Lecture 77 Flashcards

1
Q

Ligand Binding Domain

A

Low AA identity. Also involved in receptor dimerization, interaction with other proteins, and nuclear localization

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2
Q

DNA binding domain

A

High AA identity.

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3
Q

How is AF-1 (transcriptional activation function 1) activated?

A

Phosphorylation

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4
Q

How is AF-2 (transcriptional activation function 2) activated?

A

Ligand binding

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5
Q

Name five types of type I nuclear receptors.

A
Estrogen (ER)
Androgen (AR)
Glucocorticoid (GR)
Progesterone (PR)
Mineralocorticoid (MR)
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6
Q

Name seven types of type II nuclear receptors

A
Thyroid hormone (TR)
Vitamin D (VDR)
Retinoic acid (RAR)
Retinoid X (RXR)
Peroxisome proliferator-activated (PPAR)
Liver X (LXR)
Farnesoid X (FXR)
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7
Q

What is the ligand for RXR?

A

9cisRA

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8
Q

What is the ligand for PPARa?

A

Fibrates

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9
Q

What is the ligand for PPARg?

A

Glitazones

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10
Q

What is the ligand for PXR?

A

Xenobiotics

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11
Q

What is the ligand for LXR?

A

Oxysterols

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12
Q

What is the ligand for FXR?

A

Bile Acids

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13
Q

What is the ligand for VDR?

A

1,25-dihydroxy vitamin D3

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14
Q

What is the ligand for RAR?

A

All-trans retinoic acid

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15
Q

What are characteristics of Type I ligands?

A
  • All are derived from cholesterol
  • High specificity and affinity
  • pM to nM concentrations in serum
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16
Q

What are characteristics of Type II ligands?

A
  • Low specificity and affinity
  • “promiscuous”
  • present in uM to mM concentrations in serum
17
Q

How do NRs bind DNA?

A

Zinc finger motifs