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CXCR4-Targeted Library

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ChemDiv’s library of small molecule compounds targeting CXCR4 comprises 8,899 entries.

CXCR4, or C-X-C chemokine receptor type 4, is a G protein-coupled receptor (GPCR) that plays a critical role in various physiological processes through its interaction with its ligand, CXCL12 (stromal cell-derived factor 1, SDF-1). This receptor-ligand pair is essential for hematopoiesis, vascular formation, and the homing and trafficking of stem cells and immune cells within the body. CXCR4's functions extend to the development of the cardiovascular, nervous, and immune systems, making it a key player in both normal physiology and pathological conditions.

The aberrant expression or function of CXCR4 has been implicated in the development and progression of several diseases. In cancer, CXCR4 is often overexpressed in tumor cells, facilitating metastasis through its role in cell migration and invasion. Tumor cells exploit the CXCR4-CXCL12 axis to migrate towards organs with high CXCL12 expression, contributing to the establishment of secondary tumor sites. This receptor is also involved in the pathogenesis of HIV/AIDS, serving as a coreceptor for the entry of the virus into host cells. In addition to its role in cancer and infectious diseases, CXCR4 dysregulation has been associated with autoimmune diseases and cardiovascular disorders. The receptor's involvement in stem cell mobilization and immune response regulation makes it a target of interest for therapeutic intervention, with inhibitors of CXCR4 being explored for their potential to block tumor metastasis, prevent HIV infection, and modulate immune and inflammatory responses.

Compounds targeting CXCR4 play a pivotal role in drug discovery by offering therapeutic strategies for a wide range of diseases, including cancer, HIV/AIDS, hematological conditions, and autoimmune diseases. By specifically inhibiting or modulating the CXCR4/CXCL12 signaling axis, these compounds can interfere with the pathological processes in which CXCR4 is implicated, providing several benefits in therapeutic applications:

-       Cancer Therapy: CXCR4 is extensively involved in tumor progression, metastasis, and resistance to therapy. Compounds targeting CXCR4 can potentially inhibit the migration and invasion of cancer cells to distant organs, thereby reducing metastasis. Furthermore, by disrupting the CXCR4/CXCL12 axis, these compounds can sensitize tumor cells to chemotherapy and targeted therapies, overcoming drug resistance and improving treatment outcomes.

-       HIV/AIDS Treatment: CXCR4 serves as a coreceptor for the entry of certain strains of HIV into host cells. Inhibitors targeting CXCR4 can block HIV entry, providing a mechanism for controlling HIV infection and preventing the progression to AIDS. This approach can be particularly beneficial in cases where the virus uses CXCR4 preferentially or exclusively for entry, complementing existing antiretroviral therapies that target other aspects of the HIV life cycle.

-       Hematological Conditions and Stem Cell Mobilization: The CXCR4/CXCL12 interaction is crucial for the homing and retention of hematopoietic stem cells in bone marrow. By blocking CXCR4, compounds can mobilize stem cells into the peripheral blood, facilitating their collection for stem cell transplantation procedures. This is particularly valuable in the treatment of hematological malignancies and in regenerative medicine.

-       Immunomodulation: Given CXCR4's role in immune cell trafficking and inflammation, targeting this receptor can modulate immune responses. This property is promising for treating autoimmune diseases and reducing inflammatory responses, potentially leading to new treatments for conditions where current options are limited or ineffective.


Our library of CXCR4-targeted small molecule compounds represents a highly valuable resource for drug discovery, offering a focused collection of compounds designed to specifically interact with the CXCR4 receptor, a critical player in various pathological conditions including cancer, HIV/AIDS, and immune disorders. This targeted approach enables researchers to efficiently identify and optimize potent CXCR4 inhibitors or modulators, accelerating the development of novel therapeutics. The benefits of such a library include the potential to disrupt the CXCR4/CXCL12 signaling axis, thereby inhibiting tumor metastasis, preventing HIV entry into cells, mobilizing stem cells, and modulating immune responses. By providing a diverse array of compounds with the specificity to target CXCR4, the library facilitates the exploration of new treatment avenues, enhances the likelihood of discovering effective drug candidates, and ultimately contributes to the development of targeted therapies with improved efficacy and safety profiles for diseases with significant unmet medical needs.

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