Table 1 hERα-LBD variants used in this study.

From: A PROSS-designed extensively mutated estrogen receptor α variant displays enhanced thermal stability while retaining native allosteric regulation and structure

hERα variant

Substitutions precluding cysteine oxidationa

Substitutions stabilizing distinct conformational statesb

Substitutions suggested by PROSSc

Agonist-bound

Antagonist-bound

ERWT*

C381S, C417S, C530S

   

ERPRS*

C381S, C417S, C530S

  

M315I, V316I, D321E, T334S, S341Y, R363K, T371S, E397D, N407D, N413E, S433E, M437E, N439K, G442R, S450A, E471N, D473E, H474K, V478M, T485A, H488W, L489Y, A493S, T496S

ERPRS*(+)

C381S, C417S, C530S

Y537S

 

ERPRS*(−)

C381S, C417S, C530S

 

L372R

L536S

  1. aAA substitutions with respect to UNIPROT entry P03372-148.
  2. bAs suggested by Bruning et al.4 and Nettles et al.32.
  3. cCampeotto et al.25.
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