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Drug Action

antibiotics, therapeutics and their molecular targets

Medical science has discovered how to modulate the action of molecules that are misbehaving and causing disease. Medicines range from painkillers that block the action of pain-signaling molecules to antibiotics that kill pathogens by blocking their essential molecules. Atomic structures allow medical researchers to improve these drugs and to discover new ones.

Molecule of the Month Articles (33)

Actinomycin

Adrenergic Receptors

Aminoglycoside Antibiotics

Aminoglycoside Antibiotics and Resistance

	Actinomycin Some antibiotics attack cells by intercalating between the bases in a DNA double helix
	Adrenergic Receptors Adrenaline stimulates a G-protein-coupled receptor, priming us for action
	Aminoglycoside Antibiotics Antibiotic-resistant bacteria build enzymes that destroy drugs like streptomycin
	Aminoglycoside Antibiotics and Resistance Bacteria become resistant to aminoglycosides by destroying them or changing their target.
	Anaphase-Promoting Complex / Cyclosome APC/C guards the checkpoints that regulate key steps in the cell cycle
	Beta-secretase Beta-secretase trims proteins in the cell and plays an important role in Alzheimer's disease
	Circadian Clock Proteins Circadian clock proteins measure time in our cells
	Click Chemistry A modular approach to chemistry simplifies the construction of complex protein-targeting molecules.
	Cyclooxygenase Aspirin attacks an important enzyme in pain signaling and blood clotting
	Cytochrome p450 Cytochrome p450 detoxifies and solubilizes drugs and poisons by modifying them with oxygen
	Dihydrofolate Reductase DHFR is a target for cancer chemotherapy and bacterial infection
	Estrogen Receptor Estrogen binds to receptors in the nucleus and affects key genes in development
	Glucocorticoid Receptor and Dexamethasone An anti-inflammatory drug has given us a new way to fight the COVID-19 pandemic.
	Glutamate-gated Chloride Receptors The antibiotic ivermectin attacks glutamate-gated chloride channels, paralyzing parasitic worms.
	Glutathione Transferases Glutathione transferase tags toxic molecules, making them easy to recognize and remove.
	Histone Deacetylases Histone deacetylases regulate access to genetic information by modifying histones
	HIV Envelope Glycoprotein Envelope protein attaches HIV to the cells that it infects and powers fusion of the virus with the cell membrane
	Influenza Neuraminidase Neuraminidase is an important target for influenza drugs
	Integrase HIV integrase allows HIV to insert itself into the genome of an infected cell
	Interferons Interferons mobilize defenses against viral infection
	Lactate Dehydrogenase Our cells temporarily build lactate when supplies of oxygen are low
	Microtubules The largest filaments of the cytoskeleton provide tracks for transport throughout the cell
	Multidrug Resistance Transporters Many bacteria use multidrug resistance transporters to pump drugs and poisons out of the cell
	Neurotransmitter Transporters Neurotransmitters are transported out of nerve synapses to end a signal transmission
	New Delhi Metallo-Beta-Lactamase Antibiotics can save lives, but antibiotic-resistant strains of bacteria pose a dangerous threat
	Nitric Oxide Synthase Nitric oxide gas is used as a rapid-acting hormone and as a powerful defense
	Opioid Receptors Morphine and other opioid drugs bind to receptors in the nervous system, controlling pain
	P-glycoprotein P-glycoprotein pumps toxic molecules out of our cells
	Penicillin-binding Proteins Penicillin attacks the proteins that build bacterial cell walls
	Ribosome Ribosomes are complex molecular machines that build proteins
	Serotonin Receptor Serotonin receptors control mood, emotion, and many other behaviors, and are targets for many important drugs
	Tetrahydrobiopterin Biosynthesis Tetrahydrobiopterin plays an essential role in the production of aromatic amino acids, neurotransmitters and nitric oxide.
	Vancomycin The antibiotic vancomycin blocks the construction of bacterial cell walls.

Learning Resources (18)

Award-winning HIV Enzyme Illustration

(Poster)

How do Drugs Work?

(Flyer)

2016 A Year in Protein-Drug Complexes

(Calendar)

The Ribosome

(Flyer)

	Award-winning HIV Enzyme Illustration Poster Video stills of three HIV enzymes are among the 2016 Winners of FASEB's BioArt Competition. The stills are from a molecular animation created by Maria Voigt and David Goodsell that illustrates A Molecular View of HIV Therapy.
	How do Drugs Work? Flyer PDB structures are used to discuss antibiotics and antivirals, chemotherapy, drug metabolism, drugs of signaling proteins, and lifestyle drugs.
	2016 A Year in Protein-Drug Complexes Calendar PDB structures allow us to see how drugs bind to their protein targets in exquisite detail. Available as a PDF and PowerPoint.
	The Ribosome Flyer This flyer commemorates the 2009 Nobel Prize in Chemistry for studies of the structure and function of the ribosome.
	Glucagon-like Peptide-1 and Diabetes Poster Image of GLP-1 receptor recognizing a GLP-1 analog (yellow) with liraglutide.
	How Do Drugs Work? Poster PDB structures are used to discuss antibiotics and antivirals, chemotherapy, drug metabolism, drugs of signaling proteins, and lifestyle drugs.
	Insulin and Diabetes Poster Structural biology has revealed the details of insulin signaling and how this knowledge is being used to create new and better treatments for diabetes.
	Target Zero: Preventing HIV Transmission Documentary Video Target Zero shows the challenge and emotional complexity of the fight to control HIV infection.
	Immunology and Cancer Video This three-part series explores the human immune response to cancer focusing on cellular and molecular details of the process.
	Ribosomal Subunits GIF Atomic structures of the ribosomal subunits reveal a central role for RNA in protein synthesis. Ribosomes are complex molecular machines that build proteins.
	Opioids and Pain Signaling Video Pain is one of the most trying experiences of life. On the cellular level it is communicated via special neuronal pathways. On the molecular level, however, pain is communicated like any other sensation, via a set of electrical and chemical signals facilitated by complex molecular machinery. These signals can be modulated by opioids, causing us to feel less pain, or no pain at all. Learn how opioids activate the G-proteins which in turn interact with other proteins to edit the pain signal.
	Penicillin and Antibiotic Resistance Video Since its discovery in 1928, penicillin and penicillin-related antibiotics helped save countless lives from bacterial infections. However, in the face of overuse and misuse of antibiotics, bacteria evolved resistance mechanisms that allow them to proliferate even in the presence of the newest antibiotics.
	A Molecular View of HIV Therapy Video After HIV enters a T-cell, three enzymes play essential roles in the life cycle of the virus. Reverse transcriptase copies the viral RNA genome and makes a DNA copy. Integrase inserts this viral DNA into the cell’s DNA. In the last steps of the viral life cycle, HIV protease cuts HIV proteins into their functional parts. Current antiretroviral drugs target these three enzymes, hindering the virus reproduction. However, enzymes can mutate and become drug resistant, making it vital to use a combination of different drugs that target multiple enzymes. This animation was created using many PDB entries for Reverse Transcriptase (3hvt, 3dlk, 3v6d, 3v4i, 3klg, 3v81), Integrase (3os1, 3os0, 3oya), Protease (3pj6, 1kj4, 1hxb, 2az9, 2azc), HIV Polyprotein (1l6n), Capsid Protein (2m8l), and Matrix Protein (1tam).
	Learn about HIV from the RCSB Protein Data Bank Video Use the RCSB PDB Resources to Learn about HIV
	2021 Molecular Mechanisms of Drugs for Mental Disorders Video
	2019 Mechanisms of Bacterial Resistance to Aminoglycoside Antibiotics Video
	Bound! Protein-drug matching game Other Resource Bound! is a card game for students 12 and up, where players compete to match the most drugs to their protein targets.
	Dexamethasone and Cytokine Storms Article Preventing too much of a good thing during SARS-CoV-2 infection

	Diabetes Mellitus - Sitagliptin An oral non-substrate-like DPP-4 inhibitor used for treating diabetes.
	Diabetes Mellitus - Vildagliptin An oral substrate-like DPP-4 inhibitor used for treating diabetes.
	Diabetes Mellitus - Saxagliptin An oral substrate-like DPP-4 inhibitor used for treating diabetes.
	Diabetes Mellitus - Alogliptin An oral xanthine based DPP-4 inhibitor used for treating diabetes.
	Diabetes Mellitus - Linagliptin An oral xanthine based DPP-4 inhibitor used for treating diabetes.
	Diabetes Mellitus - Anagliptin An oral non-substrate-like DPP-4 inhibitor used for treating diabetes.
	Diabetes Mellitus - Acarbose An oral substrate-like glucosidase inhibitor used for treating diabetes.
	Diabetes Mellitus - Miglitol A small molecule glucosidase inhibitor used for treating diabetes.
	Diabetes Mellitus - Rosiglitazone An agonist for PPAR-g receptor used for treating diabetes
	Diabetes Mellitus - Insulin This is a polypeptide hormone, critical for glucose uptake by cells.
	Diabetes Mellitus - Insulin Lispro This designed molecule is a rapid-acting human insulin analog
	Diabetes Mellitus - Insulin Aspart This designed molecule is a rapid-acting human insulin analog
	Diabetes Mellitus - Insulin Detemir This designed molecule is a long-acting human insulin analog
	Diabetes Mellitus - Insulin Degludec This designed molecule is an ultra-long acting human insulin analog

	HIV Testing and Treatment: Current and Upcoming
	Visual Comprehension: HIV-1 Reverse Transcriptase Inhibited by NRTI

	Antibiotics and Ribosome Function
	Lysostaphin
	NDM-1 and Antibiotics
	Superbugs and Antibiotic Resistance

	Excitatory and Inhibitory Synapses Excitatory and Inhibitory Synapses (2018) by David S. Goodsell
	Insulin Action Insulin Action (2016) by David S. Goodsell.

Drug Action

Molecule of the Month Articles (33)

Learning Resources (18)

Curriculum Resources (2)

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Global Health (14)

Goodsell Molecular Landscapes (2)