OCA at 12:11, 30 October 2024

2024-10-30T12:11:40Z

← Older revision		Revision as of 12:11, 30 October 2024
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	==~~n/a~~==		==Crystal structure of monkey TLR7 ectodomain with compound 5==
	<StructureSection load='8tty' size='340' side='right'caption='[[8tty]]' scene=''>		<StructureSection load='8tty' size='340' side='right'caption='[[8tty]], [[Resolution\|resolution]] 2.10Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=8TTY OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=8TTY FirstGlance]. <br>		<table><tr><td colspan='2'>[[8tty]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Macaca_mulatta Macaca mulatta]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=8TTY OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=8TTY FirstGlance]. <br>
	</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models\|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction</td></tr>		</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models\|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution\|Resolution]] 2.101Å</td></tr>
			<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=BMA:BETA-D-MANNOSE'>BMA</scene>, <scene name='pdbligand=NAG:N-ACETYL-D-GLUCOSAMINE'>NAG</scene>, <scene name='pdbligand=QEC:N~7~-butyl-2-({4-[(cyclobutylamino)methyl]-2-methoxyphenyl}methyl)-2H-pyrazolo[4,3-d]pyrimidine-5,7-diamine'>QEC</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr>
	<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=8tty FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=8tty OCA], [https://pdbe.org/8tty PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=8tty RCSB], [https://www.ebi.ac.uk/pdbsum/8tty PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=8tty ProSAT]</span></td></tr>		<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=8tty FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=8tty OCA], [https://pdbe.org/8tty PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=8tty RCSB], [https://www.ebi.ac.uk/pdbsum/8tty PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=8tty ProSAT]</span></td></tr>
	</table>		</table>
			== Function ==
			[https://www.uniprot.org/uniprot/B3Y653_MACMU B3Y653_MACMU]
			<div style="background-color:#fffaf0;">
			== Publication Abstract from PubMed ==
			We have designed and developed novel and selective TLR7 agonists that exhibited potent receptor activity in a cell-based reporter assay. In vitro, these agonists significantly induced secretion of cytokines IL-6, IL-1beta, IL-10, TNFa, IFNa, and IP-10 in human and mouse whole blood. Pharmacokinetic and pharmacodynamic studies in mice showed a significant secretion of IFNalpha and TNFalpha cytokines. When combined with aPD1 in a CT-26 tumor model, the lead compound showed strong synergistic antitumor activity with complete tumor regression in 8/10 mice dosed using the intravenous route. Structure-activity relationship studies enabled by structure-based designs of TLR7 agonists are disclosed.

			Discovery of Novel TLR7 Agonists as Systemic Agent for Combination With aPD1 for Use in Immuno-oncology.,Poudel YB, He L, Cox M, Zhang Q, Johnson WL, Cong Q, Cheng H, Chowdari NS, Tarby C, Donnell AF, Broekema M, O'Malley DP, Zhang Y, A M Subbaiah M, Kumar BV, Subramani L, Wang B, Li YX, Sivaprakasam P, Critton D, Mulligan D, Sandhu B, Xie C, Ramakrishnan R, Nagar J, Dudhgaonkar S, Oderinde MS, Murtaza A, Schieven GL, Mathur A, Gavai AV, Vite G, Gangwar S ACS Med Chem Lett. 2024 Jan 8;15(2):181-188. doi: 10.1021/acsmedchemlett.3c00455. , eCollection 2024 Feb 8. PMID:38352830<ref>PMID:38352830</ref>

			From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
			</div>
			<div class="pdbe-citations 8tty" style="background-color:#fffaf0;"></div>
			== References ==
			<references/>
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
	[[Category: Large Structures]]		[[Category: Large Structures]]
	[[Category: ~~N/a~~]]		[[Category: Macaca mulatta]]
			[[Category: Critton DA]]

OCA at 06:22, 7 February 2024

2024-02-07T06:22:39Z

← Older revision		Revision as of 06:22, 7 February 2024
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	~~'''Unreleased structure'''~~

	~~The entry~~ 8tty is ~~ON HOLD until Paper Publication~~		==n/a==
			<StructureSection load='8tty' size='340' side='right'caption='[[8tty]]' scene=''>
	~~Authors~~:		== Structural highlights ==
			<table><tr><td colspan='2'>Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=8TTY OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=8TTY FirstGlance]. <br>
	~~Description~~:		</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models\|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction</td></tr>
	[[Category: ~~Unreleased Structures~~]]		<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=8tty FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=8tty OCA], [https://pdbe.org/8tty PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=8tty RCSB], [https://www.ebi.ac.uk/pdbsum/8tty PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=8tty ProSAT]</span></td></tr>
			</table>
			__TOC__
			</StructureSection>
			[[Category: Large Structures]]
			[[Category: N/a]]

OCA at 12:18, 18 October 2023

2023-10-18T12:18:49Z

← Older revision		Revision as of 12:18, 18 October 2023
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	'''Unreleased structure'''		'''Unreleased structure'''

	The entry 8tty is ON HOLD		The entry 8tty is ON HOLD until Paper Publication

	Authors:		Authors:

OCA: Protected "8tty" [edit=sysop:move=sysop]

2023-08-23T04:51:32Z

Protected "8tty" [edit=sysop:move=sysop]

← Older revision	Revision as of 04:51, 23 August 2023
(No difference)

OCA: New page: '''Unreleased structure''' The entry 8tty is ON HOLD Authors: Description: Category: Unreleased Structures

2023-08-23T04:51:31Z

New page: '''Unreleased structure''' The entry 8tty is ON HOLD Authors: Description: Category: Unreleased Structures

New page

'''Unreleased structure'''

The entry 8tty is ON HOLD

Authors:

Description:
[[Category: Unreleased Structures]]

8tty - Revision history

OCA at 12:11, 30 October 2024

OCA at 06:22, 7 February 2024

OCA at 12:18, 18 October 2023

OCA: Protected "8tty" [edit=sysop:move=sysop]

OCA: New page: '''Unreleased structure''' The entry 8tty is ON HOLD Authors: Description: Category: Unreleased Structures