# US 2009/0156466 A1 · Characterization of a MEKK binding site and uses thereof

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- Number: US 2009/0156466 A1
- Document ID: US20090156466A1
- Status: Published application
- Kind: A1
- Application number: 12/078,808
- Filed: 2008-04-04
- Published: 2009-06-18
- Earliest claimed: 2007-04-05
- Inventors: Michael P. Scheid
- Web page: https://patentgrep.com/patent/US20090156466A1

## CPC

- C12N 9/1205: {Phosphotransferases with an alcohol group as acceptor (2.7.1), e.g. protein kinases}
- A61K 38/45: Transferases (2)
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 37/02: Immunomodulators
- C07K 16/40: against enzymes
- G01N 33/573: for enzymes or isoenzymes
- A01K 2217/075: inducing loss of function, i.e. knock out
- A01K 2267/0368: Animal model for inflammation
- C12N: MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA (microbiological testing media C12Q1/00)
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C07K: PEPTIDES (peptides in foodstuffs A23; obtaining protein compositions for foodstuffs, working-up proteins for foodstuffs A23J; preparations for medicinal purposes A61K; peptides containing beta-lactam rings C07D; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, C07D; ergot alkaloids of the cyclic peptide type C07D519/02; macromolecular compounds having statistically distributed amino acid units in their molecules, i.e. when the preparation does not provide for a specific; but for a random sequence of the amino acid units, homopolyamides and block copolyamides derived from amino acids C08G69/00; macromolecular products derived from proteins C08H1/00; preparation of glue or gelatine C09H; single cell proteins, enzymes C12N; genetic engineering processes for obtaining peptides C12N15/00; compositions for measuring or testing processes involving enzymes C12Q; investigation or analysis of biological material G01N33/00)
- G01N: INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES (measuring or testing apparatus or processes other than immunoassay, involving enzymes or microorganisms C12M, C12Q)
- A01K: ANIMAL HUSBANDRY; AVICULTURE; APICULTURE; PISCICULTURE; FISHING; REARING OR BREEDING ANIMALS, NOT OTHERWISE PROVIDED FOR; NEW BREEDS OF ANIMALS

## Abstract

The present invention provides binding motifs, binding sites, peptides, and 14-3-3/MEKK complexes. Also provided are agents reactive with same, pharmaceutical compositions, molecules, and kits comprising same, and methods of producing same. The present invention further provides isolated nucleic acids and constructs comprising same, host cells comprising the constructs, and transgenic non-human animals. Additionally, the present invention provides methods of: (a) facilitating or inhibiting 14-3-3/MEKK interaction, (b) regulating MEKK activity, (c) identifying agents that interact with MEKK or 14-3-3, (d) detecting and monitoring the development of MEKK-mediated conditions, and (e) treating and/or preventing MEKK-mediated conditions.

## Claims

### Claim 1

A binding motif of a MERK polypeptide capable of binding a 14-3-3 polypeptide, said motif comprising an amino acid sequence that includes a threo-nine capable of phosphorylation.

### Claim 2 (depends on 1)

The binding motif of claim 1, wherein the threonine is phosphorylated.

### Claim 3

(canceled)

### Claim 4 (depends on 1)

The binding motif of claim 1, wherein the MEKK polypeptide is MEKK3.

### Claim 5 (depends on 4)

The binding motif of claim 4, wherein the MEKK polypeptide is human MEKK3.

### Claim 6 (depends on 4)

The binding motif of claim 4, wherein the amino acid sequence comprises the sequence RRTFP.

### Claim 7 (depends on 6)

The binding motif of claim 6, wherein the amino acid sequence comprises the sequence GRRTFPR.

### Claim 8 (depends on 7)

The binding motif of claim 7, wherein the amino acid sequence comprises the sequence YSDGRRTFPRIRR.

### Claim 9 (depends on 4)

The binding motif of claim 4, wherein the threonine is phosphorylated.

### Claim 10 (depends on 9)

The binding motif of claim 9, wherein the phosphorylated threonine corresponds to a threonine residue at position 294 of human MEKK3 (isoform 2) or position 345 of human MEKK3 (isoform 1).

### Claim 11 (depends on 1)

The binding motif of claim 1, wherein the MEKK polypeptide is MEKK2.

### Claim 12 (depends on 11)

The binding motif of claim 11, wherein the MEKK polypeptide is human MEKK2.

### Claim 13

(canceled)

### Claim 14 (depends on 11)

The binding motif of claim 11, wherein the amino acid sequence comprises the sequence GRKTFPR.

### Claim 15 (depends on 14)

The binding motif of claim 14, wherein the amino acid sequence comprises the sequence YNDGRKTFPRARR.

### Claim 16

(canceled)

### Claim 17

(canceled)

### Claim 18

(canceled)

### Claim 19

(canceled)

### Claim 20

(canceled)

### Claim 21

(canceled)

### Claim 22

(canceled)

### Claim 23

(canceled)

### Claim 24

(canceled)

### Claim 25

(canceled)

### Claim 26

(canceled)

### Claim 27

(canceled)

### Claim 28

(canceled)

### Claim 29

(canceled)

### Claim 30

(canceled)

### Claim 31

(canceled)

### Claim 32 (depends on 1)

A method of treating and/or preventing a MEKK-mediated condition in a subject, comprising modulation phosphorylation of a MEKK polypeptide in the subject, wherein the MEKK polypeptide includes the binding motif of claim 1 and phosphorylation of the threonine is modulated.

### Claim 33

(canceled)

### Claim 34

(canceled)

### Claim 35

(canceled)

### Claim 36

(canceled)

### Claim 37

(canceled)

### Claim 38

(canceled)

### Claim 39

(canceled)

### Claim 40

(canceled)

### Claim 41

(canceled)

### Claim 42

(canceled)

### Claim 43

(canceled)

### Claim 44

(canceled)

### Claim 45

(canceled)

### Claim 46

(canceled)

### Claim 47

(canceled)

### Claim 48

(canceled)

### Claim 49

(canceled)

### Claim 50

(canceled)

### Claim 51

(canceled)

### Claim 52

(canceled)

### Claim 53

(canceled)

### Claim 54

(canceled)

### Claim 55

(canceled)

### Claim 56

(canceled)

### Claim 57

(canceled)

### Claim 58

(canceled)

### Claim 59

(canceled)

### Claim 60

(canceled)

### Claim 61

(canceled)

### Claim 62

(canceled)

### Claim 63

(canceled)

### Claim 64

(canceled)

### Claim 65

(canceled)

### Claim 66

(canceled)

### Claim 67

(canceled)

### Claim 68

(canceled)

### Claim 69

(canceled)

### Claim 70

(canceled)

### Claim 71

(canceled)

### Claim 72

(canceled)

### Claim 73

(canceled)

### Claim 74

(canceled)

### Claim 75

(canceled)

### Claim 76

(canceled)

### Claim 77

(canceled)

### Claim 78

(canceled)

### Claim 79

(canceled)

### Claim 80

(canceled)

### Claim 81

(canceled)

### Claim 82

(canceled)

### Claim 83

(canceled)

### Claim 84

(canceled)

### Claim 85

(canceled)

### Claim 86

(canceled)

### Claim 87

(canceled)

### Claim 88

(canceled)

### Claim 89

(canceled)

### Claim 90

(canceled)

### Claim 91

(canceled)

### Claim 92 (depends on 32)

The method of claim 32, wherein the MEKK is MEKK2 or MEKK3.

### Claim 93 (depends on 32)

The method of claim 32, wherein the subject is a human.

### Claim 94

(canceled)

### Claim 95

(canceled)

### Claim 96

(canceled)

### Claim 97

(canceled)

### Claim 98 (depends on 32)

The method of claim 32, wherein the MEKK-mediated condition is a chronic inflammatory disease or a condition associated with expression of pro-inflammatory cytokines.

### Claim 99 (depends on 98)

The method of claim 98, wherein the MEKK-mediated condition is an autoimmune disorder.

### Claim 100 (depends on 99)

The method of claim 99, wherein the autoimmune disorder is arthritis, asthma, or lupus.

### Claim 101 (depends on 98)

The method of claim 98, wherein the MEKK-mediated condition is arthritis.

### Claim 102

(canceled)

### Claim 103

(canceled)

### Claim 104

(canceled)

### Claim 105

(canceled)

### Claim 106

(canceled)

### Claim 107

(canceled)

### Claim 108

(canceled)

### Claim 109

(canceled)

### Claim 110

(canceled)

### Claim 111

(canceled)

### Claim 112

(canceled)

### Claim 113

(canceled)

### Claim 114

(canceled)

### Claim 115

(canceled)

### Claim 116

(canceled)

### Claim 117

(canceled)

### Claim 118

(canceled)

### Claim 119

(canceled)

### Claim 120

(canceled)

### Claim 121

(canceled)

### Claim 122

(canceled)

### Claim 123

(canceled)

### Claim 124

(canceled)