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For equilibrium dimerization models with identical K3 values of modulator binding to the dimer, a decrease in the EC50 for dimerization and an increase in positive cooperativity is observed when a second binding site is present.
Finally, the C-terminal glycine of Atg12 covalently binds to the Lys149 side chain of Atg5 before binding to the dimer protein Atg16 to form the E3-like complex45.
The intrinsic KD (K3) values for CYTZ and TCMZ binding to the dimer show the same 10-fold difference as the EC50 for dimerization (∼5 μM and 50 μM, respectively).
The detailed rationale is given in the supplementary data, but the affinity for modulator binding to the dimer would need to be several orders of magnitude higher than binding to the monomer for the data to fit (SI Figure S5).
EC50 values for modulator binding to the dimer are comparable to values found previously for other thiazides (BPAM-97, ∼5 μM; IDRA-21, ∼460 μM) binding to the constitutive (L483Y) LBD dimer using isothermal titration calorimetry (ITC).
Alternatively, small molecules also activate procaspase 3 allosterically through binding to the dimer interface [ 6] or other sites [ 4], presumably by a similar mechanism of releasing the IL from the interface.
Similar(53)
(D ) Biochemical analyses indicating weaker IκBα binding to the RelA p52 dimer.
This exchange enables the 'release' of the Gα subunit from its tight binding to the Gβγ dimer subunit.
One model for the assembly of the CBF3 complex (Russell et al, 1999) requires that an initial association of Ctf13 and Skp1 occur, followed by binding to the Cep3 dimer, and subsequently Ndc10 and centromeric DNA.
If monomeric SwHaCE also binds SwH-NOX, there may be a complex equilibrium involving dimerization of SwHaCE, monomeric association of the SwH-NOX/ SwHaCE complex, and two monomers of SwH-NOX binding to the SwHaCE dimer to form the final heterotetrameric species.
It has been reported that IRAK-M inhibits IRAK signaling by binding to the IRAK-1/IRAK-4 dimer assembled on the receptor-bound MyD88, thereby preventing IRAK-1/TRAF6 downstream signaling [ 9].
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