Glucuronidase: Difference between revisions

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==β-Glucuronidase==
 
<StructureSection load='3hn3' size='340' side='right' caption='Ribbon diagram of glycosylated human βα-glucuronidase complex with MPD(PDB code [[3hn3]]).' scene=''>
<StructureSection load='3hn3' size='340' side='right' caption='Ribbon diagram of glycosylated human βα-glucuronidase complex with MPD(PDB code [[3hn3]]).' scene=''>


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== Function ==
== Function ==
'''&beta;-glucuronidase''' is a ubiquitous enzyme that catalyzes the hydrolysis of a glucuronide moiety from a variety of substrates.  This enzyme is present throughout biological systems, including bacteria up through humans.  '''α-glucuronidase''' catalyzes the conversion of  α-D-glucuronoside to alcohol and D-glucuronate.
'''&beta;-glucuronidase''' is a ubiquitous enzyme that catalyzes the hydrolysis of a glucuronide moiety from a variety of substrates.  This enzyme is present throughout biological systems, including bacteria up through humans.  '''α-glucuronidase''' catalyzes the conversion of  α-D-glucuronoside to alcohol and D-glucuronate<ref>PMID:8599764</ref>.


== Relevance ==
== Relevance ==
Deficiencies in the human form of &beta;-glucuronidase (<scene name='59/596447/Human_bglucuronidase/1'>overall structure</scene>, PDB ID 3HN3<ref>DOI:10.2210/pdb3hn3/pdb</ref>) is associated with a disease known as Sly Syndrome (AKA Mucopolysaccharidosis VII -- MPS VII).  This disease is characterized by mental retardation, short stature, macrocephaly, and enlarged joints.  As is commonly seen with genetic disorders, patients with this disease present a spectrum of symptom severity, but the disease is always ultimately fatal.
The ''E. coli'' form of &beta;-glucuronidase (<scene name='59/596447/E_coli_b-glucuronidase/1'>overall structure</scene>, PDB ID 3LPF<ref>DOI:10.2210/pdb3lpf/pdb</ref>) is associated with the side effects seen with administration of the cancer chemotherapy drug CPT-11.  This drug gets converted to SN38, a topoisomerase inhibitor, by the liver.  The body adds a glucuronide group to this molecule (now SN38-G) to mark it for elimination, which partially occurs through the intestine.  Once in the intestine, bacterial &beta;-glucuronidase cleaves the glucuronide from the SN38-G, releasing the SN38 into the intestinal lumen.  The released SN38 prevents cell division, compromising the epithelial lining of the intestines, a painful and dangerous side-effect of CPT-11 administration.
The ''E. coli'' form of &beta;-glucuronidase (<scene name='59/596447/E_coli_b-glucuronidase/1'>overall structure</scene>, PDB ID 3LPF<ref>DOI:10.2210/pdb3lpf/pdb</ref>) is associated with the side effects seen with administration of the cancer chemotherapy drug CPT-11.  This drug gets converted to SN38, a topoisomerase inhibitor, by the liver.  The body adds a glucuronide group to this molecule (now SN38-G) to mark it for elimination, which partially occurs through the intestine.  Once in the intestine, bacterial &beta;-glucuronidase cleaves the glucuronide from the SN38-G, releasing the SN38 into the intestinal lumen.  The released SN38 prevents cell division, compromising the epithelial lining of the intestines, a painful and dangerous side-effect of CPT-11 administration.


Selective inhibition of bacterial &beta;-glucuronidase is desired to alleviate this side-effect of CPT-11 treatment, hopefully without inhibiting the human form of the enzyme.
Selective inhibition of bacterial &beta;-glucuronidase is desired to alleviate this side-effect of CPT-11 treatment, hopefully without inhibiting the human form of the enzyme.


==Disease==
Deficiencies in the human form of &beta;-glucuronidase (<scene name='59/596447/Human_bglucuronidase/1'>overall structure</scene>, PDB ID 3HN3<ref>DOI:10.2210/pdb3hn3/pdb</ref>) is associated with a disease known as Sly Syndrome (AKA Mucopolysaccharidosis VII -- MPS VII).  This disease is characterized by mental retardation, short stature, macrocephaly, and enlarged joints.  As is commonly seen with genetic disorders, patients with this disease present a spectrum of symptom severity, but the disease is always ultimately fatal.


== Structural highlights ==
== Structural highlights ==
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== References ==
== References ==
<references/>
<ref>DOI:10.2210/pdb3hn3/pdb</ref>
<ref>DOI:10.2210/pdb3hn3/pdb</ref>
<ref>DOI:10.2210/pdb3lpf/pdb</ref>
<ref>DOI:10.2210/pdb3lpf/pdb</ref>
[[Category:Topic Page]]
[[Category:Topic Page]]

Revision as of 13:14, 7 March 2016

Ribbon diagram of glycosylated humanβα-glucuronidase complex with MPD(PDB code 3hn3).

Drag the structure with the mouse to rotate

3D Structures of glucuronisidase

Updated on 07-March-2016

    • 1bhg, 3hn3 – hBGUS – human
    • 3k46 – EcBGUS – Escherichia coli
    • 3k4a – EcBGUS (mutant)
    • 3vny – AcBGUS – Acidobacterium capsulatum
    • 4jkk, 4jkl – BGUS – Streptococcus agalactiae
  • β-glucuronidase binary complex
    • 3vnz – AcBGUS + glucuronic acid
    • 3vo0 – AcBGUS + glucuronic acid derivative
    • 3k4d – EcBGUS + glucaro-D-lactam
    • 3lpf, 3lpg, 4jhz – EcBGUS + inhibitor
    • 4jkm – BGUS + MBP – Clostridium perfringens


References

[1] [2]

Proteopedia Page Contributors and Editors (what is this?)

Kimberly Lane, Michal Harel, Alexander Berchansky