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. 2021 Aug 26;22(17):9223. doi: 10.3390/ijms22179223

Figure 24.

Figure 24

(A) Structural development of a hPPARγ-selective partial agonist from a hPPARγ pan agonist. (B–E) X-ray crystallographic structure of the homo-dimeric structure of MEKT-75 complexed with the hPPARγ LBD. (B) Homo-dimeric structure of MEKT-75 complexed with the hPPARγ LBD. (C) Full agonist form monomer. (D) Partial agonist form monomer. (E) Superposed structure of the homo-dimeric structure of MEKT-75 complexed with the hPPARγ LBD. MEKT-75 was omitted. (F) Superposed structure of the partial agonist form MEKT-75 monomer and the TIPP-703 monomer complexed with the hPPARγ LBD. (G) Partial agonist form MEKT-75 monomer. (H) Overall structure of TIPP-703 complexed with the hPPARγ LBD. (I) Superposed structure of the full agonist form MEKT-75 monomer and the TIPP-703 monomer complexed with the hPPARγ LBD. (J) Partial agonist form MEKT-75 monomer. (K) Overall structure of TIPP-703 complexed with the hPPARγ LBD. (K,L) (left) Zoomed view of the fully active form of MEKT-75. (right) Zoomed view of the non-fully active form of MEKT-75.