Breaking News
October 15, 2018 - Research reveals how the inner ear processes speech
October 15, 2018 - Many parents still skeptical about safety and effectiveness of flu shot, survey finds
October 15, 2018 - Payer Policies May Discourage Non-Pharma Tx for Low Back Pain
October 15, 2018 - Exercise may delay cognitive decline in people with rare Alzheimer’s disease
October 15, 2018 - Researchers modify CRISPR to reorganize genome | News Center
October 15, 2018 - Innovative brain tumor operation set to tailor to patients’ needs
October 15, 2018 - Findings offer new insight into early changes that occur during AD pathology
October 15, 2018 - Neurons regulating reproductive hormone release have different activity in epileptic mice
October 15, 2018 - More parents are concerned about taking babies swimming in public pools
October 15, 2018 - Health Tip: Know the Risk Factors for Lower Back Pain
October 15, 2018 - Study shows cigarillo flavors enhanced by high-intensity sweeteners
October 15, 2018 - Study traces hospital-acquired bloodstream infections to patients’ own bodies | News Center
October 15, 2018 - Abnormal vision in childhood can affect development of brain areas responsible for attention
October 15, 2018 - Color-changing contact lens could help doctors to monitor eye disease medications
October 15, 2018 - Tobacco heating products cause less staining to teeth than conventional cigarettes
October 15, 2018 - Young adults who are obese can expect to lose up to 10 years in life expectancy
October 15, 2018 - Scientists uncover how proteins meet on the cell membrane
October 15, 2018 - Affordable housing with supportive social services for senior citizens can reduce hospital use
October 15, 2018 - The latest ECG device from Schiller
October 15, 2018 - Following a Tissue Sample
October 15, 2018 - Prisoners need drug and alcohol treatments but AA programs aren’t the answer
October 15, 2018 - Andrea Califano and Jordan Orange Elected to National Academy of Medicine
October 15, 2018 - The impending risk of African Swine Fever Virus
October 15, 2018 - Breastfeeding reduces the number of antibiotic-resistant bacteria in infant gut
October 15, 2018 - Researchers develop comprehensive molecular atlas of postnatal mouse heart development
October 15, 2018 - ObsEva SA Presents Clinical Data from Phase III IMPLANT 2 Trial of Nolasiban in IVF at the American Society of Reproductive Medicine (ASRM) Annual Meeting
October 15, 2018 - Engineering teratoma-derived fibroblasts to enhance osteogenesis
October 15, 2018 - Lab study shows effectiveness of potential therapy for treatment-resistant hypothyroidism
October 15, 2018 - JCU study firms up association between diet and depression
October 15, 2018 - Researchers to study the use of CRISPR on human liver on-a-chip platform
October 15, 2018 - Sub-concussive impacts not associated with decline in neurocognitive function
October 15, 2018 - Researchers find potential treatment to halt premature labor and birth
October 15, 2018 - As U.S. suicides rates rise, Hispanics show relative immunity
October 15, 2018 - FDA Issues a Complete Response Letter to Acacia Pharma for Barhemsys
October 15, 2018 - Photoactive bacteria bait may help in fight against MRSA infections
October 15, 2018 - Increasing vigorous exercise reduces risk factors of type 2 diabetes, cardiovascular disease in children
October 15, 2018 - First-of-its-kind study to test a personalized vaccine in cancer patient
October 15, 2018 - Extension trial assesses benefit of switching from flash monitoring to RT-CGM for hypoglycemia
October 15, 2018 - Half of parents say young children are afraid of doctor’s visits
October 15, 2018 - Study shows how fingerprint-based drug screening works on the living and deceased
October 15, 2018 - Study reveals potential to monitor progression of Alzheimer’s disease by measuring brain antioxidant levels
October 15, 2018 - FDA Approves Xarelto to Reduce the Risk of Major Cardiovascular Events in Patients with Chronic Coronary Artery Disease (CAD) or Peripheral Artery Disease (PAD)
October 15, 2018 - Promising new therapeutic approach against Ebola virus identified
October 15, 2018 - Study unravels how cancer stem cells use normal genes in abnormal ways
October 15, 2018 - Healthcare systems fail to deliver at affordable prices finds report
October 15, 2018 - Intensive BP Therapy in Diabetes May Lower Risk for CV Events
October 15, 2018 - Muscle relaxants increase risk of respiratory complications
October 15, 2018 - Female birds become more promiscuous after hatchings fail in the first breeding attempt
October 15, 2018 - Humans occupied Madagascar thousands of years later than previously thought
October 15, 2018 - Is Kidney Dialysis Always Needed When Septic Shock Strikes?
October 15, 2018 - Study shows invasive lung cancer surgery can lead to long-term opioid use
October 15, 2018 - Sugar, a “sweet” tool to understand brain injuries
October 14, 2018 - King’s commemorates activities and research on World Arthritis Day
October 14, 2018 - Humana and VFW NY team up on Stop 22 initiative to increase awareness of veterans committing suicide
October 14, 2018 - Water fluoridation contributes to urinary fluoride levels in pregnant women in Canada
October 14, 2018 - Study of children in Romanian orphanages tells cautionary tale about family separation
October 14, 2018 - Previous Endologix AFX Safety Notice classified by FDA as Class I recall
October 14, 2018 - Legal scholars sound alarm on academies’ report about returning research results to participants
October 14, 2018 - UNIST selects six extraordinary scholars to be induced as ‘Rising-star Distinguished Professor’
October 14, 2018 - Scientists find new way to help asthmatics breathe more easily
October 14, 2018 - New ‘gag rule’ may adversely impact health care of pregnant women
October 14, 2018 - Rosacea – Genetics Home Reference
October 14, 2018 - When the fighting crosses the line
October 14, 2018 - New findings could benefit patients with triple-negative breast cancer
October 14, 2018 - UK Biobank provides wealth of information for further genetic studies
October 14, 2018 - KHN’s ‘What the Health?’ Falling premiums and rising political tensions
October 14, 2018 - Duvelisib Promising for Chronic Lymphocytic Leukemia, SLL
October 14, 2018 - Tailored drug cocktails offer hope to kids with aggressive brain tumors
October 14, 2018 - Common gene variants linked to migraine risk in African-American children
October 14, 2018 - Funding requests are being accepted by BlueCross BlueShield of Tennessee Community Trust
October 14, 2018 - Using pulsed electric fields in cancer therapy
October 14, 2018 - Major Childbirth Complications More Likely for Black Women
October 14, 2018 - Young cancer survivors at greater risk of mental health disorders
October 14, 2018 - Common herbicide compound could help fight hospital-acquired fungal infections
October 14, 2018 - Alterations in genes encoding proteins contribute to ADHD development
October 14, 2018 - New patient-centric website launched in Europe to empower people with chronic conditions
October 14, 2018 - Antimicrobial signaling molecule has lower activity against hepatitis C virus in most humans
October 14, 2018 - Genomic dark matter activity connects Parkinson’s and psychiatric diseases
October 14, 2018 - Cornell dots equipped with antibody fragments offer a new cancer weapon
October 14, 2018 - Addressing social and cultural factors is key to reducing burden of type 2 diabetes
Stevens researchers develop new class of molecules for breast cancer treatment

Stevens researchers develop new class of molecules for breast cancer treatment

image_pdfDownload PDFimage_print

Researchers at Stevens Institute of Technology and colleagues have designed and developed a new class of molecules that use a never-before-known mechanism that may halt or destroy breast cancer tumors, particularly for patients with drug-resistant or dangerously metastatic stages of the disease.

The molecule, developed by Abhishek Sharma, a chemistry professor at Stevens, could potentially add to the arsenal of drugs actively being developed to degrade or inhibit estrogen receptors, proteins inside cells that have been proven to be the single most important target in breast cancer therapy over the last 30 years.

“The unique benefit of our compounds is that this is a fundamentally different type of structure that was previously not known to degrade or inhibit estrogen receptors,” said Sharma, whose work was recently published in the journal ACS Medicinal Chemistry Letters. “It’s not a tweak of an existing drug; it works in a completely different way.”

Several big pharma companies have invested heavily into developing such drugs, known as selective estrogen receptor degraders, or SERDs, due to the huge market potential and unmet clinical need. However, their approach has focused primarily on modifying the structure of SERDs that were originally discovered decades ago.

The problem: many breast cancer tumors become resistant to these drugs, necessitating more toxic chemotherapies to prevent the cancer from relapsing and progressing. SERDs are also difficult to formulate into pills, and treatment requires large, painful injections directly into a patient’s muscles. More recently, drugs in clinical trials have been pulled because of side effects.

Sharma’s team, including cancer biologists and physicians at Memorial Sloan Kettering Cancer Center in New York and at the University of Illinois, wanted to find a better way to treat breast cancer, which afflicts one in eight U.S. women and tens of millions worldwide.

They took a core substance already known to act as a good “homing device” for estrogen receptors and attached it to a series of experimental side-chain compounds known as degrons. Once the homing device attached to the estrogen receptor, the degrons degraded it by way of hijacking a cancer cell’s protein-disposal machinery and routing it to the receptor (a protein).

The team went a step further, synthesizing several variations of the novel compound, each taking weeks to months to design and produce. They then tested more than a dozen of them to see how they interacted with the cancer cells’ estrogen receptors. The new compounds were found to deliver a one-two punch, not only degrading estrogen receptors and inhibiting the signals that cue the cell to grow, but also blocking the hormone estrogen from binding to it. Importantly, the compounds also strongly inhibited the growth and proliferation of breast cancer cells.

“We consider these results to be very promising,” said Sharma. “This is a novel molecular structure, and several analogs produced excellent early activity.”

Next, the Stevens team will select several of the most promising candidates from the new compounds and develop them into more potent drug candidates to test in mouse models.

Source:

https://www.stevens.edu/news/novel-molecule-could-spur-new-class-drugs-breast-cancer

Tagged with:

About author

Related Articles