GO-203-2C

Investigational

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C89H170N52O20S2
Molecular Weight	2352.768
Optical Activity	UNSPECIFIED
Defined Stereocenters	16 / 16
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CC(=O)N[C@H](CCCNC(N)=N)C(=O)N[C@H](CCCNC(N)=N)C(=O)N[C@H](CCCNC(N)=N)C(=O)N[C@H](CCCNC(N)=N)C(=O)N[C@H](CCCNC(N)=N)C(=O)N[C@H](CCCNC(N)=N)C(=O)N[C@H](CCCNC(N)=N)C(=O)N[C@H](CCCNC(N)=N)C(=O)N[C@H](CCCNC(N)=N)C(=O)N[C@@H]1CSSC[C@@H](NC(=O)[C@@H](CCC(N)=O)NC1=O)C(=O)N[C@H](CCCNC(N)=N)C(=O)N[C@H](CCCNC(N)=N)C(=O)N[C@H](CCCCN)C(=O)N[C@H](CC(N)=O)C(O)=O

InChI

InChIKey=MDQMFOHHSFMREL-YIYMUJAPSA-N

InChI=1S/C89H170N52O20S2/c1-44(142)126-45(16-4-30-115-79(93)94)63(145)128-47(17-5-31-116-80(95)96)65(147)129-49(19-7-33-118-82(99)100)66(148)130-50(20-8-34-119-83(101)102)67(149)131-51(21-9-35-120-84(103)104)68(150)132-52(22-10-36-121-85(105)106)69(151)133-53(23-11-37-122-86(107)108)70(152)134-54(24-12-38-123-87(109)110)71(153)136-56(26-14-40-125-89(113)114)74(156)140-60-43-163-162-42-59(141-75(157)57(138-77(60)159)27-28-61(91)143)76(158)137-55(25-13-39-124-88(111)112)72(154)135-48(18-6-32-117-81(97)98)64(146)127-46(15-2-3-29-90)73(155)139-58(78(160)161)41-62(92)144/h45-60H,2-43,90H2,1H3,(H2,91,143)(H2,92,144)(H,126,142)(H,127,146)(H,128,145)(H,129,147)(H,130,148)(H,131,149)(H,132,150)(H,133,151)(H,134,152)(H,135,154)(H,136,153)(H,137,158)(H,138,159)(H,139,155)(H,140,156)(H,141,157)(H,160,161)(H4,93,94,115)(H4,95,96,116)(H4,97,98,117)(H4,99,100,118)(H4,101,102,119)(H4,103,104,120)(H4,105,106,121)(H4,107,108,122)(H4,109,110,123)(H4,111,112,124)(H4,113,114,125)/t45-,46-,47-,48-,49-,50-,51-,52-,53-,54-,55-,56-,57-,58-,59-,60-/m1/s1

HIDE SMILES / InChI

Description
Sources: https://clinicaltrials.gov/ct2/show/NCT01279603 | https://clinicaltrials.gov/ct2/show/NCT02204085 http://www.bloodjournal.org/content/130/Suppl_1/2659.abstract?sso-checked=true | https://www.cancer.gov/publications/dictionaries/cancer-drug/def/muc1-targeted-peptide-go-2-03-2c

GO-203-2c is a cell-penetrating peptide that binds to MUC1, a protein that causes cancer (oncoprotein). MUC1 is over-expressed in many human cancers, such breast, prostate, lung, colon, pancreas, and ovary cancer, and has been associated with poor prognosis. GO-203-2c blocks homodimerization of the MUC1-C subunit required for nuclear translocation and downstream signaling. This binding eventually leads to cell death (in laboratory setting). Since MUC1 is over-expressed in many cancers, the potential of GO-203-2c in treatment of cancers is being investigated. A phase I clinical trial has been completed in which GO-203-2c was shown to be safe and demonstrating both anti-leukemia and immunomodulatory effects. A phase II study is investigating its potential in the treatment of Acute Myeloid Leukemia.

Approval Year

Name

Type

Language

GO-203-2C

Code

English

ACETYL-D-ARGINYL-D-ARGINYL-D-ARGINYL-D-ARGINYL-D-ARGINYL-D-ARGINYL-D-ARGINYL-D-ARGINYL-D-ARGINYL-D-CYSTEINYL-D-GLUTAMINYL-D-CYSTEINYL-D-ARGINYL-D-ARGINYL-D-LYSYL-DASPARAGINYLAMIDE DISULFIDE

Common Name

English

Classification Tree Code System Code

FDA ORPHAN DRUG

494415