Retinoid Differentiation Therapy for Common Types of Acute Myeloid Leukemia

Table 1

Preferential binding of synthetic retinoid analogs to subtypes of RAR. The equilibrium binding affinities of each retinoid analog were determined against baculovirus expressed RAR or RXR isoforms by displacement of [³H]-ATRA.

Binding affinities (ED50 in nM) against RARs and RXRs
Retinoid analog	RAR𝛼	RAR𝛽	RAR𝛾	RXRs
RAR agonists
Pan-RAR (AGN191183)	15.7	7.2	6.7	9,113 (𝛼)–2,556 (𝛾)
RAR𝛼 (AGN195183)	20.1	>5,000	>5,000	>10,000
RAR𝛽𝛾 (AGN190168)	>1,000	14.2	135	>10,000
RAR𝛾 (AGN205327)	3,766	734	32	>10,000
RAR antagonists
Pan-RAR (AGN194310)	4.3	5	2	>10,000
RAR𝛼 (AGN196996)	3.9	4,036	>10,000	>10,000
RAR𝛽𝛾 (AGN194431)	300	6	20	>10,000
RAR𝛾 (AGN205728)	2,400	4,248	3	>10,000