Literature DB >> 10762046

Diacylglycerols with lipophilically equivalent branched acyl chains display high affinity for protein kinase C (PK-C). A direct measure of the effect of constraining the glycerol backbone in DAG lactones.

K Nacro1, B Bienfait, N E Lewin, P M Blumberg, V E Marquez.   

Abstract

New synthetic diacylglycerols (DAGs) with equivalent branched acyl chains were compared with commercially available DAGs as PK-C ligands. The results support the view that there is a minimal lipophilic requirement provided by the equivalent acyl groups that results in high binding affinity. Locking the glycerol backbone of the most potent DAG into a five-member lactone resulted in a 10-fold increase in potency.

Entities:  

Mesh:

Substances:

Year:  2000        PMID: 10762046     DOI: 10.1016/s0960-894x(00)00070-6

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  3 in total

1.  Ceramides: branched alkyl chains in the sphingolipid siblings of diacylglycerol improve biological potency.

Authors:  Ji-Hye Kang; Himanshu Garg; Dina M Sigano; Nicholas Francella; Robert Blumenthal; Victor E Marquez
Journal:  Bioorg Med Chem       Date:  2009-01-11       Impact factor: 3.641

2.  Rational design of drugs that induce human immunodeficiency virus replication.

Authors:  Dean H Hamer; Sven Bocklandt; Louise McHugh; Tae-Wook Chun; Peter M Blumberg; Dina M Sigano; Victor E Marquez
Journal:  J Virol       Date:  2003-10       Impact factor: 5.103

Review 3.  Structural insights into C1-ligand interactions: Filling the gaps by in silico methods.

Authors:  Sachin Katti; Tatyana I Igumenova
Journal:  Adv Biol Regul       Date:  2021-01-18
  3 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.