Discovery of Small Molecule CXCR4 Antagonists (Record no. 44932)
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| 000 -LEADER | |
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| fixed length control field | 01842nam a2200241Ia 4500 |
| 003 - CONTROL NUMBER IDENTIFIER | |
| control field | MX-MdCICY |
| 005 - DATE AND TIME OF LATEST TRANSACTION | |
| control field | 20250625140636.0 |
| 040 ## - CATALOGING SOURCE | |
| Transcribing agency | CICY |
| 090 ## - LOCALLY ASSIGNED LC-TYPE CALL NUMBER (OCLC); LOCAL CALL NUMBER (RLIN) | |
| Classification number (OCLC) (R) ; Classification number, CALL (RLIN) (NR) | B-10700 |
| 008 - FIXED-LENGTH DATA ELEMENTS--GENERAL INFORMATION | |
| fixed length control field | 250602s9999 xx |||||s2 |||| ||und|d |
| 245 10 - TITLE STATEMENT | |
| Title | Discovery of Small Molecule CXCR4 Antagonists |
| 490 0# - SERIES STATEMENT | |
| Volume/sequential designation | Journal of Medicinal Chemistry, 50(23), p.5655-5664, 2007 |
| 520 3# - SUMMARY, ETC. | |
| Summary, etc. | In light of a proposed molecular mechanism for the C-X-C chemokine receptor type 4 (CXCR4)antagonist 1 (AMD3100), a template with the general structure 2 was designed, and 15 was identified as a lead by means of an affinity binding assay against the ligand-mimicking CXCR4 antagonist 3 (TN14003). Following a structure-activity profile around 15, the design and synthesis of a series of novel small molecular CXCR4 antagonists led to the discovery of 32 (WZ811). The compound shows subnanomolar potency (EC50 ) 0.3 nM)in an affinity binding assay. In addition, when subjected to in Vitro functional evaluation, 32 efficiently inhibits CXCR4/stromal cell-derived factor-1 (SDF-1)-mediated modulation of cyclic adenosine monophophate (cAMP)levels (EC50 ) 1.2 nM)and SDF-1 induced Matrigel invasion (EC50 ) 5.2 nM). Molecular field topology analysis (MFTA), a 2D quantitative structure-activity relationship (QSAR)approach based on local molecular properties (Van der Waals radii (VdW), atomic charges, and local lipophilicity), applied to the 32 series suggests structural modifications to improve potency. |
| 700 12 - ADDED ENTRY--PERSONAL NAME | |
| Personal name | Zhan, W. |
| 700 12 - ADDED ENTRY--PERSONAL NAME | |
| Personal name | Liang, Z. |
| 700 12 - ADDED ENTRY--PERSONAL NAME | |
| Personal name | Zhu, A. |
| 700 12 - ADDED ENTRY--PERSONAL NAME | |
| Personal name | Kurtkaya, S. |
| 700 12 - ADDED ENTRY--PERSONAL NAME | |
| Personal name | Shim, H. |
| 700 12 - ADDED ENTRY--PERSONAL NAME | |
| Personal name | Snyder, J.P. |
| 700 12 - ADDED ENTRY--PERSONAL NAME | |
| Personal name | Liotta, D.C. |
| 856 40 - ELECTRONIC LOCATION AND ACCESS | |
| Uniform Resource Identifier | <a href="https://drive.google.com/file/d/1KjUfesWkU1mc3_CgGgIdZciI9PMx0fz9/view?usp=drivesdk">https://drive.google.com/file/d/1KjUfesWkU1mc3_CgGgIdZciI9PMx0fz9/view?usp=drivesdk</a> |
| Public note | Para ver el documento ingresa a Google con tu cuenta: @cicy.edu.mx |
| 942 ## - ADDED ENTRY ELEMENTS (KOHA) | |
| Source of classification or shelving scheme | Clasificación local |
| Koha item type | Documentos solicitados |
| Lost status | Source of classification or shelving scheme | Damaged status | Not for loan | Collection | Home library | Current library | Shelving location | Date acquired | Total checkouts | Full call number | Date last seen | Price effective from | Koha item type |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Clasificación local | Ref1 | CICY | CICY | Documento préstamo interbibliotecario | 25.06.2025 | B-10700 | 25.06.2025 | 25.06.2025 | Documentos solicitados |