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Discovery of potent and selective D3 antagonist with alleviated hERG liability and optimized pharmacokinetic properties
One of the most challenging hurdles in creating safe and effective new medicines for many diseases is finding drugs that are effective without causing off-target cardiac issues, such as cardiac arrythmias. In collaboration with NIDA, scientists at NCATS have developed a series of novel and highly specific dopamine D3 receptor agonists and antagonists...
Published: 6/13/2025
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Inventor(s):
Khalida Shamim
,
Wenwei Huang
,
Wei Zheng
,
Catherine Chen
,
Xiuli Huang
,
Xin Hu
,
Xin Xu
,
Pranav Shah
,
Elias Padilha
,
Philip Sanderson
,
Amy Newman
Keywords(s):
Category(s):
Application > Therapeutics
,
Collaboration Sought > Licensing
,
Collaboration Sought > Materials Available
,
TherapeuticArea > Neurology
,
TherapeuticArea > Psychiatry/Mental Health
First in class Small Molecule Agonists of the mammalian Relaxin family receptor 1 (RXFP1) and use in treatment of cancer, fibrotic, and vascular disorders (HHS Ref No. E-145-2024-0-US-02)
It is well documented in literature that activation of RXFP1 by relaxin induces: 1) up-regulation of the endothelin system which leads to vasodilation; 2) extracellular matrix remodeling through regulation of collagen deposition, cell invasiveness, proliferation, and overall tissue homeostasis; 3) a moderation of inflammation by reducing levels of inflammatory...
Published: 5/30/2025
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Inventor(s):
Juan Marugan
,
Mark Henderson
,
Kenneth Wilson
,
Wenwei Huang
,
Wenjuan Ye
,
Noel Southall
,
Jiankang Jiang
,
Khalida Shamim
,
Bing Li
,
Alexander Agoulnik
,
Abhijeet Kapoor
,
Joshua Hutcheson
,
Ana Cabrera
,
Irina Agoulnik
Keywords(s):
Category(s):
Application > Therapeutics
,
Application > Research Materials
,
TherapeuticArea > Oncology
,
TherapeuticArea > Cardiology
,
TherapeuticArea > Pulmonology
,
TherapeuticArea > Dermatology
,
TherapeuticArea > Reproductive Health
,
TherapeuticArea > Geriatrics
Novel ACRV1/ALK2 Inhibitors and Methods for Inhibiting BMP Signaling for the Treatment of Fibrodysplasia Ossificans Progressiva (FOP)
This technology includes the identification and use of novel ACRV1/ALK2 inhibitors for the treatment of fibrodysplasia ossificans progressiva (FOP), an autosomal-dominant rare disease that affects one person in every 1-2 million. FOP is characterized by malformation of the great (big) toes during embryonic development and by progressive heterotopic...
Published: 10/28/2024
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Inventor(s):
Jian-kang Jiang
,
Khalida Shamim
,
Philip Sanderson
,
Wei Zheng
,
Xiuli Huang
,
Gregory Tawa
,
Asaf Alimardanov
,
Arthur Lee
,
Junfeng Huang
,
Wenwei Huang
Keywords(s):
ALK2
,
BMP
,
INHIBITING
,
Inhibitors
,
Methods
,
Novel
,
SIGNALING
,
VGXXXX
,
WIXXXX
,
WKXXXX
,
XEXXXX
Category(s):
TherapeuticArea > Endocrinology
,
Application > Therapeutics
,
Application > Research Materials
Repurposed Use of the Alkaloids Emetine and Cephaeline to Treat Zika Virus Infection
This technology includes the use of two related compounds, Emetine and Cephaeline, as a potent inhibitor of the Zika virus (ZIKV). Emetine and it's analog Cephaeline were identified in a high-throughput assay aimed at identifying anti-ZIKV compounds. Both Emetine and Cephaeline are potent inhibitors of ZIKV infection in cell culture, and Emeline is...
Published: 10/28/2024
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Inventor(s):
Emily Lee
,
Wei Zheng
,
Miao Xu
,
Ruili Huang
,
Shu Yang
,
Wenwei Huang
,
Khalida Shamim
,
Hao Li
,
Hengli Tang
Keywords(s):
compounds
,
Emetine
,
Flavivirus
,
Infection
,
Prevention
,
treatment
,
VLXXXX
,
WIXXXX
,
WKXXXX
Category(s):
Application > Therapeutics
,
TherapeuticArea > Infectious Disease
,
Application > Research Materials
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