7t3f

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Development of BRD4 inhibitors as arsenicals antidotes

Structural highlights

7t3f is a 1 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Method:X-ray diffraction, Resolution 1.28Å
Ligands:EM0, GOL
Resources:FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Disease

BRD4_HUMAN Note=A chromosomal aberration involving BRD4 is found in a rare, aggressive, and lethal carcinoma arising in midline organs of young people. Translocation t(15;19)(q14;p13) with NUT which produces a BRD4-NUT fusion protein.[1] [2]

Function

BRD4_HUMAN Plays a role in a process governing chromosomal dynamics during mitosis (By similarity).

Publication Abstract from PubMed

Arsenicals belong to the class of chemical warfare agents known as vesicants, which are highly reactive, toxic and cause robust inflammatory response. Cutaneous exposure to arsenicals causes a wide range of systemic organ damage, beginning with cutaneous injuries, and later manifest multi-organ damage and death. Thus, the development of suitable antidotes that can effectively block injury following exposure to these agents is of great importance. Bromodomain 4 (BRD4), a member of the bromodomain and extra terminal domain (BET) family, plays crucial role in regulating transcription of inflammatory, proliferation and cell cycle genes. In this context, the development of potent small molecule inhibitors of BRD4 could serve as potential antidotes for arsenicals. Herein, we describe the synthesis and biological evaluation of a series of compounds.

Development of BRD4 inhibitors as anti-inflammatory agents and antidotes for arsenicals.,Yatchang MF, Mathew B, Srivastava RK, Khan J, Muzaffar S, Zhang S, Wu M, Zhai L, Ruiz P, Agarwal A, Bostwick JR, Suto MJ, Athar M, Augelli-Szafran CE Bioorg Med Chem Lett. 2022 May 15;64:128696. doi: 10.1016/j.bmcl.2022.128696., Epub 2022 Mar 19. PMID:35318165[3]

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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See Also

References

  1. ↑ French CA, Miyoshi I, Kubonishi I, Grier HE, Perez-Atayde AR, Fletcher JA. BRD4-NUT fusion oncogene: a novel mechanism in aggressive carcinoma. Cancer Res. 2003 Jan 15;63(2):304-7. PMID:12543779
  2. ↑ French CA, Miyoshi I, Aster JC, Kubonishi I, Kroll TG, Dal Cin P, Vargas SO, Perez-Atayde AR, Fletcher JA. BRD4 bromodomain gene rearrangement in aggressive carcinoma with translocation t(15;19). Am J Pathol. 2001 Dec;159(6):1987-92. PMID:11733348 doi:10.1016/S0002-9440(10)63049-0
  3. ↑ Yatchang MF, Mathew B, Srivastava RK, Khan J, Muzaffar S, Zhang S, Wu M, Zhai L, Ruiz P, Agarwal A, Bostwick JR, Suto MJ, Athar M, Augelli-Szafran CE. Development of BRD4 inhibitors as anti-inflammatory agents and antidotes for arsenicals. Bioorg Med Chem Lett. 2022 May 15;64:128696. doi: 10.1016/j.bmcl.2022.128696., Epub 2022 Mar 19. PMID:35318165 doi:http://dx.doi.org/10.1016/j.bmcl.2022.128696

Contents


PDB ID 7t3f

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OCA

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