PT-141 (20mg – 100mg)

PT-141 (Bremelanotide)

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Peptide Partners Manufacturer Id: VI32

Batch Id: PT202512

Research Studies

(for educational purposes only)

Melanocortin Receptors, Melanotropic Peptides and Penile Erection

Title: Melanocortin Receptors, Melanotropic Peptides and Penile Erection

Authors: Stephen H King, Alexander V Mayorov, Preeti Balse-Srinivasan, Victor J Hruby, Todd W Vanderah, Hunter Wessells

URL: https://pmc.ncbi.nlm.nih.gov/articles/PMC2694735/

Published: Current Topics in Medicinal Chemistry, 2007;7(11):1098–1106

PT-141 (Bremelanotide) is a synthetic heptapeptide that represents a deaminated derivative and likely metabolite of melanotan-II (MT-II). This compound demonstrates strong binding affinity to melanocortin receptors 1, 3, and 4, with a higher affinity for MC4R over MC3R. Application of PT-141 to HEK-293 cells expressing MC4R increases cyclic adenosine monophosphate (cAMP) production, indicating that this compound, like MT-II, acts as an agonist at melanocortin receptors. This in vitro cell culture study demonstrated receptor activation through the cAMP signaling pathway, which is a key second messenger system in G-protein coupled receptor signaling. The study utilized human embryonic kidney cells (HEK-293) transfected to express the melanocortin-4 receptor, providing direct evidence of PT-141’s agonist activity at this receptor subtype through measurement of intracellular cAMP accumulation.

In plain English

This research showed that PT-141 works by binding to and activating specific protein receptors on cell surfaces called melanocortin receptors. When PT-141 attaches to these receptors on cells grown in laboratory dishes, it triggers a chain reaction inside the cells that produces more of a chemical messenger called cAMP. This proves that PT-141 functions as an activator (agonist) of these receptors, particularly the MC4R type, which is important for understanding how the drug might work in the body to affect sexual function and other processes controlled by these receptors.

Melanocortin Receptor Agonist Bremelanotide Induces Cell Death and Growth Inhibition in Glioblastoma Cells via Suppression of Survivin Expression

Title: Melanocortin Receptor Agonist Bremelanotide Induces Cell Death and Growth Inhibition in Glioblastoma Cells via Suppression of Survivin Expression

Authors: Shuhei Suzuki, Chifumi Kitanaka, Masashi Okada

URL: https://ar.iiarjournals.org/content/44/9/3875

Published: Anticancer Research, September 2024, 44(9):3875-3883

The effects of bremelanotide, a melanocortin receptor agonist, were investigated in human glioblastoma cell lines using in vitro methodologies. Bremelanotide reduced survivin expression and induced cell death in glioblastoma cells at concentrations that were not toxic to normal human cells. Both of these effects were canceled in the presence of an antagonist of melanocortin receptors 3 and 4, confirming receptor-mediated mechanisms. Bremelanotide-induced cell death was prevented by forced over-expression of survivin in glioblastoma cells, suggesting that bremelanotide induces glioblastoma cell death by inhibiting the expression of survivin, an anti-apoptotic protein. Additionally, bremelanotide promoted cell death induced by chemotherapeutic agents such as temozolomide and osimertinib. The study utilized human glioblastoma cell lines (U-87, GS-Y01, and GS-Y03) and normal human fibroblasts (IMR-90) to assess cell viability, survivin protein expression, and apoptotic markers through western blotting, cell viability assays, and molecular biology techniques.

In plain English

This study discovered that bremelanotide can kill brain cancer cells (glioblastoma) grown in laboratory culture dishes without harming normal cells. The drug works by reducing levels of a protein called survivin that helps cancer cells stay alive. When survivin levels drop, the cancer cells die through a natural cell death process. The researchers proved this by showing that when they artificially increased survivin levels in the cancer cells, bremelanotide could no longer kill them. Importantly, bremelanotide also made standard chemotherapy drugs work better against these brain cancer cells, suggesting it could potentially be used alongside existing cancer treatments.

Structural insights into ligand recognition and activation of the melanocortin-4 receptor

Title: Structural insights into ligand recognition and activation of the melanocortin-4 receptor

Authors: Huibing Zhang, Li-Nan Chen, Dehua Yang, Chunyou Mao, Qingya Shen, Wenbo Feng, Dan-Dan Shen, Antao Dai, Shanshan Xie, Yan Zhou, Jiao Qin, Jin-Peng Sun, Daniel H. Scharf, Tingjun Hou, Tianhua Zhou, Ming-Wei Wang, Yan Zhang

URL: https://www.nature.com/articles/s41422-021-00552-3

Published: Cell Research, 25 August 2021, volume 31, pages 1163–1175

This study reports four high-resolution structures of full-length melanocortin-4 receptor (MC4R) in complex with the heterotrimeric Gs protein stimulated by different ligands, including the FDA-approved drug bremelanotide (Vyleesi™). The structures were determined using single-particle cryo-electron microscopy (cryo-EM), an advanced in vitro structural biology technique that allows visualization of protein complexes at near-atomic resolution. The bremelanotide-MC4R-Gs complex structure was deposited in the Protein Data Bank under accession number 7F55 and Electron Microscopy Data Bank under accession code 31458, at a resolution of 3.1 Ångströms. Together with pharmacological studies, the results reveal the conserved binding mode of peptidic agonists and provide molecular details of agonist recognition underlying receptor subtype selectivity. The study demonstrates a distinct activation mechanism for MC4R, offering new insights into G protein coupling and receptor activation at the molecular level.

In plain English

Scientists used a powerful microscopy technique to take extremely detailed pictures of bremelanotide attached to its target receptor (MC4R) in cells. These images are so detailed that they can see the exact shape and position of individual atoms in the drug-receptor complex. This is like getting a blueprint showing exactly how a key fits into a lock. By understanding the precise three-dimensional structure of how bremelanotide binds to and activates the MC4R receptor, researchers can better understand why the drug works and potentially design improved medications that are more selective and effective. This structural information is now publicly available in scientific databases for other researchers to use in drug development efforts.