenic mutations in KRAS can reprogram glutamine metabolism to increase the production of…

Pancreas Cancer

Certepetide is a Tumor-penetrating Enhancer via RGD Motif Interaction with Alphav-integrins

Louis Gilman September 1, 2022

αV integrin is a protein that is encoded by the ITGAV gene. Studies show the participation of αV integrins in the proliferation, motility and proteolysis of various cancer cells. Neuropilin-1…

Cancer Multiple Myeloma Pancreas Cancer

Panobinostat is a Potent and Orally Active Non-selective HDAC Inhibitor

Louis Gilman July 30, 2022

HDACs (Histone deacetylases) are a class of enzymes that remove acetyl groups from an ε-N-acetyl lysine amino acid on a histone, allowing the histones to wrap the DNA more tightly.…

Pancreas Cancer

FH535 is a Potent Inhibitor of Wnt/β-catenin and PPAR

Louis Gilman April 3, 2022

The Wnt signaling pathway is important in normal development and in cancer. This signaling pathway is regulated by Wnt ligands, the APC-Axin complex and β-catenin. Wnt/β-catenin signaling pathway plays a…

Breast Cancer Pancreas Cancer

PX-12 is an Irreversible Inhibitor of Thioredoxin-1 (Trx-1)

Louis Gilman March 15, 2022

Colorectal cancer is one of the leading causes of cancer-related mortality in most industrialized nations. It needs to find an effective adjuvant therapy for colorectal cancer. There includes non-steroidal anti-inflammatory…

Pancreas Cancer

IACS-15414 is an Orally Active SHP2 Inhibitor

Louis Gilman January 31, 2022

Src-homology-2-containing protein tyrosine phosphatase 2 (SHP2), encoded by the PTPN11 gene, is a classical nonreceptor protein tyrosine phosphatase (PTP). SHP2 is a ubiquitous protein tyrosine phosphatase with a relatively conserved…

Head and Neck Cancer Melanoma Pancreas Cancer

β-Lapachone, a Naturally Occurring O-naphthoquinone, is a Topoisomerase I Inhibitor

Louis Gilman January 15, 2022

β-Lapachone is an ortho-naphthoquinone and inhibits topoisomerase I. β-Lapachone is a classic quinone-containing antitumor NQO1-bioactivatable drug that directly kills NQO1-overexpressing cancer cells. NQO1 is an antioxidative enzyme that helps recover…

Pancreas Cancer

Troglitazone is an Orally Active PPARγ Agonist

Louis Gilman November 30, 2021

Pancreatic cancer is the fourth leading cause of cancer-related deaths in Japan. Gemcitabine has been the standard therapy for advanced pancreatic cancer for over a decade. Additional novel combination therapies…

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BI 7446 is a STING Agonist for Immuno-oncology Research

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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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