NDLI: Trigonal scaffolds for multivalent targeting of melanocortin receptors

Content Provider	PubMed Central
Author	Dayan, Elshan N. G. R. Jayasundera, Thanuja Anglin, Bobbi L. Weber, Craig S. Lynch, Ronald M. Mash, Eugene A.
Abstract	Melanocortin receptors can be used as biomarkers to detect and possibly treat melanoma. To these ends, molecules bearing one, two, or three copies of the weakly binding ligand MSH(4) were attached to scaffolds based on phloroglucinol, tripropargylamine, and 1,4,7-triazacyclononane by means of the copper-assisted azide-alkyne cyclization. This synthetic design allows rapid assembly of multivalent molecules. The bioactivities of these compounds were evaluated using a competitive binding assay that employed human embryonic kidney cells engineered to overexpress the melanocortin 4 receptor. The divalent molecules exhibited 10- to 30-fold higher levels of inhibition when compared to the corresponding monovalent molecules, consistent with divalent binding, whereas the trivalent molecules were only statistically (~2-fold) better than the divalent molecules, still consistent with divalent binding but inconsistent with trivalent binding. Possible reasons for these behaviors and planned refinements of the multivalent constructs targeting melanocortin receptors based on these scaffolds are discussed.
Related Links	http://dx.doi.org/10.1039/c4ob02094d
Ending Page	1791
Page Count	14
Starting Page	1778
File Format	PDF
ISSN	14770520
e-ISSN	14770539
Journal	Organic & biomolecular chemistry
Issue Number	6
Volume Number	13
Language	English
Publisher Date	2015-01-01
Access Restriction	Open
Subject Keyword	Physical and Theoretical Chemistry Organic Chemistry Biochemistry Research in Higher Education
Content Type	Text
Resource Type	Article
Subject	Organic Chemistry Biochemistry Physical and Theoretical Chemistry

Sl.	Authority	Responsibilities	Communication Details
1	Ministry of Education (GoI), Department of Higher Education	Sanctioning Authority	https://www.education.gov.in/ict-initiatives
2	Indian Institute of Technology Kharagpur	Host Institute of the Project: The host institute of the project is responsible for providing infrastructure support and hosting the project	https://www.iitkgp.ac.in
3	National Digital Library of India Office, Indian Institute of Technology Kharagpur	The administrative and infrastructural headquarters of the project	Dr. B. Sutradhar bsutra@ndl.gov.in
4	Project PI / Joint PI	Principal Investigator and Joint Principal Investigators of the project	Dr. B. Sutradhar bsutra@ndl.gov.in Prof. Saswat Chakrabarti will be added soon
5	Website/Portal (Helpdesk)	Queries regarding NDLI and its services	support@ndl.gov.in
6	Contents and Copyright Issues	Queries related to content curation and copyright issues	content@ndl.gov.in
7	National Digital Library of India Club (NDLI Club)	Queries related to NDLI Club formation, support, user awareness program, seminar/symposium, collaboration, social media, promotion, and outreach	clubsupport@ndl.gov.in
8	Digital Preservation Centre (DPC)	Assistance with digitizing and archiving copyright-free printed books	dpc@ndl.gov.in
9	IDR Setup or Support	Queries related to establishment and support of Institutional Digital Repository (IDR) and IDR workshops	idr@ndl.gov.in

Synthesis of Rigid Multivalent Scaffolds Based on Adamantane

Pyrrole-based Scaffolds For Turn Mimics

Multicomponent Assembly Strategies for the Synthesis of Diverse Tetrahydroisoquinoline Scaffolds

Multicomponent Synthesis of Diverse 1,4-Benzodiazepine Scaffolds

Diazoacetoacetate Enones for the Synthesis of Diverse Natural Product-Like Scaffolds

Photoactive Barbiturate Receptors

Synthesis of Rigid Multivalent Scaffolds Based on Adamantane

An RCM Strategy to Stereodiverse δ-Sultam Scaffolds

Synthesis and Diversification of 1,2,3-Triazole-Fused 1,4-Benzodiazepine Scaffolds

Trigonal scaffolds for multivalent targeting of melanocortin receptors

Similar Documents

Synthesis of Rigid Multivalent Scaffolds Based on Adamantane

Pyrrole-based Scaffolds For Turn Mimics

Multicomponent Assembly Strategies for the Synthesis of Diverse Tetrahydroisoquinoline Scaffolds

Multicomponent Synthesis of Diverse 1,4-Benzodiazepine Scaffolds

Diazoacetoacetate Enones for the Synthesis of Diverse Natural Product-Like Scaffolds

Photoactive Barbiturate Receptors

Synthesis of Rigid Multivalent Scaffolds Based on Adamantane

An RCM Strategy to Stereodiverse δ-Sultam Scaffolds

Synthesis and Diversification of 1,2,3-Triazole-Fused 1,4-Benzodiazepine Scaffolds

Trigonal scaffolds for multivalent targeting of melanocortin receptors