PMID- 32359655
OWN - NLM
STAT- MEDLINE
DCOM- 20210623
LR  - 20210623
IS  - 1557-7988 (Electronic)
IS  - 0076-6879 (Linking)
VI  - 637
DP  - 2020
TI  - Design of synthetic retinoids.
PG  - 453-491
LID - S0076-6879(20)30089-6 [pii]
LID - 10.1016/bs.mie.2020.02.011 [doi]
AB  - This chapter has been conceived as an introductory text to aid in the 
      understanding of the key design strategies for the development of synthetic 
      analogs of endogenous retinoids as ligands for the retinoic acid receptors (RARs) 
      and retinoid X receptors (RXRs). The structure and binding characteristics of the 
      endogenous retinoids are first explained to put the main chemical design 
      challenges in context. Existing biochemical and structural data is then used to 
      describe the guiding principles used to develop agonists and antagonists of the 
      RARs and RXRs. In light of the increasing proliferation of biophysical methods 
      that employ fluorescence measurements or molecular tags, we also examine the 
      application of retinoids as probes and the chemical principles required to 
      develop these tools.
CI  - (c) 2020 Elsevier Inc. All rights reserved.
FAU - Chisholm, David R
AU  - Chisholm DR
AD  - LightOx Ltd., Newcastle upon Tyne, United Kingdom. Electronic address: 
      david.chisholm@lightox.co.uk.
FAU - Whiting, Andrew
AU  - Whiting A
AD  - Department of Chemistry, Durham University, Lower Mountjoy, Durham, United 
      Kingdom.
LA  - eng
PT  - Journal Article
DEP - 20200319
PL  - United States
TA  - Methods Enzymol
JT  - Methods in enzymology
JID - 0212271
RN  - 0 (Ligands)
RN  - 0 (Receptors, Retinoic Acid)
RN  - 0 (Retinoid X Receptors)
RN  - 0 (Retinoids)
SB  - IM
MH  - Ligands
MH  - *Receptors, Retinoic Acid
MH  - Retinoid X Receptors
MH  - *Retinoids
MH  - Structure-Activity Relationship
OTO - NOTNLM
OT  - Binding pocket
OT  - CRABP
OT  - Conformation
OT  - H12
OT  - RAR
OT  - RXR
OT  - Retinoid
OT  - Selectivity
OT  - Synthetic design
EDAT- 2020/05/04 06:00
MHDA- 2021/06/24 06:00
CRDT- 2020/05/04 06:00
PHST- 2020/05/04 06:00 [entrez]
PHST- 2020/05/04 06:00 [pubmed]
PHST- 2021/06/24 06:00 [medline]
AID - S0076-6879(20)30089-6 [pii]
AID - 10.1016/bs.mie.2020.02.011 [doi]
PST - ppublish
SO  - Methods Enzymol. 2020;637:453-491. doi: 10.1016/bs.mie.2020.02.011. Epub 2020 Mar 
      19.