User:R. Jeremy Johnson/ABCG2 Transporter: Difference between revisions

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The [https://en.wikipedia.org/wiki/ABCG2 ABCG2 multidrug transporter] is a membrane protein from the '''A'''TP-'''B'''inding '''C'''assette [https://en.wikipedia.org/wiki/ATP-binding_cassette_transporter (ABC)] transporter family, specifically the G-subfamily. Also known as the breast cancer resistance protein (BCRP), ABCG2 has physiological roles in various tissue cells including the [https://en.wikipedia.org/wiki/Mammary_gland mammary gland] and the [https://en.wikipedia.org/wiki/Blood%E2%80%93brain_barrier blood-brain], [https://en.wikipedia.org/wiki/Blood%E2%80%93testis_barrier blood-testis], and [https://en.wikipedia.org/wiki/Placenta maternal-fetal] barriers.<ref name="Taylor">PMID:28554189</ref> ABCG2 protects cells by exporting [https://en.wikipedia.org/wiki/Xenobiotic xenobiotic] molecules out of the cell using ATP hydrolysis. ABCG2 also affects the [https://en.wikipedia.org/wiki/Pharmacokinetics pharmacokinetics] of many drugs and contributes to [https://en.wikipedia.org/wiki/Multiple_drug_resistance multidrug resistance].<ref name="Manolaridis">PMID:30405239</ref> ABCG2 belongs to the family of 48 transporter proteins called ATP-binding cassette transporters (ABC transporters). A high percentage of the ABC family transporters (19 of the 48) transport [https://en.wikipedia.org/wiki/List_of_chemotherapeutic_agents chemotherapeutic agents] out of cells, making expression levels of ABC transporters a major indicator of cancer treatment prognosis.<ref name="Robey">PMID:29643473</ref>

Using [https://en.wikipedia.org/wiki/Cryogenic_electron_microscopy cryoelectron microscopy] (cryo-EM), the two cavity substrate transport structure (<scene name='83/832932/Highlight_cavity_1/3'>Cavity 1</scene>; <scene name='83/832932/Atp_bound_use_cav_2/3'>Cavity 2</scene>), inward facing nucleotide binding domain (<scene name='83/832932/Overall_structure_nbd_unbound/6'>NBD</scene>), and condensed extracellular loop 3 (<scene name='83/832939/El-3/3'>EL-3</scene>) structure of ABCG2 have been elucidated. These structures also illustrated the transporter cycle of ABCG2, the binding locations for inhibitors, and the link between cancer and the ABC transporter family.<ref name="Taylor"/><ref name="Manolaridis"/><ref name="Jackson"/>

Using [https://en.wikipedia.org/wiki/Cryogenic_electron_microscopy cryoelectron microscopy] (cryo-EM), the two cavity substrate transport structure (<scene name='83/832932/Highlight_cavity_1/3'>Cavity 1</scene>; <scene name='83/832932/Atp_bound_use_cav_2/3'>Cavity 2</scene>), inward facing nucleotide binding domain (<scene name='83/832932/Overall_structure_nbd_unbound/6'>NBD</scene>), and condensed extracellular loop 3 (<scene name='83/832939/El-3/3'>EL-3</scene>) structure of ABCG2 have been elucidated. These structures also illustrated the transporter cycle of ABCG2, the binding locations for inhibitors, and the link between cancer and the ABC transporter family.<ref name="Taylor"/><ref name="Manolaridis"/><ref name="Jackson">PMID:29610494</ref>

== Structural highlights ==

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 The [https://en.wikipedia.org/wiki/ABCG2 ABCG2 multidrug transporter] is a membrane protein from the '''A'''TP-'''B'''inding '''C'''assette [https://en.wikipedia.org/wiki/ATP-binding_cassette_transporter (ABC)] transporter family, specifically the G-subfamily. Also known as the breast cancer resistance protein (BCRP), ABCG2 has physiological roles in various tissue cells including the [https://en.wikipedia.org/wiki/Mammary_gland mammary gland] and the [https://en.wikipedia.org/wiki/Blood%E2%80%93brain_barrier blood-brain], [https://en.wikipedia.org/wiki/Blood%E2%80%93testis_barrier blood-testis], and [https://en.wikipedia.org/wiki/Placenta maternal-fetal] barriers.<ref name="Taylor">PMID:28554189</ref>  ABCG2 protects cells by exporting [https://en.wikipedia.org/wiki/Xenobiotic xenobiotic] molecules out of the cell using ATP hydrolysis. ABCG2 also affects the [https://en.wikipedia.org/wiki/Pharmacokinetics pharmacokinetics] of many drugs and contributes to [https://en.wikipedia.org/wiki/Multiple_drug_resistance multidrug resistance].<ref name="Manolaridis">PMID:30405239</ref> ABCG2 belongs to the family of 48 transporter proteins called ATP-binding cassette transporters (ABC transporters). A high percentage of the ABC family transporters (19 of the 48) transport [https://en.wikipedia.org/wiki/List_of_chemotherapeutic_agents chemotherapeutic agents] out of cells, making expression levels of ABC transporters a major indicator of cancer treatment prognosis.<ref name="Robey">PMID:29643473</ref>
-Using [https://en.wikipedia.org/wiki/Cryogenic_electron_microscopy cryoelectron microscopy] (cryo-EM), the two cavity substrate transport structure (<scene name='83/832932/Highlight_cavity_1/3'>Cavity 1</scene>; <scene name='83/832932/Atp_bound_use_cav_2/3'>Cavity 2</scene>), inward facing nucleotide binding domain (<scene name='83/832932/Overall_structure_nbd_unbound/6'>NBD</scene>), and condensed extracellular loop 3 (<scene name='83/832939/El-3/3'>EL-3</scene>) structure of ABCG2 have been elucidated. These structures also illustrated the transporter cycle of ABCG2, the binding locations for inhibitors, and the link between cancer and the ABC transporter family.<ref name="Taylor"/><ref name="Manolaridis"/><ref name="Jackson"/>
+Using [https://en.wikipedia.org/wiki/Cryogenic_electron_microscopy cryoelectron microscopy] (cryo-EM), the two cavity substrate transport structure (<scene name='83/832932/Highlight_cavity_1/3'>Cavity 1</scene>; <scene name='83/832932/Atp_bound_use_cav_2/3'>Cavity 2</scene>), inward facing nucleotide binding domain (<scene name='83/832932/Overall_structure_nbd_unbound/6'>NBD</scene>), and condensed extracellular loop 3 (<scene name='83/832939/El-3/3'>EL-3</scene>) structure of ABCG2 have been elucidated. These structures also illustrated the transporter cycle of ABCG2, the binding locations for inhibitors, and the link between cancer and the ABC transporter family.<ref name="Taylor"/><ref name="Manolaridis"/><ref name="Jackson">PMID:29610494</ref>
 == Structural highlights ==