Immuno-oncology에서 Small molecules의 장점

  • 단백질 기반 체료제가 접근할수 없는 intracellular target 가능
  • 높은 Oral bioavailability
  • 국소 tumor microenvironment에 high level로 도달 가능
  • immune checkpoint blocker에 의해 직접적으로 조절되지 않는, immunesuppressive cell 타입들에도 적용 가능.
Cat. No. Product Name Action Description

3700

Imiquimod

TLR7 agonist

TRL7 activation induces release of proinflammatory cytokines and activation of NF-κB signaling. Imiquimod activates antigen presenting cells and antitumor cellular immune response.

5698

1-Methyl-D-tryptophan

IDO inhibitor

IDO activity in tumors inhibits proliferation and induces apoptosis of T-cells. Inhibition with 1-Methyl-D-tryptophan enhances the antitumor immune response of T-cells in vitro.

5794

LM 10

TDO inhibitor

TDO is expressed in tumors and prevents immune rejection of tumor cells. Inhibition with LM 10 restores ability of mice to reject TDO expressing tumors.

5872

AZ 10397767

CXCR2 antagonist

 

CXCR2 ligands recruit neutrophils to tumors. Antagonism with AZ 10397767 reduces recruitment both in vitro and in vivo and is associated with slower growing tumors.

5945

2’,3’-cGAMP sodium salt

STING agonist

 

2’,3’-cGAMP binds to stimulator of interferon genes (STING) to activate the innate immune response. Causes repolarization of TAMs to antitumor phenotype.

6007

INCB 024360-analog

IDO inhibitor

 

Inhibition of IDO with INCB 024360-analog enhances antitumor immune response and inhibits tumor growth in vivo.

6083

PSB 12379

Ecto-5'-nucleotidase (CD73) inhibitor

 

CD73 catalyzes hydrolysis of extracellular AMP to adenosine, which causes local immunosuppression via adenosine receptors. Inhibition with PSB 12379 causes immune response in tumor microenvironment.


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-2018년 07월 09일-