Intermolecular Interactions between Cholecystokinin-8 and the Third Extracellular Loop of the Cholecystokinin-2 Receptor†,‡

Abstract The inability to over-express AQP6 in the plasma membrane of heterologous cells has hampered efforts to further characterize the function of this aquaglyceroporin membrane protein at atomic detail. Using the AGR reporter system we have identified a region within loop C of AQP6 that is responsible for severely hampering its plasma membrane localization. Serine substitution corroborated that amino acids present within AQP6194-213 of AQP6 loop C contribute to intracellular retention. This intracellular retention signal may preclude proper plasma membrane trafficking and severely curtail expression of AQP6 in heterologous cells.

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Secondary Structure of the Third Extracellular Loop Responsible for Ligand Selectivity of a Mammalian Gonadotropin-Releasing Hormone Receptor

Journal of Medicinal Chemistry ◽

10.1021/jm011036k ◽

2002 ◽

Vol 45 (5) ◽

pp. 1026-1034 ◽

Cited By ~ 19

Author(s):

Renate Petry ◽

David Craik ◽

Gerald Haaima ◽

Bernhard Fromme ◽

Horst Klump ◽

...

Keyword(s):

Secondary Structure ◽

Hormone Receptor ◽

Gonadotropin Releasing Hormone ◽

Extracellular Loop ◽

Releasing Hormone ◽

Ligand Selectivity ◽

The Third ◽

Gonadotropin Releasing Hormone Receptor

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The disruption of the third extracellular loop of the red cell anion exchanger AE1 does not affect electroneutral Cl−/HCO3− exchange activity

Blood Cells Molecules and Diseases ◽

10.1016/j.bcmd.2004.01.010 ◽

2004 ◽

Vol 32 (3) ◽

pp. 379-383 ◽

Cited By ~ 6

Author(s):

Mark D Parker ◽

Michael J.A Tanner

Keyword(s):

Anion Exchanger ◽

Red Cell ◽

Extracellular Loop ◽

The Third ◽

Exchange Activity

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Polymorphism of 3-(5-phenyl-1,3,4-oxadiazol-2-yl)- and 3-[5-(pyridin-4-yl)-1,3,4-oxadiazol-2-yl]-2H-chromen-2-ones

Acta Crystallographica Section C Structural Chemistry ◽

10.1107/s2053229619014256 ◽

2019 ◽

Vol 75 (11) ◽

pp. 1541-1553

Author(s):

Svitlana V. Shishkina ◽

Irina S. Konovalova ◽

Pavlo V. Trostianko ◽

Anna O. Geleverya ◽

Sergiy M. Kovalenko ◽

...

Keyword(s):

Anticancer Activity ◽

Intermolecular Interactions ◽

Pairwise Interaction ◽

Interaction Energies ◽

The Third ◽

Weak Intermolecular Interactions ◽

Polymorphic Modifications ◽

The Difference ◽

Polymorphic Structure ◽

Head Type

This study of 3-(5-phenyl-1,3,4-oxadiazol-2-yl)-2H-chromen-2-one, C17H10N2O3, 1, and 3-[5-(pyridin-4-yl)-1,3,4-oxadiazol-2-yl]-2H-chromen-2-one, C16H9N3O3, 2, was performed on the assumption of the potential anticancer activity of the compounds. Three polymorphic structures for 1 and two polymorphic structures for 2 have been studied thoroughly. The strongest intermolecular interaction is stacking of the `head-to-head' type in all the studied crystals. The polymorphic structures of 1 differ with respect to the intermolecular interactions between stacked columns. Two of the polymorphs have a columnar or double columnar type of crystal organization, while the third polymorphic structure can be classified as columnar-layered. The difference between the two structures of 2 is less pronounced. Both crystals can be considered as having very similar arrangements of neighbouring columns. The formation of polymorphic modifications is caused by a subtle balance of very weak intermolecular interactions and packing differences can be identified only using an analysis based on a study of the pairwise interaction energies.

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