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nuclear receptor

nuclear receptor as one of drug target

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nuclear receptor

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  1. Reseptor inti(nuclear receptor) Nuclear Receptor

  2. Pathway maps Transcription_Androgen Receptor nuclear signaling

  3. Reseptor inti(nuclear receptor) • Berada di dalamsel (sitoplasma) atau di nukleus aktivitasnyaberada di dalamintiaktivitasutama : regulasitranskripsigen • Liganuntukreseptor ini umumnyaberbobotmolekulkecil(< 1000 dalton), bersifatlipofilik, mudahmasukkedalamseluntukmencapaireseptor-nya • Contohligan : hormonglukokortikoid, vitamin D, asamretinoat, danhormontiroid, dll.

  4. SHR SHR RXR ? R Classification - subfamilies • Subfamilies • Type I: Steroid receptors • undergonuclear translocation upon ligand activation • bind as homodimers to invertedrepeat DNA half sites, • Type II: RXR heterodimers • retained in thenucleusregardlessofthepresenceof ligand • usually bind as heterodimers with RXR to directrepeats. • Type III: orphanNRs • dimericorphanreceptors • Monomericorphanreceptors • Half receptors

  5. Altern.class. • Evolutionaryanalysisofthereceptors has led to a subdivision in six different subfamilies

  6. Lokasi Reseptor

  7. Reseptor steroid Steroid ? • Senyawa lipid yang memiliki 3 cincinsikloheksandan 1 cincinsiklopentan contoh ? • kolesterol, hormon estrogen, testosteron, kortikoid, dll Kortikosteroid ? • Steroid yang disintesisdandilepaskanoleh cortex adrenal : ada 2 : glukokortikoiddanmineralokortikoid • Padamanusia: • glukokortikoidutamaadalahkortisol/ hidrokortison (padatikus: kortikosteron), danmineralokortikoidutamaadalahaldosteron

  8. MekanismekerjaGlukodan mineral (Kortokoid)

  9. Perbandingan Aktivitas Kortikosteroid

  10. Bagaimanasteroidbekerja ? • Steroid (glukokortikoid, mineralokortikoid) bekerjadengan cara berikatandenganreseptornyasuatureseptorintraselulermeregulasitranskripsigenmRNA proteintertentumempengaruhifungsiseltertentu • Reseptorsteroidjikasedangtidakberikatandgnliganbisaterdapat di dalamnukleusatauberada di luarnukleusdenganberikatandengansuatuprotein chaperon (pengantar), yaituheat shock proteins (hsps)

  11. Issues and Resolutions • Description of the issue • How was it resolved? • What and how did it impact the project? • Time • Cost • Other

  12. Timeline

  13. Looking Ahead

  14. Appendix • Budget • Design documents • Marketing plan • Supplemental documents • Contact information

  15. PPAR receptor

  16. Bioactive lipids and theirnuclearreceptors

  17. Thank you for attention

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