Pharmaceutical Drugs: Inhibitors and the Nature of Disease

Pharmaceutical Drugs: Inhibitors and the Nature of Disease


Hey it’s professor Dave, let’s learn about pharmaceuticals. We all get sick from time
to time. Whether it’s just a cold, or something more serious, and there’s great
controversy amongst the public about how to treat disease. Some argue that conventional medicine is
best suited to address the health needs of the human body, while others are
skeptical, avoiding the entire system in favor of some kind of alternative. But
before anyone discredits Western medicine, they must understand that all
disease has a molecular basis. Whether the cause is bacterial infection, a
genetic mutation, or anything else, any proposed treatment that does not address
this fundamental cause for the disease is very unlikely to have any merit. So
let’s examine a few types of diseases and the methods that science has come up
with to combat them, which we can refer to as drugs. One category of disease is
genetic disorder. These can be hereditary, passed down from
parent to offspring or they can be the result of a mutation sustained during a
person’s lifetime. These will always involve some change to
DNA that affects the product of gene expression, resulting in a protein with
behavior that deviates from what is normal. If we need to shut down a
particular biochemical process that has gone awry, one solution that we have
stumbled upon in science is the concept of an inhibitor. We know that there are
enzymes and receptors that mediate so much of what goes on in the cell, and
sometimes we may need to silence one of these. An inhibitor is a molecule that
will fit into the active site of, say, an enzyme, and bind either reversibly
through electrostatic interactions or more permanently through covalent bonds,
such that the normal substrate is unable to enter. This kind of inhibition, called
competitive inhibition, prevents the substrate from coordinating and
therefore also prevents the enzyme from performing its function. There is also
noncompetitive inhibition, where a compound binds to the enzyme in some
other location and causes a conformational change that decreases the
active site’s affinity for the substrate. This also disrupts enzymatic function.
Many poisons work this way, and are dangerous because of the important
cellular processes they inhibit. But when an irregular cellular process is doing
harm to the organism, an inhibitor can stop this activity. Inhibitors are
therefore a huge part of the pharmaceutical industry. We have to
recognize that if a disease such as some form of cancer is the direct result of a
genetic mutation and results in either a misbehaving or non-functional
protein, then that is the fundamental cause of the disease. Any potential
solution or cure must specifically address that cause, by somehow
inhibiting the expression of that gene, inhibiting the resulting protein, or some
other similar biochemical strategy. When the cause is this specific, there is
nothing about diet or exercise that can have any impact whatsoever, since your
general health, as important as it is, is not linked to the highly specific origin
of such a disease. That’s why skepticism towards the pharmaceutical industry,
which can certainly be legitimate from a social or economic standpoint, if
misplaced onto the science itself, can have disastrous consequences on the
health of an individual or an entire population. Another application for
inhibitors can be found in the domain of mental health. We learned about
neurotransmitters, and it is the case that molecules like serotonin, dopamine,
and norepinephrine will dictate your mood by transmitting signals through the
synaptic cleft. If these neurotransmitters exist in insufficient
concentrations, it can lead to depression. One solution to this problem is to use a
reuptake inhibitor. This is a molecule that blocks the receptors that reabsorb
some of the neurotransmitter molecules which results in a greater concentration of neurotransmitters in the
synaptic space, and therefore more effective transmission. Once again, the
fundamental cause of the problem is that not enough of a particular molecule is
being transmitted, so a drug that addresses that problem by increasing the
transmission of that molecule one way or another is going to be best suited for
solving that issue. In this way, those who criticize antidepressants as being
merely a chemical solution to a deeper problem are not fully aware of the
specific chemical nature of the problem in the first place. This does not mean psychotropic drugs
are the solution for every mental health issue, but they can be very successful
for certain people. Some diseases are the result of some kind of deficiency in an
essential vitamin or mineral. Take vitamin C, for example. As we now
understand, this molecule, also called L-ascorbic acid, acts as a coenzyme in
certain enzymatic pathways, such as collagen synthesis. Collagen, a structural
protein present in connective tissue, is the most abundant protein in the human
body, and vitamin C is needed to activate the enzyme that performs one of the
steps in synthesizing collagen. If we do not consume enough vitamin C, collagen
synthesis is impaired and we get scurvy, like a pirate on the high seas. The reason this would happen is that
vitamin C is predominantly found in fruits and vegetables, and these tend to
spoil during a long journey. A vitamin is therefore just a molecule that we need
to ingest for proper cellular function because we can no longer synthesize it
ourselves, as the ability was lost somewhere over the course of biological
evolution. But plants still make all these nutrients, so as long as we eat the
plants we will be just fine. The amazing feat of modern chemistry is
to recognize the link between a disease like scurvy and a molecule like ascorbic
acid, and furthermore to know the structure of this molecule such that we
can build it ourselves, and offer it in the form of supplements to
those who do not have access to the whole foods that contain them. Contrary to popular belief, there can be
absolutely no difference between a molecule of ascorbic acid found in a
fruit and one made in a lab, because they are identical arrangements of precisely
the same atoms. It is the shape of a molecule that causes its bioactivity, not
its source. Another category of disease is the pathogenic. A pathogen is any
microorganisms that can cause disease like bacteria or viruses. Most bacteria
are harmless or even beneficial to the human body, but there are some that cause
infectious diseases, like tuberculosis or pneumonia. It was not that long ago that we were
completely unaware that these organisms even existed. But once we realized that
they were responsible for certain diseases, our studies of these organisms
led to the invention of antibiotics, which can kill certain bacteria. Many of
these operate on the basis of a difference between bacterial cell
structure and human cell structure. Bacterial cells possess a cell wall made
of a substance called peptidoglycan, which human cells do not possess. The
first antibiotic ever discovered, penicillin, inhibits a bacterial enzyme
that is used to regenerate the cell wall. So in the presence of the drug the cell
wall of bacterial cells will rupture, spilling their contents and thus killing
the bacteria. Antibiotics like penicillin and others that followed have almost
single-handedly doubled the human lifespan. Viruses, however, have different
structures and mechanisms of survival from bacterial cells, as viruses are not
cells at all, they are much tinier and operate by inserting their genetic
material into a host cell, hijacking the cellular machinery, and forcing it to
generate more viruses, while typically destroying the cell in the process. Thus,
antibiotics do not work on viruses. Instead, vaccines have proven effective
in training the human body to prepare a response to certain types of viruses
by introducing a piece of the virus so that the immune system can recognize and
remember it for optimal future response. This is how we have largely eradicated
many diseases like smallpox, polio, and measles. However, again, skepticism of vaccination
threatens to facilitate the return of some of these diseases. For other viruses
a more complex approach is required, but any legitimate antiviral drug will
disarm some biochemical process that the virus relies on. For example, in order to
invade a host cell, receptors on the virus must recognize certain receptors
on the cell. If inhibitors are introduced that block either of these receptors, the
virus will not be able to enter and reproduce. Other drugs can inhibit the
transcription of viral DNA once it is inside the cell. And ribozymes are
specially designed enzymes that can target viral DNA and chop it up so it
can’t be transcribed. Whatever the case may be, any legitimate treatment must be
preceded by a sophisticated knowledge of the biochemistry involved. By contrast, some diseases are strictly
physiological, like many forms of cardiovascular disease. These involve the
heart or blood vessels and can occur because of poor diet, lack of exercise, or
other lifestyle factors. These are the ones in which a holistic approach to
general health can be effective in preventing, but there are also
medications that offer some assistance. All of these systems will be covered in
greater detail in the upcoming biology series. So we must understand that in
order to treat a disease, it is imperative that we understand how it
operates on the cellular and molecular level, and then come up with a strategy
that addresses some detail on one of these levels. That is the approach of
pharmaceutical drugs, which are specially designed molecules that can inhibit
specific biochemical processes. This allows us to eliminate pathogens,
silence mutant enzymes, and more. If by blind chance an ancient tradition has discovered a food
or plant that has legitimate medicinal properties, which is certainly possible
since humans have been curious and bold enough to try things far before we
understood chemistry, that substance has those medicinal properties because it
contains an active ingredient, some molecule inside it that performs a
biochemical function similar to the strategies we have discussed, not because
the plant as a whole is sacred or magic. Everything in your body is made of
molecules, and every biological process involves the interaction of those
molecules. Unfortunately, most people do not have a background in chemistry and
biochemistry so when trying to make assessments about
health and medical treatment they must simply go by what they have heard. But
there is a lot of misinformation out there, whether it is genuine
misunderstanding or deliberate manipulation for financial gain. A
vilification of Western medicine is a popular meme that leads people away from
legitimate medical treatment, as they instead opt for alternative medicines
with no real impact other than a placebo effect, which can be enough to cure your
headache, but will never cure your cancer. Luckily, as you continue to build your
understanding of science, you won’t be so easily manipulated. Thanks for watching, guys. Subscribe to my channel for more tutorials, and as always, feel free to email me:

17 Replies to “Pharmaceutical Drugs: Inhibitors and the Nature of Disease”

  1. Perfect timing! I'm taking pharmacology right now.We are talking about the cardiovascular system and the drugs that affect it like chronotropes and anti-arrhythmic drugs.

  2. Near start: scientific basis, not "molecular", and point out the fact that the symptoms can be observed and accurately theorized, and accurate predictions made towards death on all diseases.

  3. Nice video, could you please upload more videos about organic chem? for example aromatic substitution and etc? thx <3

  4. wonderful professor….my chemistry classes are quite cheap despite the poor illustration by my lecturers and its all because of your gifted you tube tutorials….thnks man

  5. can you please also make videos about pharmacokinetics and pharmacodynamics wiht examples? a lot of students struggle with this. Thank you for your great work!!

  6. many people have chronic pain, resulting from an injury such as spinal injury. This form of 'disease' is a mechanical problem such as a spinal bone or disc joint, inpinging on a nerve/ spinal cord, which then causes disease on a 'molecular basis', by causing pain signals. This pain causes disability by reducing movement/ muscle loss/ arthritis in joints. and ultimately depression. Depression caused by many years of this physical pain and disability can not be treated by any pharmaceuticals such as anti depressants. Stem cell treatment to regrow damaged nerves, is the only hope for chronic nerve disease. Damaged nerve cells in the central nervous system (CNS), do not repair, because these cells do not divide. These CNS cells in the: brain- spinal cord- spinal nerve roots, are the same cells you have as an embryo. These CNS cells grow larger as you grow, but have little repair capacity, if damaged. Many human trials are now underway with stem cells. Hopefully stem cells will regenerate nerve signals in damaged CNS.

  7. Great video! Just wanted to add that the validity of scientific claims should always be investigated with healthy science-based skepticism. Even professionals sometimes make mistakes.

  8. Well explained video Prof. Congratulations. But being so much educated and knowledgeable, you failed to know the truth of the alternative system of medicine, Homeopathy. I am surprised and sorry for that. In the past few years, the scientists are working on the molecular mechanism of homoeopathic medicines in vitro as well as in vivo. The results are positive. So I guess you cannot have a placebo effect on cell lines and animals! Kindly search through the scholarly journals about the effect of homoeopathic ultra high diluted medicine on the treatment of cancers. Also refer to the papers on nano-particles in these ultra high dilutions by scientists of chemical engineering.

    Sincere request to not to spread rumours without having full knowledge on a science.

    Teixeira MZ. Proofs that homeopathic medicine works: dossier

    “scientific evidence for homeopathy” (Revista de Homeopatia, São

    Paulo HomeopathicMedical Association). Homeopathy 2018;107:45

    2 Teixeira MZ. Special dossier: “Scientific Evidence for Homeopathy”.

    Rev Assoc Med Bras (1992) 2018;64:93–94

    Khuda-Bukhsh AR. Potentized homoeopathic drugs act through

    regulation of gene-expression: a hypothesis to explain their

    mechanism and pathways of action in vitro. Complement Ther

    Med 1997;5:43–46

    Khuda-Bukhsh AR. Towards understanding molecular mechanisms of action of homeopathic drugs: an overview. Mol Cell

    Biochem 2003;253:339–345

    Khuda-Bukhsh AR. Current trends in high dilution research with

    particular reference to gene regulatory hypothesis. Nucleus 2014;

    57:3–17

    Kay PH, Khuda-Bukhsh AR. The contribution of homeogenomic and

    homeogenetic studies in the support of the practice of homoeopathy. Indian J Res Homoeopathy 2016;10:101–107

    Dei A, Bernardini S. Hormetic effects of extremely diluted

    solutions on gene expression. Homeopathy 2015;104:116–122

    Bellavite P, Signorini A, Marzotto M, Moratti E, Bonafini C, Olioso

    D. Cell sensitivity, non-linearity and inverse effects. Homeopathy

    2015;104:139–160

    Bigagli E, Luceri C, Bernardini S, Dei A, Filippini A, Dolara P. Exploring

    the effects of homeopathic Apis mellifica preparations on human

    gene expression profiles. Homeopathy 2014;103:127–132

    Marzotto M, Olioso D, Brizzi M, Tononi P, Cristofoletti M, Bellavite

    P. Extreme sensitivity of gene expression in human SH-SY5Y

    neurocytes to ultra-low doses of Gelsemium sempervirens.

    BMC Complement Altern Med 2014;14:104

    Olioso D, Marzotto M, Moratti E, Brizzi M, Bellavite P. Effects of

    Gelsemium sempervirens L. on pathway-focused gene expression

    profiling in neuronal cells. J Ethnopharmacol 2014;153:535–539

    Marzotto M, Olioso D, Bellavite P. Gene expression and highly

    diluted molecules. Front Pharmacol 2014;5:237

    Preethi K, Ellanghiyil S, Kuttan G, Kuttan R. Induction of apoptosis

    of tumor cells by some potentiated homeopathic drugs: implications on mechanism of action. Integr Cancer Ther 2012;

    11:172–182

    Frenkel M, Mishra BM, Sen S, et al. Cytotoxic effects of ultra-diluted

    remedies on breast cancer cells. Int J Oncol 2010;36:395–403

    Samadder A, Das S, Das J, Paul A, Boujedaini N, Khuda-Bukhsh AR.

    The potentized homeopathic drug, Lycopodium clavatum (5C and

    15C) has anti-cancer effect on HeLa cells in vitro. J Acupunct

    Meridian Stud 2013;6:180–187

    Arora S, Aggarwal A, Singla P, Jyoti S, Tandon S. Anti-proliferative

    effects of homeopathic medicines on human kidney, colon and

    breast cancer cells. Homeopathy 2013;102:274–282

    Bishayee K, Sikdar S, Khuda-Bukhsh AR. Evidence of an epigenetic

    modification in cell-cycle arrest caused by the use of ultra-highlydiluted Gonolobus condurango extract. J Pharmacopuncture

    2013;16:7–13

    Sikdar S, Kumar Saha S, Rahman Khuda-Bukhsh A. Relative

    apoptosis-inducing potential of homeopathic Condurango 6c

    and 30c in h460 lung cancer cells in vitro: apoptosis-induction

    by homeopathic Condurango in h460 cells. J Pharmacopuncture

    2014;17:59–69

    Arora S, Tandon S. DNA fragmentation and cell cycle arrest: a

    hallmark of apoptosis induced by Ruta graveolens in human colon

    cancer cells. Homeopathy 2015;104:36–47

    Saha S, Bhattacharjee P, Guha D, et al. Sulphur alters NFκB-p300

    cross-talk in favour of p53-p300 to induce apoptosis in non-small

    cell lung carcinoma. Int J Oncol 2015;47:573–582

    Hope that's enough proof that homoeopathy works at the molecular level and also in cancers.

    Best regards

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