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4lr6

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Revision as of 08:35, 20 January 2015

Structure of BRD4 bromodomain 1 with a 3-methyl-4-phenylisoxazol-5-amine fragment

Structural highlights

4lr6 is a 1 chain structure with sequence from Human. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Ligands:	,
Related:	4lrg
Gene:	BRD4, BRD4_HUMAN, HUNK1 (HUMAN)
Resources:	FirstGlance, OCA, RCSB, PDBsum

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

The identification of a novel series of small molecule BET inhibitors is described. Using crystallographic binding modes of an amino-isoxazole fragment and known BET inhibitors, a structure-based drug design effort lead to a novel isoxazole azepine scaffold. This scaffold showed good potency in biochemical and cellular assays and oral activity in an in vivo model of BET inhibition.

Discovery, Design, and Optimization of Isoxazole Azepine BET Inhibitors.,Gehling VS, Hewitt MC, Vaswani RG, Leblanc Y, Cote A, Nasveschuk CG, Taylor AM, Harmange JC, Audia JE, Pardo E, Joshi S, Sandy P, Mertz JA, Sims RJ 3rd, Bergeron L, Bryant BM, Bellon S, Poy F, Jayaram H, Sankaranarayanan R, Yellapantula S, Bangalore Srinivasamurthy N, Birudukota S, Albrecht BK ACS Med Chem Lett. 2013 Jul 16;4(9):835-40. doi: 10.1021/ml4001485. eCollection, 2013 Sep 12. PMID:24900758^[3]

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

References

↑ 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
↑ 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
↑ Gehling VS, Hewitt MC, Vaswani RG, Leblanc Y, Cote A, Nasveschuk CG, Taylor AM, Harmange JC, Audia JE, Pardo E, Joshi S, Sandy P, Mertz JA, Sims RJ 3rd, Bergeron L, Bryant BM, Bellon S, Poy F, Jayaram H, Sankaranarayanan R, Yellapantula S, Bangalore Srinivasamurthy N, Birudukota S, Albrecht BK. Discovery, Design, and Optimization of Isoxazole Azepine BET Inhibitors. ACS Med Chem Lett. 2013 Jul 16;4(9):835-40. doi: 10.1021/ml4001485. eCollection, 2013 Sep 12. PMID:24900758 doi:http://dx.doi.org/10.1021/ml4001485

1 Structural highlights
2 Disease
3 Function
4 Publication Abstract from PubMed
5 References

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/4lr6"

@@ Line 25: / Line 25: @@
 </StructureSection>
 [[Category: Human]]
-[[Category: Albrecht, B.]]
+[[Category: Albrecht, B]]
-[[Category: Audia, J.]]
+[[Category: Audia, J]]
-[[Category: Bellon, S.]]
+[[Category: Bellon, S]]
-[[Category: Bergeron, L.]]
+[[Category: Bergeron, L]]
-[[Category: Birudukota, S.]]
+[[Category: Birudukota, S]]
-[[Category: Bryant, B.]]
+[[Category: Bryant, B]]
-[[Category: Cote, A.]]
+[[Category: Cote, A]]
-[[Category: Gehling, V.]]
+[[Category: Gehling, V]]
-[[Category: Harmange, J C.]]
+[[Category: Harmange, J C]]
-[[Category: Hewitt, M.]]
+[[Category: Hewitt, M]]
-[[Category: Jayaram, H.]]
+[[Category: Jayaram, H]]
-[[Category: Joshi, S.]]
+[[Category: Joshi, S]]
-[[Category: Leblanc, Y.]]
+[[Category: Leblanc, Y]]
-[[Category: Mertz, J.]]
+[[Category: Mertz, J]]
-[[Category: Nandana, B S.]]
+[[Category: Nandana, B S]]
-[[Category: Nasveschuk, C.]]
+[[Category: Nasveschuk, C]]
-[[Category: Pardo, E.]]
+[[Category: Pardo, E]]
-[[Category: Poy, F.]]
+[[Category: Poy, F]]
-[[Category: Ravichandran, S.]]
+[[Category: Ravichandran, S]]
-[[Category: Sandy, P.]]
+[[Category: Sandy, P]]
-[[Category: Sims, R.]]
+[[Category: Sims, R]]
-[[Category: Taylor, A.]]
+[[Category: Taylor, A]]
-[[Category: Vaswani, R.]]
+[[Category: Vaswani, R]]
-[[Category: Yellapuntala, S.]]
+[[Category: Yellapuntala, S]]
 [[Category: Bet inhibitor]]
 [[Category: Brd4 first bromodomain]]
 [[Category: Transcription regulator-inhibitor complex]]

4lr6

From Proteopedia

Revision as of 08:35, 20 January 2015

Structure of BRD4 bromodomain 1 with a 3-methyl-4-phenylisoxazol-5-amine fragment

Structural highlights

Disease

Function

Publication Abstract from PubMed

References

Contents

Proteopedia Page Contributors and Editors (what is this?)

Views

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