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Image Search Results


Bifunctional small molecule dTAG-13 binds to the FKBP12 F36V domain of tagged CYP1A2 and recruits an E3 ligase; ubiquitination (curved arrow) directs fusion protein degradation. The AP1867 moiety of dTAG-13 (bottom left) binds FKBP12 F36V selectively; the thalidomide moiety recruits cereblon.

Journal: bioRxiv

Article Title: Reversible in vivo regulation of drug metabolizing enzyme CYP1A2 activity through a dTAG knock-in strategy

doi: 10.64898/2026.05.06.722533

Figure Lengend Snippet: Bifunctional small molecule dTAG-13 binds to the FKBP12 F36V domain of tagged CYP1A2 and recruits an E3 ligase; ubiquitination (curved arrow) directs fusion protein degradation. The AP1867 moiety of dTAG-13 (bottom left) binds FKBP12 F36V selectively; the thalidomide moiety recruits cereblon.

Article Snippet: dTAG-13 was purchased from MedChemExpress (Monmouth Junction, NJ).

Techniques: Ubiquitin Proteomics

a , Hepatic CYP1A2 and CYP1A2 dTAG protein expression in WT, HET, and HOM mice. b , Densitometric quantification of CYP1A2 and CYP1A2 dTAG protein. c , CYP1A2 dTAG catalytic activity. d , Dose-dependent degradation of CYP1A2 dTAG protein mediated by dTAG-13 in HMO mice. e , Densitometric quantification of CYP1A2 dTAG protein in liver 4 hours post dTAG-13 treatment. f & g , CYP1A2 dTAG activity in MLMs prepared from HOM mice treated with vehicle or dTAG-13. h , Hepatic immunostaining of CYP1A2 dTAG in HOM mice (vehicle). i , Hepatic immunostaining of CYP1A2 dTAG in HOM mice (dTAG-13). For densitometric quantification in , native Cyp1a2 level was set as 100%; in , protein levels in vehicle-treated mice were set as 100%. M, male; F, Female. na, not available; ns, not significant; **, p<0.01, ***; P<0.001; HET, heterozygous; HOM, homozygous. n = 4.

Journal: bioRxiv

Article Title: Reversible in vivo regulation of drug metabolizing enzyme CYP1A2 activity through a dTAG knock-in strategy

doi: 10.64898/2026.05.06.722533

Figure Lengend Snippet: a , Hepatic CYP1A2 and CYP1A2 dTAG protein expression in WT, HET, and HOM mice. b , Densitometric quantification of CYP1A2 and CYP1A2 dTAG protein. c , CYP1A2 dTAG catalytic activity. d , Dose-dependent degradation of CYP1A2 dTAG protein mediated by dTAG-13 in HMO mice. e , Densitometric quantification of CYP1A2 dTAG protein in liver 4 hours post dTAG-13 treatment. f & g , CYP1A2 dTAG activity in MLMs prepared from HOM mice treated with vehicle or dTAG-13. h , Hepatic immunostaining of CYP1A2 dTAG in HOM mice (vehicle). i , Hepatic immunostaining of CYP1A2 dTAG in HOM mice (dTAG-13). For densitometric quantification in , native Cyp1a2 level was set as 100%; in , protein levels in vehicle-treated mice were set as 100%. M, male; F, Female. na, not available; ns, not significant; **, p<0.01, ***; P<0.001; HET, heterozygous; HOM, homozygous. n = 4.

Article Snippet: dTAG-13 was purchased from MedChemExpress (Monmouth Junction, NJ).

Techniques: Expressing, Activity Assay, Immunostaining

a , HOM-v vs. WT-v. b , HOM-d vs. HOM-v. v, vehicle; d, dTAG-13. * Cyp1a2 in the figure refers to CYP1A2 or CYP1A2 dTAG . (n = 6, 3 males and 3 females).

Journal: bioRxiv

Article Title: Reversible in vivo regulation of drug metabolizing enzyme CYP1A2 activity through a dTAG knock-in strategy

doi: 10.64898/2026.05.06.722533

Figure Lengend Snippet: a , HOM-v vs. WT-v. b , HOM-d vs. HOM-v. v, vehicle; d, dTAG-13. * Cyp1a2 in the figure refers to CYP1A2 or CYP1A2 dTAG . (n = 6, 3 males and 3 females).

Article Snippet: dTAG-13 was purchased from MedChemExpress (Monmouth Junction, NJ).

Techniques:

a , The PK profile of caffeine. b , The PK profile of paraxanthine (a CYP1A2-mediated primary metabolite). c , The PK parameters of caffeine. The caffeine (10 mg/kg, p.o.) was administered to mice 4 h post vehicle or dTAG-13 (20 mg/kg, i.p.). Two-week wash-out following PK of caffeine in Cyp1a2 dTAG -HOM mice treated with vehicle, PK in Cyp1a2 dTAG -HOM mice treated with dTAG-13 was performed. (n = 6). *, p<0.05; **, p<0.01, ***. P<0.001. HOM, homozygous.

Journal: bioRxiv

Article Title: Reversible in vivo regulation of drug metabolizing enzyme CYP1A2 activity through a dTAG knock-in strategy

doi: 10.64898/2026.05.06.722533

Figure Lengend Snippet: a , The PK profile of caffeine. b , The PK profile of paraxanthine (a CYP1A2-mediated primary metabolite). c , The PK parameters of caffeine. The caffeine (10 mg/kg, p.o.) was administered to mice 4 h post vehicle or dTAG-13 (20 mg/kg, i.p.). Two-week wash-out following PK of caffeine in Cyp1a2 dTAG -HOM mice treated with vehicle, PK in Cyp1a2 dTAG -HOM mice treated with dTAG-13 was performed. (n = 6). *, p<0.05; **, p<0.01, ***. P<0.001. HOM, homozygous.

Article Snippet: dTAG-13 was purchased from MedChemExpress (Monmouth Junction, NJ).

Techniques: