EP 0618927 A4 19950524 - CYTOKINES WITH AN UNPAIRED CYSTEINE RESIDUE AND CONJUGATES THEREOF.

Title (en)

CYTOKINES WITH AN UNPAIRED CYSTEINE RESIDUE AND CONJUGATES THEREOF.

Title (de)

CYTOKINE MIT EINEM UNGEPAARTEN CYSTEIN-REST UND KONJUGATEN DAVON.

Title (fr)

CYTOKINES DOTEES D'UN RESIDU DE CYSTEINE NON APPARIE ET LEURS PRODUITS DE CONJUGAISON.

Publication

EP 0618927 A4 19950524 (EN)

Application

EP 93901259 A 19921210

Priority

US 9210889 W 19921210
US 80545291 A 19911210

Abstract (en)

[origin: WO9312142A1] Disclosed are cytokines which are site-specifically mutated to have one unpaired cysteine residue located apart from the receptor-binding site, and conjugates thereof, in particular, conjugates where a lipophilic group is conjugated to the unpaired cysteine residue, and to such conjugates of cytokines which have an unpaired cysteine residue located apart from the receptor-binding site in the native form. All of these cytokines are of the type such that conjugation of a lipophilic group to the unpaired cysteine residue does not significantly affect the receptor binding or biological acitivity of the conjugated product. Also disclosed are conjugates where a lipophilic group, an antibody, horseradish peroxidase, alkaline phosphatase, fluorescein substances, biotin, or a cytotoxin is conjugated to the unpaired cysteine residue. These fatty acyl conjugated cytokines penetrate better and are retained longer in local sites and can be locally administered to treat, e.g., solid tumors, spinal injuries, the external genital area, the throat, ears, nasal linings, eyes, and skin.

IPC 1-7

C07K 13/00; A61K 45/05

IPC 8 full level

A61K 38/00 (2006.01); A61K 38/19 (2006.01); A61K 38/21 (2006.01); A61K 47/48 (2006.01); A61P 43/00 (2006.01); C07K 1/02 (2006.01); C07K 1/107 (2006.01); C07K 1/113 (2006.01); C07K 14/48 (2006.01); C07K 14/485 (2006.01); C07K 14/52 (2006.01); C07K 14/525 (2006.01); C07K 14/53 (2006.01); C07K 14/54 (2006.01); C07K 14/545 (2006.01); C07K 14/55 (2006.01); C07K 14/555 (2006.01); C07K 14/56 (2006.01); C07K 14/57 (2006.01); C07K 14/575 (2006.01); C07K 14/65 (2006.01); C07K 16/00 (2006.01); C07K 19/00 (2006.01)

CPC (source: EP)

A61K 38/212 (2013.01); A61K 47/51 (2017.07); A61K 47/557 (2017.07); A61P 43/00 (2017.12); C07K 14/52 (2013.01); C07K 14/555 (2013.01)

Citation (search report)

[XY] EP 0458064 A2 19911127 - AMERICAN CYANAMID CO [US]
[XY] WO 9012874 A2 19901101 - GENETICS INST [US]
[Y] EP 0236987 A2 19870916 - TAKEDA CHEMICAL INDUSTRIES LTD [JP]
[Y] EP 0354992 A2 19900221 - YEDA RES & DEV [IL]
[Y] WO 9112229 A1 19910822 - CA NAT RESEARCH COUNCIL [CA]
[Y] EP 0441765 A1 19910814 - UNIV WASHINGTON [US]
[Y] EP 0105777 A1 19840418 - CENTRE NAT RECH SCIENT [FR]
[DY] WILCOX ET AL: "THE MAJORITY OF CELLULAR FATTY ACID ACYLATED PROTEINS ARE LOCALIZED TO THE CYTOPLASMIC SURFACE OF THE PLASMA MEMBRANE", BIOCHEMISTRY, vol. 26, 1987, WASHINGTON D.C.,USA, pages 1029 - 1036
See references of WO 9312142A1

Designated contracting state (EPC)

AT BE CH DE DK ES FR GB GR IE IT LI LU MC NL PT SE

DOCDB simple family (publication)

WO 9312142 A1 19930624; AU 3323593 A 19930719; AU 666914 B2 19960229; CA 2124672 A1 19930624; EP 0618927 A1 19941012; EP 0618927 A4 19950524; JP 2704214 B2 19980126; JP H07502508 A 19950316

DOCDB simple family (application)

US 9210889 W 19921210; AU 3323593 A 19921210; CA 2124672 A 19921210; EP 93901259 A 19921210; JP 51116393 A 19921210