FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2971326194> ?p ?o ?g. }

• W2971326194 abstract "Abstract As an important member of cytochrome P450 (CYP) enzymes, human CYP1A2 is associated with the metabolism of caffeine and melatonin and the activation of precarcinogens. Besides, this CYP protein also involves in metabolizing 5-10% of clinical medicines. Some peripheral mutations in CYP1A2 (P42R, I386F, R431W, and R456H) significantly decrease the enzyme activities, resulting in a vital reduction in substrate metabolisms. To explore the effects of these peripheral mutations, we constructed a membrane-binding model for the full-length human CYP1A2 and studied their dynamic behaviors on lipid membranes. Free energy calculations indicate that the peripheral mutations donot influence substrate binding. P42R is located in the N-terminal anchor, and its positive charged sidechain is adverse to membrane binding. I386F enhances the van der Waals contacts of the water channel bottleneck and R456H breaks the hydrogen bonding interactions that function to position the BC loop, both of which result in a significant inhibition on the water channel. R431W causes a sidechain conformational rearrangement for aromatic residues around the substrate channel, making it in a closed state in most cases. Our computational simulations demonstrate that pi-pi stacking interactions are essential for substrate binding and channel opening. We hope that these findings may be of general relevance to the mutation-induced activity changes for CYP proteins, providing useful information for understanding the CYP-mediated drug metabolism." @default.
• W2971326194 created "2019-09-05" @default.
• W2971326194 creator A5000489839 @default.
• W2971326194 creator A5007870731 @default.
• W2971326194 creator A5078033151 @default.
• W2971326194 date "2019-09-03" @default.
• W2971326194 modified "2023-09-28" @default.
• W2971326194 title "Impact of peripheral mutations on the access channels of human cytochrome P450 1A2" @default.
• W2971326194 cites W1539100167 @default.
• W2971326194 cites W1764799499 @default.
• W2971326194 cites W1855224084 @default.
• W2971326194 cites W1963968986 @default.
• W2971326194 cites W1968158648 @default.
• W2971326194 cites W1968984443 @default.
• W2971326194 cites W1972508135 @default.
• W2971326194 cites W2001277249 @default.
• W2971326194 cites W2009013339 @default.
• W2971326194 cites W2013847640 @default.
• W2971326194 cites W2018363141 @default.
• W2971326194 cites W2020828286 @default.
• W2971326194 cites W2021232512 @default.
• W2971326194 cites W2035819928 @default.
• W2971326194 cites W2041917695 @default.
• W2971326194 cites W2044901017 @default.
• W2971326194 cites W2053485654 @default.
• W2971326194 cites W2065283382 @default.
• W2971326194 cites W2068007832 @default.
• W2971326194 cites W2068493131 @default.
• W2971326194 cites W2069518737 @default.
• W2971326194 cites W2071537307 @default.
• W2971326194 cites W2076350095 @default.
• W2971326194 cites W2079745478 @default.
• W2971326194 cites W2090988665 @default.
• W2971326194 cites W2105668062 @default.
• W2971326194 cites W2107965661 @default.
• W2971326194 cites W2113524447 @default.
• W2971326194 cites W2114393702 @default.
• W2971326194 cites W2118163167 @default.
• W2971326194 cites W2120885049 @default.
• W2971326194 cites W2131080603 @default.
• W2971326194 cites W2134967712 @default.
• W2971326194 cites W2148012276 @default.
• W2971326194 cites W2150981663 @default.
• W2971326194 cites W2155080119 @default.
• W2971326194 cites W2164705071 @default.
• W2971326194 cites W2183696852 @default.
• W2971326194 cites W2264490550 @default.
• W2971326194 cites W2327129143 @default.
• W2971326194 cites W2411913461 @default.
• W2971326194 cites W2555870966 @default.
• W2971326194 cites W2559974546 @default.
• W2971326194 cites W2770039067 @default.
• W2971326194 cites W2798194035 @default.
• W2971326194 cites W2954094311 @default.
• W2971326194 cites W4233120011 @default.
• W2971326194 doi "https://doi.org/10.1101/754739" @default.
• W2971326194 hasPublicationYear "2019" @default.
• W2971326194 type Work @default.
• W2971326194 sameAs 2971326194 @default.
• W2971326194 citedByCount "0" @default.
• W2971326194 crossrefType "posted-content" @default.
• W2971326194 hasAuthorship W2971326194A5000489839 @default.
• W2971326194 hasAuthorship W2971326194A5007870731 @default.
• W2971326194 hasAuthorship W2971326194A5078033151 @default.
• W2971326194 hasBestOaLocation W29713261941 @default.
• W2971326194 hasConcept C104317684 @default.
• W2971326194 hasConcept C12554922 @default.
• W2971326194 hasConcept C181199279 @default.
• W2971326194 hasConcept C185592680 @default.
• W2971326194 hasConcept C18903297 @default.
• W2971326194 hasConcept C196013638 @default.
• W2971326194 hasConcept C2777289219 @default.
• W2971326194 hasConcept C501734568 @default.
• W2971326194 hasConcept C50605568 @default.
• W2971326194 hasConcept C526171541 @default.
• W2971326194 hasConcept C55493867 @default.
• W2971326194 hasConcept C86745063 @default.
• W2971326194 hasConcept C86803240 @default.
• W2971326194 hasConcept C95444343 @default.
• W2971326194 hasConceptScore W2971326194C104317684 @default.
• W2971326194 hasConceptScore W2971326194C12554922 @default.
• W2971326194 hasConceptScore W2971326194C181199279 @default.
• W2971326194 hasConceptScore W2971326194C185592680 @default.
• W2971326194 hasConceptScore W2971326194C18903297 @default.
• W2971326194 hasConceptScore W2971326194C196013638 @default.
• W2971326194 hasConceptScore W2971326194C2777289219 @default.
• W2971326194 hasConceptScore W2971326194C501734568 @default.
• W2971326194 hasConceptScore W2971326194C50605568 @default.
• W2971326194 hasConceptScore W2971326194C526171541 @default.
• W2971326194 hasConceptScore W2971326194C55493867 @default.
• W2971326194 hasConceptScore W2971326194C86745063 @default.
• W2971326194 hasConceptScore W2971326194C86803240 @default.
• W2971326194 hasConceptScore W2971326194C95444343 @default.
• W2971326194 hasLocation W29713261941 @default.
• W2971326194 hasOpenAccess W2971326194 @default.
• W2971326194 hasPrimaryLocation W29713261941 @default.
• W2971326194 hasRelatedWork W1983350301 @default.
• W2971326194 hasRelatedWork W2002511916 @default.
• W2971326194 hasRelatedWork W2025568556 @default.
• W2971326194 hasRelatedWork W2028114416 @default.

• next