Identification of Ghrelin Receptor Blocker, D-[Lys3] GHRP-6 as a CXCR4 Receptor Antagonist
<p>[D-Lys3]-Growth Hormone Releasing Peptide-6 (DLS) is widely utilized <i>in vivo</i> and <i>in vitro</i> as a selective ghrelin receptor (GHS-R) antagonist. Unexpectedly, we identified that DLS also has the ability to block CXCL12 binding and activity through CXCR4 on...
| Main Author: | |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
Ivyspring International Publisher
2012-01-01
|
| Series: | International Journal of Biological Sciences |
| Online Access: | http://www.biolsci.org/v08p0108.htm |
| _version_ | 1818418732801720320 |
|---|---|
| author | Kalpesh Patel, Vishwa Deep Dixit, Jun Ho Lee, Jie Wan Kim, Eric M. Schaffer, Dzung Nguyen, Dennis D. Taub |
| author_facet | Kalpesh Patel, Vishwa Deep Dixit, Jun Ho Lee, Jie Wan Kim, Eric M. Schaffer, Dzung Nguyen, Dennis D. Taub |
| author_sort | Kalpesh Patel, Vishwa Deep Dixit, Jun Ho Lee, Jie Wan Kim, Eric M. Schaffer, Dzung Nguyen, Dennis D. Taub |
| collection | DOAJ |
| description | <p>[D-Lys3]-Growth Hormone Releasing Peptide-6 (DLS) is widely utilized <i>in vivo</i> and <i>in vitro</i> as a selective ghrelin receptor (GHS-R) antagonist. Unexpectedly, we identified that DLS also has the ability to block CXCL12 binding and activity through CXCR4 on T cells and peripheral blood mononuclear cells (PBMCs). Moreover, as CXCR4 has been shown to act as a major co-receptor for HIV-1 entry into CD4 positive host cells, we have also found that DLS partially blocks CXCR4-mediated HIV-1 entry and propagation in activated human PBMCs. These data demonstrate that DLS is not the specific and selective antagonist as thought for GHS-R1a and appears to have additional effects on the CXCR4 chemokine receptor. Our findings also suggest that structural analogues that mimic DLS binding properties may also have properties of blocking HIV infectivity, CXCR4 dependent cancer cell migration and attenuating chemokine-mediated immune cell trafficking in inflammatory disorders.</p> |
| first_indexed | 2024-12-14T12:27:21Z |
| format | Article |
| id | doaj.art-dce9eed494a54126ae1e9a969afea4b6 |
| institution | Directory Open Access Journal |
| issn | 1449-2288 |
| language | English |
| last_indexed | 2024-12-14T12:27:21Z |
| publishDate | 2012-01-01 |
| publisher | Ivyspring International Publisher |
| record_format | Article |
| series | International Journal of Biological Sciences |
| spelling | doaj.art-dce9eed494a54126ae1e9a969afea4b62022-12-21T23:01:17ZengIvyspring International PublisherInternational Journal of Biological Sciences1449-22882012-01-0181108117Identification of Ghrelin Receptor Blocker, D-[Lys3] GHRP-6 as a CXCR4 Receptor AntagonistKalpesh Patel, Vishwa Deep Dixit, Jun Ho Lee, Jie Wan Kim, Eric M. Schaffer, Dzung Nguyen, Dennis D. Taub<p>[D-Lys3]-Growth Hormone Releasing Peptide-6 (DLS) is widely utilized <i>in vivo</i> and <i>in vitro</i> as a selective ghrelin receptor (GHS-R) antagonist. Unexpectedly, we identified that DLS also has the ability to block CXCL12 binding and activity through CXCR4 on T cells and peripheral blood mononuclear cells (PBMCs). Moreover, as CXCR4 has been shown to act as a major co-receptor for HIV-1 entry into CD4 positive host cells, we have also found that DLS partially blocks CXCR4-mediated HIV-1 entry and propagation in activated human PBMCs. These data demonstrate that DLS is not the specific and selective antagonist as thought for GHS-R1a and appears to have additional effects on the CXCR4 chemokine receptor. Our findings also suggest that structural analogues that mimic DLS binding properties may also have properties of blocking HIV infectivity, CXCR4 dependent cancer cell migration and attenuating chemokine-mediated immune cell trafficking in inflammatory disorders.</p>http://www.biolsci.org/v08p0108.htm |
| spellingShingle | Kalpesh Patel, Vishwa Deep Dixit, Jun Ho Lee, Jie Wan Kim, Eric M. Schaffer, Dzung Nguyen, Dennis D. Taub Identification of Ghrelin Receptor Blocker, D-[Lys3] GHRP-6 as a CXCR4 Receptor Antagonist International Journal of Biological Sciences |
| title | Identification of Ghrelin Receptor Blocker, D-[Lys3] GHRP-6 as a CXCR4 Receptor Antagonist |
| title_full | Identification of Ghrelin Receptor Blocker, D-[Lys3] GHRP-6 as a CXCR4 Receptor Antagonist |
| title_fullStr | Identification of Ghrelin Receptor Blocker, D-[Lys3] GHRP-6 as a CXCR4 Receptor Antagonist |
| title_full_unstemmed | Identification of Ghrelin Receptor Blocker, D-[Lys3] GHRP-6 as a CXCR4 Receptor Antagonist |
| title_short | Identification of Ghrelin Receptor Blocker, D-[Lys3] GHRP-6 as a CXCR4 Receptor Antagonist |
| title_sort | identification of ghrelin receptor blocker d lys3 ghrp 6 as a cxcr4 receptor antagonist |
| url | http://www.biolsci.org/v08p0108.htm |
| work_keys_str_mv | AT kalpeshpatelvishwadeepdixitjunholeejiewankimericmschafferdzungnguyendennisdtaub identificationofghrelinreceptorblockerdlys3ghrp6asacxcr4receptorantagonist |